Patents by Inventor Hirosada Sugihara

Hirosada Sugihara 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: 5550131
    Abstract: Compounds of the formula ##STR1## wherein A represents amidino group or an optionally substituted aminoethyl; R.sup.10 represents one species selected from a group consisting of nitro group, a halogen atom, a lower alkenyl group, a lower alkynyl group, a lower alkyloxycarbonyl group and a group represented by the formula OR.sup.11 (wherein R.sup.11 is hydrogen atom or a lower alkyl group, a lower alkenyl group, a lower alkynyl group, a lower alkanoyl group, a carbamoyl group or a methanesulfonyl group, each of which may be substituted; R.sup.12 and R.sup.13 respectively represent hydrogen atom, hydroxyl group, a lower alkoxy group or a halogen atom; X represents hydroxyl group, p-hydroxyphenyl group or an optionally esterified or amidated carboxyl group; Y represents an optionally esterified or amidated carboxyl group; and n denotes 1 or 2, or a salt thereof and an agent for inhibiting adhesion of cells which comprise these compounds are desclosed.
    Type: Grant
    Filed: June 17, 1994
    Date of Patent: August 27, 1996
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Hirosada Sugihara, Zenichi Terashita, Hideto Fukushi
  • Patent number: 5294713
    Abstract: The compounds of the formula ##STR1## wherein G stands for an amidino group or an optionally cyclic amino group, these being respectively optionally substituted; D stands for a spacer having 2 to 6 atomic chain optionally bonded through a hetero-atom and/or a 5- to 6-membered ring (provided that the 5- to 6-membered ring is, depending on its bonding position, counted as 2 to 3 atomic chains); R.sup.1 stands for hydrogen, benzyl group or a lower alkyl group; R.sup.2 and R.sup.3 independently stand for a residual group formed by removing --CH(NH.sub.2)COOH from an .alpha.-amino acid, or R.sup.1 and R.sup.2 may form a 5- to 6-membered ring taken together with the adjacent N and C; X stands for hydrogen or an optionally substituted lower alkyl group; and Z stands for a group capable of forming an anion or a group convertible into an anion in a living body, or salts thereof and agents for inhibiting cell-adhesion, which are characterized by containing these compounds.
    Type: Grant
    Filed: August 7, 1992
    Date of Patent: March 15, 1994
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Hirosada Sugihara, Zenichi Terashita
  • Patent number: 4997836
    Abstract: Novel trisubstituted piperazine compounds of the formula (I) and pharmaceutically acceptable salts thereof: ##STR1## wherein R.sup.1, R.sup.2 and R.sup.
    Type: Grant
    Filed: November 9, 1989
    Date of Patent: March 5, 1991
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Hirosada Sugihara, Kohei Nishikawa
  • Patent number: 4954625
    Abstract: Novel compounds of the formula: ##STR1## [wherein A is an .alpha.-amino acid residue; B is a group represented by the formula: ##STR2## wherein R.sup.4 is hydrogen, lower alkyl, aralkyl or amino-lower alkyl), whereby the linkage between the symbols A and B designates a peptide bond and the group R.sup.4 in B may be linked with A; R.sup.1 is hydrogen, lower alkyl or aralkyl; R.sup.2 is hydrogen, lower alkyl, aralkyl or acyl; X is alkylene] and salts thereof posses, for example, inhibitory activity on angiotensin converting enzyme, and are useful as an agent for diagnosis, prevention or treatment of hypertension as well as circulatory diseases such as cardiopathy and cerebral apoplexy.
    Type: Grant
    Filed: August 30, 1989
    Date of Patent: September 4, 1990
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Hirosada Sugihara, Kohei Nishikawa, Katsumi Ito
  • Patent number: 4937246
    Abstract: Platelet Activating Factor (PAF) antagonists which comprise the compounds of the formula (I): ##STR1## wherein A is an optionally substituted phenyl or an optionally substituted heterocyclic group; X is methylene group, carbonyl group or thiocarbonyl group; R.sup.1, R.sup.2 and R.sup.3 are independently a lower alkyl group, and their salts are excellent in absorption from the intestinal canal.Among the compounds of the formula (I), those wherein A is an optionally substituted 2,3-dihydro-1-benzoxepin-4-yl group are novel compounds and exhibit excellent PAF antagonism.
