Patents by Inventor Mitsuhiro Wakimasu
Mitsuhiro Wakimasu 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: 6610655Abstract: Cyclic pentapeptides are disclosed having the following formula (I)-Cyclo(-A1-A2-A3-A4-A5-)-wherein A1, A2, A3, A4 and A5 are amino acid residues. The pentapeptide has amino acid residues in positions 1-2-3 to form a &ggr;-turn, and amino acid residues in positions 3-4-5-1 to form a &bgr;-turn in combination with the &ggr;-turn. D-&agr;-amino acid residues are selected for A1, A3, and A5 and L-&agr;-amino acid residues are selected for A2 and A4. Compounds having &ggr;-turns and &bgr;-turns can be synthesized, regardless of the kinds of amino acid residues, and it is possible to synthesize compounds in which desired amino acid residues are introduced into sites of &bgr;-turn and &ggr;-turn based on their importance from the viewpoint of biological activity. The present invention is therefore available for design of compounds having biological activity.Type: GrantFiled: November 15, 2001Date of Patent: August 26, 2003Assignee: Takeda Chemical Industries, Inc.Inventors: Mitsuhiro Wakimasu, Hiroshi Inooka, Satoshi Endo, Takashi Kikuchi
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Publication number: 20020168337Abstract: According to a first embodiment, there is provided a sustained-release preparation comprising a water-insoluble or slightly water-soluble polyvalent metal salt of a water-soluble physiologically active substance which is not an endothelin antagonist, and a biodegradable polymer. The sustained-release preparation of the first embodiment is highly efficient in incorporating the water-soluble physiologically active substance and suppresses the initial burst of the water-soluble physiologically active substance. The sustained-release preparation of the present invention is capable of releasing the water-soluble physiologically active substance while retaining its bioactivity after administration in vivo. Furthermore, the water-soluble physiologically active substance in the sustained-release preparation is kept stable for a long period of time, with little loss of bioactivity.Type: ApplicationFiled: May 2, 2002Publication date: November 14, 2002Applicant: TAKADA CHEMICAL INDUSTRIES LTD.Inventors: Yasutaka Igari, Yutaka Yamagata, Satoshi Iinuma, Hiroaki Okada, Hitoshi Ikeda, Masao Tsuda, Kazumichi Yamamoto, Mitsuhiro Wakimasu
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Publication number: 20020115823Abstract: Cyclic pentapeptides having a &ggr;-turn and a &bgr;-turn wherein the cyclic pentapeptide has the following formula (I);Type: ApplicationFiled: November 15, 2001Publication date: August 22, 2002Inventors: Mitsuhiro Wakimasu, Hiroshi Inooka, Satoshi Endo, Takashi Kikuchi
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Publication number: 20020058622Abstract: According to a first embodiment, there is provided a sustained-release preparation comprising a water-insoluble or slightly water-soluble polyvalent metal salt of a water-soluble physiologically active substance which is not an endothelin antagonist, and a biodegradable polymer. The sustained-release preparation of the first embodiment is highly efficient in incorporating the water-soluble physiologically active substance and suppresses the initial burst of the water-soluble physiologically active substance. The sustained-release preparation of the present invention is capable of releasing the water-soluble physiologically active substance while retaining its bioactivity after administration in vivo. Furthermore, the water-soluble physiologically active substance in the sustained-release preparation is kept stable for a long period of time, with little loss of bioactivity.Type: ApplicationFiled: November 6, 2001Publication date: May 16, 2002Inventors: Yasutaka Igari, Yutaka Yamagata, Satoshi Iinuma, Hiroaki Okada, Hitoshi Ikeda, Masao Tsuda, Kazumichi Yamamoto, Mitsuhiro Wakimasu
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Patent number: 6346604Abstract: Cyclic pentapeptides having a &ggr;-turn and a &bgr;-turn wherein the cyclic pentapeptide has the following formula (I): Cyclo(—A1—A2—A3—A4—A5—) (I) wherein A1, A2, A3, A4 and A5 are amino acid residues; said pentapeptide having amino acid residues in positions 1-2-3 to form a &ggr;-turn, and amino acid residues in positions 3-4-5-1 to form a &bgr;-turn in combination with the &ggr;-turn; in which D-&agr;-amino acid residues are selected for A1, A3 and A5 and L-&agr;-amino acid residues are selected for A2 and A4 or wherein L-&agr;-amino acid residues are selected for A1, A3 and A5 and D-&agr;-amino acid residues are selected for A2 and A4; are provided.Type: GrantFiled: November 12, 1997Date of Patent: February 12, 2002Assignee: Takeda Chemical Industries, Inc.Inventors: Mitsuhiro Wakimasu, Hiroshi Inooka, Satoshi Endo, Takashi Kikuchi
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Patent number: 6147051Abstract: Compounds having antagonistic activity on endothelin receptors can be effectively used for prophylaxis and/or treatment of hypofunction of organs which occurs in their surgery or transplant.Type: GrantFiled: November 21, 1995Date of Patent: November 14, 2000Assignee: Takeda Chemical Industries Ltd.Inventors: Toshifumi Watanabe, Mitsuhiro Wakimasu, Chieko Kitada
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Patent number: 5965526Abstract: Cyclic pentapeptides are disclosed having the following formula (I) --Cyclo(-A.sub.1 -A.sub.2 -A.sub.3 -A.sub.4 -A.sub.5 -)-- wherein A.sub.1, A.sub.2, A.sub.3, A.sub.4 and A.sub.5, are amino acid residues. The pentapeptide has amino acid residues in positions 1-2-3 to form a .gamma.-turn, and amino acid residues in positions 3-4-5-1 to form a .beta.-turn in combination with the .gamma.-turn. D-.alpha.-amino acid residues are selected for A.sub.1, A.sub.3, and A.sub.5 and L-.alpha.-amino acid residues are selected for A.sub.2 and A.sub.4. Compounds having .gamma.-turns and .beta.-turns can be synthesized, regardless of the kinds of amino acid residues, and it is possible to synthesize compounds in which desired amino acid residues are introduced into sites of .beta.-turn and .gamma.-turn based on their importance from the viewpoint of biological activity. The present invention is therefore available for design of compounds having biological activity.Type: GrantFiled: October 31, 1995Date of Patent: October 12, 1999Assignee: Takeda Chemical Industries, Inc.Inventors: Mitsuhiro Wakimasu, Hiroshi Inooka, Satoshi Endo, Takashi Kikuchi
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Patent number: 5948754Abstract: A cyclic hexapeptide represented by the formula:cyclo?A--Asp(R.sup.1)--Y--NH--CHR.sup.2 --CO--C--D--Trp(N.sup.in --R.sup.3)--! (I)wherein A is a D-acidic-.alpha.-amino acid residue; Y is an acidic-.alpha.-amino acid residue; C is an L-.alpha.-amino acid residue; R.sup.1 is a group represented by the formula: ##STR1## wherein X.sup.1 and X.sup.2 are independently H, C.sub.1-6 alkyl, C.sub.1-6 alkoxy, halogen or nitro, and may bind together to form a ring in cooperation with the adjacent carbon atom; R.sup.2 is C.sub.1-6 alkyl, C.sub.3-7 cycloalkyl, C.sub.3-7 cycloalkyl-C.sub.1-3 alkyl, C.sub.1-6 alkylthio-C.sub.1-3 alkyl, C.sub.3-7 cycloalkylthio-C.sub.1-3 alkyl, C.sub.1-5 alkoxy-C.sub.1-3 alkyl, C.sub.3-7 cycloalkoxy-C.sub.1-3 alkyl, C.sub.1-6 alkylthio, C.sub.3-7 cycloalkylthio, C.sub.1-5 alkoxy or C.sub.3-7 cycloalkoxy; R.sup.3 is H, C.sub.1-6 alkyl, C.sub.3-7 cycloalkyl, --COR.sup.4, --COOR.sup.5 or --CONHR.sup.6 ; when X.sup.1, X.sup.2 and R.sup.3 are all hydrogen atoms, R.sup.Type: GrantFiled: October 30, 1996Date of Patent: September 7, 1999Assignee: Takeda Chemical Industries, Ltd.Inventors: Mitsuhiro Wakimasu, Takashi Kikuchi, Akira Kawada