    Type: Grant
    Filed: November 22, 1988
    Date of Patent: June 26, 1990
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Hirosada Sugihara, Katsumi Itoh, Kohei Nishikawa
  • Patent number: 4880809
    Abstract: Novel 1,4-disubstituted piperazine compounds represented by the formula (I): ##STR1## wherein A is a condensed polycyclic hydrocarbon group;R is a phenyl group substituted with a lower alkoxy group;X is methylene group, carbonyl group or thiocarbonyl group;and m is 2 or 3, and their saltsare useful as a platelet activating factor antagonist.
    Type: Grant
    Filed: March 14, 1988
    Date of Patent: November 14, 1989
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Hirosada Sugihara, Katsumi Itoh, Kohei Nishikawa
  • Patent number: 4871842
    Abstract: Novel compounds of the formula: ##STR1## [wherein A is an .alpha.-amino acid residue; B is a group represented by the formula: ##STR2## (wherein R.sup.4 is hydrogen, lower alkyl, aralkyl or amino-lower alkyl), whereby the linkage between the symbols A and B designates a peptide bond and the group R.sup.4 in B may be linked with A; R.sup.1 is hydrogen, lower alkyl or aralkyl; R.sup.2 is hydrogen, lower alkyl, aralkyl or acyl; X is alkylene] and salts thereof possess, for example, inhibitory activity on angiotensin converting enzyme, and are useful as an agent for diagnosis, prevention or treatment of hypertension as well as circulatory diseases such as cardiopathy and cerebral apoplexy.
    Type: Grant
    Filed: July 14, 1988
    Date of Patent: October 3, 1989
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Hirosada Sugihara, Kohei Nishikawa, Katsumi Ito
  • Patent number: 4816466
    Abstract: Novel Compounds of the formula: ##STR1## [wherein A is an .alpha.-amino acid residue; B is a group represented by the formula: ##STR2## (wherein R.sup.4 is hydrogen, lower alkyl, aralkyl or amino-lower alkyl), whereby the linkage between the symbols A and B designates a peptide bond and the group R.sup.4 is B may be linked with A; R.sup.1 is hydrogen, lower alkyl or aralkyl; R.sup.2 is hydrogen, lower alkyl, aralkyl or acyl; X is alkylene] and salts thereof posses, for example, inhibitory activity on angiotension converting enzyme, and are useful as an agent for diagnosis, prevention or treatment of hypertension as well as circulatory diseases such as cardiopathy and cerebral apoplexy.
    Type: Grant
    Filed: April 12, 1988
    Date of Patent: March 28, 1989
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Hirosada Sugihara, Kohei Nishikawa, Katsumi Ito
  • Patent number: 4751316
    Abstract: Novel 1,5-benzoxathiepin derivatives of the formula: ##STR1## [wherein R.sub.1 and R.sub.2 are independently hydrogen, halogen, hydroxy, lower alkyl or lower alkoxy; R.sub.3 and R.sub.4 are independently hydrogen, optionally substituted lower alkyl or optionally substituted cycloalkyl or optionally substituted aralkyl, or both jointly form an optionally substituted ring together with the adjacent nitrogen atom; X is hydrogen, optionally substituted lower alkyl, optionally substituted aryl or a carboxyl group which may be esterified or amidated; Y is >C.dbd.O or >CH--OR.sub.5 (wherein R.sub.5 is hydrogen, acyl or optionally substituted carbamoyl); m is an integer of 0 to 2; n is an integer of 1 to 6] and salts thereof exhibit serotonin S.sub.
    Type: Grant
    Filed: April 15, 1987
    Date of Patent: June 14, 1988
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Hirosada Sugihara, Minoru Hirata
  • Patent number: 4739066
    Abstract: Novel condensed seven-membered ring compounds of the formula: ##STR1## [wherein R.sup.1 and R.sup.2 are independently hydrogen, halogen, trifluoromethyl, lower alkyl or lower alkoxy, or both jointly form tri- or tetramethylene; R.sup.3 and R.sup.5 are independently hydrogen, lower alkyl or aralkyl; R.sup.4 is hydrogen or lower alkyl; R.sup.6 is a condensed or non-condensed hetero-alicyclic containing at least one atom of N, O and S as a ring-forming atom which may be substituted; A is an alkylene chain; n is 1 or 2] and salts thereof.These compounds exhibit inhibitory activity on angiotensin converting enzyme and so forth, and are of value as an agent for diagnosis, prevention and treatment of circulatory diseases, such as hypertension, cardiopathy and cerebral apoploxy.