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Patent number: 5883075Abstract: Disclosed are (1) a cyclic hexapeptide represented by formula I or a salt thereof: ##STR1## wherein X and Y each represent .alpha.-amino acid residues, A represents a D-acidic-.alpha.-amino acid residue, B represents a neutral-.alpha.-amino acid residue, C represents an L-.alpha.-amino acid residue and D represents a D-.alpha.-amino acid residue having an aromatic ring group; and (2) a pharmaceutical composition comprising the peptide represented by formula I or a pharmaceutically aceptable salt thereof as an active ingredient.Type: GrantFiled: July 9, 1996Date of Patent: March 16, 1999Assignee: Takeda Chemical Industries, Ltd.Inventors: Mitsuhiro Wakimasu, Takashi Kikuchi, Akira Kawada, Hideo Shirafuji
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Patent number: 5753619Abstract: Cyclic hexapeptides having antagonistic activity on endothelin receptors of the formula ?I!: ##STR1## wherein X and Y each is an .alpha.-amino acid residue having D-, L-form or DL-form, A is a D-acidic-.alpha.-amino acid residue, B is a neutral-.alpha.-amino acid residue having D- or L-form, C is an L-.alpha.-amino acid residue and E is a D-.alpha.-amino acid residue having an aromatic ring group can be effectively used for prophylaxis and/or treatment of pulmonary circulatory diseases.Type: GrantFiled: November 29, 1995Date of Patent: May 19, 1998Assignee: Takeda Chemical Insustries, Ltd.Inventors: Toshifumi Watanabe, Keiji Kusumoto, Mitsuhiro Wakimasu
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Patent number: 5616684Abstract: Cyclic peptides and their salts have antagonistic activity on endothelin receptors and antagonistic activity on NK2 receptors. The peptides have the formula ##STR1## wherein X and Y each represent .alpha.-amino acid residues, A represents a D-acidic-.alpha.-amino acid residue, B represents a neutral .alpha.-amino acid residue, C represents an L-.alpha.-amino acid residue and D represents a D-.alpha.-amino acid residue having an aromatic ring group; wherein hydroxy, thiol, amino, imino and carboxyl groups can be substituted or unsubstituted. Pharmaceutical compositions containing such peptides are also described.Type: GrantFiled: April 20, 1994Date of Patent: April 1, 1997Assignee: Takeda Chemical Industries, Ltd.Inventors: Mitsuhiro Wakimasu, Takashi Kikuchi, Akira Kawada, Hideo Shirafuji
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Patent number: 5478809Abstract: A compound of the formula: ##STR1## wherein each R.sup.1, R.sup.2 and R.sup.3 is an aliphatic acyl group, X is an amino acid sequence consisting of 1 to 5 amino acid residues which contain at least one acidic amino acid residue, n is an integer of 0 to 4, provided that when n is 0, X has glutamyl-glycyl at its N-terminal and when n is 1 or 2, the acidic amino acid residue is an acidic amino acid residue other than D-glutamyl, or a salt thereof has an activity of remarkably improving anhematopoiesis and is useful as an immuno-stimulating agent having a leukocyte-increasing activity.Type: GrantFiled: December 28, 1993Date of Patent: December 26, 1995Assignee: Takeda Chemical Industries, Ltd.Inventors: Seiichi Tanida, Tsuneaki Hida, Mitsuhiro Wakimasu