    Type: Grant
    Filed: August 27, 1986
    Date of Patent: April 19, 1988
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Hirosada Sugihara, Kohei Nishikawa, Katsumi Ito
  • Patent number: 4736031
    Abstract: Novel condensed seven-membered heterocyclic compounds of the formula: ##STR1## wherein R.sub.1 and R.sub.2 are independently hydrogen, halogen, hydroxy, lower alkyl or lower alkoxy,R.sub.3 and R.sub.4 are independently hydrogen, optionally substituted lower alkyl, optionally substituted cycloalkyl or optionally substituted aralkyl, or both jointly form an optionally substituted ring together with the adjacent nitrogen atom,X is hydrogen, optionally substituted lower alkyl, optionally substituted aryl or a carboxyl group which may be esterified or amidated,Y is >C.dbd.O or >CH--OR.sub.5 in which R.sub.5 is hydrogen, acyl or optionally substituted carbamoyl,A is oxygen atom or sulfur atom, E is oxygen atom or methylene, andG is lower alkylene, provided that when A is sulfur atom, E is methylene,and salts thereof exhibit serotonin S.sub.
    Type: Grant
    Filed: April 15, 1986
    Date of Patent: April 5, 1988
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Hirosada Sugihara, Minoru Hirata
  • Patent number: 4672064
    Abstract: Novel 1,5-benzoxathiepin derivatives of the formula: ##STR1## [wherein R.sub.1 and R.sub.2 are independently hydrogen, halogen, hydroxy, lower alkyl or lower alkoxy; R.sub.3 and R.sub.4 are independently hydrogen, optionally substituted lower alkyl or optionally substituted cycloalkyl or optionally substituted aralkyl, or both jointly form an optionally substituted ring together with the adjacent nitrogen atom; X is hydrogen, optionally substituted lower alkyl, optionally substituted aryl or a carboxyl group which may be esterified or amidated; Y is ##STR2## (wherein R.sub.5 is hydrogen, acyl or optionally substituted carbamoyl); m is an integer of 0 to 2; n is an integer of 1 to 6] and salts thereof exhibit serotonin S.sub.
    Type: Grant
    Filed: December 10, 1985
    Date of Patent: June 9, 1987
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Hirosada Sugihara, Minoru Hirata
  • Patent number: 4638000
    Abstract: Novel condensed seven-membered ring compounds of the formula: ##STR1## [wherein R.sup.1 and R.sup.2 are independently hydrogen, halogen, trifluoromethyl, lower alkyl or lower alkoxy, or both jointly form tri- or tetramethylene; R.sup.3 and R.sup.5 are independently hydrogen, lower alkyl or aralkyl; R.sup.4 is hydrogen or lower alkyl; R.sup.6 is a condensed or non-condensed hetero-alicyclic containing at least one atom of N, O and S as a ring-forming atom which may be substituted; A is an alkylene chain; n is 1 or 2] and salts thereof.These compounds exhibit inhibitory activity on angiotensin converting enzyme and so forth, and are of value as an agent for diagnosis, prevention and treatment of circulatory diseases, such as hypertension, cardiopathy and cerebral apoploxy.
    Type: Grant
    Filed: January 14, 1985
    Date of Patent: January 20, 1987
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Hirosada Sugihara, Kohei Nishikawa, Katsumi Ito
  • Patent number: 4591458
    Abstract: Novel 3-amino-4-oxo-2,3,4,5-tetrahydro-1,5-benzoxazepine derivatives of the formula ##STR1## [wherein R.sup.1 and R.sup.2 are independently hydrogen, halogen trifluoromethyl, lower alkyl or lower alkoxy, or both jointly form tri- or tetramethylene; R.sup.3 is hydrogen, optionally substituted lower alkyl or optionally substituted aralkyl; R.sup.4 is hydrogen, optionally substituted alkyl, optionally substituted aralkyl or optionally substituted cycloalkylalkyl; Y is a carboxyl group which may be esterified or amidated; m is 1 or 2] and salts thereof.These compounds and salts thereof exhibits inhibitory activity on angiotensin converting enzyme and so forth, and are of value as an agent for diagnosis, prevention and treatment of circulatory diseases (e.g. hypertension, cardiopathy, cerebral apoploxy).
    Type: Grant
    Filed: July 26, 1985
    Date of Patent: May 27, 1986
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Hirosada Sugihara, Kohei Nishikawa, Katsumi Ito
  • Patent number: 4564612
    Abstract: Novel condensed, seven-membered ring compounds of the formula: ##STR1## [wherein R.sup.1 and R.sup.2 each represent hydrogen, halogen, trifluoromethyl, lower alkyl or alkoxy, or both jointly form tri- or tetramethylene; R.sup.3 is hydrogen, lower alkyl or aralkyl; R.sup.4 is hydrogen or alkyl, aralkyl or cycloalkylalkyl which may be substituted; X is a group represented by the formula S(O).sub.n (where n is an integer of 0 to 2); Y is a carboxyl group which may be esterified or amidated; m is 1 or 2] and salts thereof.These compounds exhibit inhibitory activity on angiotensin converting enzyme and so forth, and are of value as an agent for diagnosis, prevention and treatment of hypertension.
    Type: Grant
    Filed: April 11, 1984
    Date of Patent: January 14, 1986
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Hirosada Sugihara, Kohei Nishikawa, Katsumi Ito
  • Patent number: 4558068
    Abstract: Novel spirobenzofuranone compounds of the formula: ##STR1## wherein R is a hydrogen atom or a lower alkyl and --X-- is ##STR2## and a pharmaceutically acceptable salt thereof, have gastric secretion inhibitive, antiulcer activities, and are of value as drugs.
    Type: Grant
    Filed: July 12, 1984
    Date of Patent: December 10, 1985
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Hirosada Sugihara, Masazumi Watanabe, Mitsuru Kawada, Isuke Imada
  • Patent number: 4548932
    Abstract: Novel 3-amino-4-oxo-2,3,4,5-tetrahydro-1,5-benzoxazepine derivatives of the formula ##STR1## [wherein R.sup.1 and R.sup.2 are independently hydrogen, halogen, trifluoromethyl, lower alkyl or lower alkoxy, or both jointly form tri- or tetramethylene; R.sup.3 is hydrogen, optionally substituted lower alkyl or optionally substituted aralkyl; R.sup.4 is hydrogen, optionally substituted alkyl, optionally substituted aralkyl or optionally substituted cycloalkylalkyl; Y is a carboxyl group which may be esterified or amidated; m is 1 or 2] and salts thereof.These compounds and salts thereof exhibits inhibitory activity on angiotensin converting enzyme and so forth, and are of value as an agent for diagnosis, prevention and treatment of circulatory diseases (e.g. hypertension, cardiopathy, cerebral apoploxy).
    Type: Grant
    Filed: August 3, 1984
    Date of Patent: October 22, 1985
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Hirosada Sugihara, Kohei Nishikawa, Katsumi Ito
  • Patent number: 4362740
    Abstract: New spiro compounds of the formula: ##STR1## wherein n is an integer of 1 to 4, and X is halogen, lower alkyl, nitro, amino which may be substituted, hydroxyl which may be substituted, acyl, carboxyl, lower alkoxycarbonyl, carbamoyl which may be substituted, sulfamoyl which may be substituted, lower alkylthio or lower alkylsulfonyl, or two of X at the 5- and 6-positions together form --CH.dbd.CH--CH.dbd.CH--, exhibit inhibitory activity to thrombocyte aggregation and are useful for the prophylaxis or treatment of cardiovascular disturbance such as thrombosis.
    Type: Grant
    Filed: September 19, 1980
    Date of Patent: December 7, 1982
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Isuke Imada, Hirosada Sugihara, Mitsuru Kawada
  • Patent number: 4342779
    Abstract: Novel 7-acetylspirobenzofuranone compound of the formula: ##STR1## has gastric secretion inhibitive, antiinflammatory and analgesic activities, and is of value as drugs.
    Type: Grant
    Filed: April 17, 1981
    Date of Patent: August 3, 1982
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Hirosada Sugihara, Masazumi Watanabe, Mitsuru Kawada, Isuke Imada
  • Patent number: 4330554
    Abstract: Novel spirobenzofuranone compounds of the formula: ##STR1## have gastric secretion inhibitive, antiinflammatory and analgesic activities, and are of value as drugs.
    Type: Grant
    Filed: April 17, 1981
    Date of Patent: May 18, 1982
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Hirosada Sugihara, Masazumi Watanabe, Mitsuru Kawada, Isuke Imada