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Patent number: 5478808Abstract: A compound of the formula: ##STR1## wherein each of R.sup.1 and R.sup.2 is hydrogen or aliphatic acyl, A is amino which may be protected, X is an amino acid sequence consisting of 1 to 10 amino acid residues which contain at least one amino acid residue having a water-solubility enhancing group, or a salt thereof has an activity of remarkably improving hematopoietic disorder and is useful as an immuno-stimulating agent or an agent for treating thrombocytopenia.Type: GrantFiled: December 28, 1993Date of Patent: December 26, 1995Assignee: Takeda Chemical Industries, Ltd.Inventors: Seiichi Tanida, Tsuneaki Hida, Mitsuhiro Wakimasu, Setsuo Harada, Koichi Yukishige
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Patent number: 5352659Abstract: Disclosed are a peptide represented by formula (I) or a pharmaceutically acceptable salt thereof: ##STR1## wherein M represents a mercaptoacyl group; P, Q, R, S, T, U, V, W, X, Y and Z each represent amino acid residues, wherein an amino acid side chain of Y is either a substituted saturated aliphatic hydrocarbon group having 1 to 15 carbon atoms or an unsubstituted saturated aliphatic hydrocarbon group having 4 to 15 carbon atoms other than (1S)-1-methylpropyl; (2) a method for producing the above-mentioned peptide or the salt thereof, which comprises subjecting a peptide represented by formula (II) or a salt thereof to an oxidation reaction:M-P-Cys-Q-R-S-T-Asp-U-Glu-Cys-Val-Tyr-V-Cys-His-W-X-Y-Ile-Z-OH(II)wherein M, P, Q, R, S, T, U, V, W, X, Y and Z are as diefined above; and (3) use of the above-mentioned peptide or the pharmaceutically acceptable salt thereof as an anti-endothelin agent.Type: GrantFiled: February 14, 1992Date of Patent: October 4, 1994Assignee: Takeda Chemical IndustriesInventors: Mitsuhiro Wakimasu, Takashi Kikuchi, Kazuki Kubo
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Patent number: 5330978Abstract: A phosphonic acid derivative compound represented by formula [I ] or a pharmaceutically acceptable salt thereof: ##STR1## wherein R.sub.1, R.sub.2 and R.sub.3 each represent hydrocarbon groups which may be substituted, except cases in which (1) R.sub.2 is unsubstituted methyl, ( 2 ) R.sub.3 is an unsubstituted hydrocarbon group having 1 to 3 carbon atoms, and (3) R.sub.1 is benzyloxycarbonylaminomethyl, R.sub.2 is isobutyl and R.sub.3 is isobutyl or phenylmethyl, which has endothelin-converting enzyme inhibiting activity and is useful as pharmaceutical drugs such as therapeutic agents for hypertension, cardiac or cerebral circulatory diseases and renal diseases.Type: GrantFiled: June 3, 1992Date of Patent: July 19, 1994Assignee: Takeda Chemical Industries, Ltd.Inventors: Mitsuhiro Wakimasu, Masaaki Mori, Akira Kawada
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Patent number: 5306808Abstract: Disclosed are a peptide derivative represented by the formula [I] or a pharmaceutically acceptable salt thereof: ##STR1## wherein A, B, C, D, E and F each represent amino acid residues, and satisfy any one condition of (i) A=Ser, B=Ser, C=Ser, D=Leu, E=Met and F=Phe, (ii) A=Ser, B=Ser, C=Ser, D=Trp, E=Leu and F=Phe, and (iii) A=Thr, B=Phe, C=Thr, D=Tyr, E=Lys and F=Tyr; and W, X, Y and Z each represent amino acid residues, and satisfy any one condition of (i) at least one of W and Y is an amino acid residue other than an L-alanine residue or other than an L-cysteine residue, (ii) X is an amino acid residue other than an L-Lysine residue, and (iii) Z is an amino acid residue other than an L-aspartic acid residue; (2) a method for producing the peptide derivative or the salt thereof; and (3) an agent for improving a circulatory function mainly comprising the peptide derivative or the salt thereof, such as a vasodilator or a vasoconstrictor.Type: GrantFiled: October 17, 1991Date of Patent: April 26, 1994Assignee: Takeda Chemical Industries, Ltd.Inventors: Mitsuhiro Wakimasu, Takashi Kikuchi, Kazuki Kubo
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Patent number: 5159061Abstract: A peptide derivative of the formula ##STR1## wherein A is hydrogen or a hydrocarbon acyl having 2 to 18 carbon atoms which is substituted by an amino group at the .alpha.-position; B is F-Gly wherein F is a neutral .alpha.-amino acid residue, or NH-(CH.sub.2)nCO wherein n is an integer of 1 to 4; C is a neutral .alpha.-amino acid residue; and E is L-Arg or D-Arg; when A, B and C are hydrogen, Gly-Gly, and Met or Ile, respectively, E is D-Arg, or its pharmacologically acceptable salt has strong hypotensive and natriuretic activity; therefore it is useful as a therapeutic drug for hypertension, a diuretic, and a therapeutic drug for cardiac and cerebral circulatory diseases.Type: GrantFiled: September 25, 1987Date of Patent: October 27, 1992Assignee: Takeda Chemical Industries, Ltd.Inventors: Masahiko Fujino, Mitsuhiro Wakimasu, Kohei Nishikawa
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Patent number: 4748154Abstract: A peptide derivative of the general formula ##STR1## wherein R.sup.1 is a hydrogen atom, a C.sub.1-18 alkyl group or a substituted or unsubstituted phenyl C.sub.1-3 alkyl group;A is an amino or N--C.sub.1-6 alkylamino acid residue;B is a hydroxyl group, a substituted or unsubstituted amino group, or an amino acid or an amide thereof,or a physiologically acceptable salt thereof, can be advantageously used for the treatment and/or prevention of a disease including, among others, senile dementia (Alzheimer's dementia), cerebrovascular dementia, Alzheimer's disease, Pick's disease, Huntington's chorea, Creutzfeldt-Jakob disease, Parkinson's disease, and dementia due to spinocerebellar degeneration.Type: GrantFiled: December 8, 1986Date of Patent: May 31, 1988Assignee: Takeda Chemical Industries, Ltd.Inventors: Giichi Goto, Akinobu Nagaoka, Mitsuhiro Wakimasu
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Patent number: 4681848Abstract: The invention relates to novel polypeptide of the formula ##STR1## wherein X is a bond, or a peptide or amino acid residue 1 to 16 amino acids counting from the C terminus of the peptide chain of ##STR2## and Y is a peptide or amino acid residue having 1 to 5 amino acids counting from the N terminus of the peptide chain of ##STR3## and conjugate between the same and a carrier protein, as well as hydridoma and monoclonal antibody derived by the use of the polypeptide or the conjugate, and a method of detecting and of purifying human gamma-interferon using the antibodies.Type: GrantFiled: September 20, 1983Date of Patent: July 21, 1987Assignee: Takeda Chemical Industries, Ltd.Inventors: Kyozo Tsukamoto, Yuzo Ichimori, Mitsuhiro Wakimasu
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Patent number: RE35886Abstract: A phosphonic acid derivative compound represented by formula ?I ! or a pharmaceutically acceptable salt thereof: ##STR1## wherein R.sub.1, R.sub.2 and R.sub.3 each represent hydrocarbon groups which may be substituted, except cases in which (1) R.sub.2 is unsubstituted methyl, ( 2 ) R.sub.3 is an unsubstituted hydrocarbon group having 1 to 3 carbon atoms, and (3) R.sub.1 is benzyloxycarbonylaminomethyl, R.sub.2 is isobutyl and R.sub.3 is isobutyl or phenylmethyl, which has endothelin-converting enzyme inhibiting activity and is useful as pharmaceutical drugs such as therapeutic agents for hypertension, cardiac or cerebral circulatory diseases and renal diseases.This is a Reissue of a Patent which was the subject of a Reexamination Certificate No. B1 5,330,978, dated Jun. 18, 1996, Request No. 90/00400, Oct. 18, 1995.Type: GrantFiled: July 12, 1996Date of Patent: September 1, 1998Assignee: Takeda Chemical Industries, Ltd.Inventors: Mitsuhiro Wakimasu, Masaaki Mori, Akira Kawada