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).
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Patent number: 5550131Abstract: 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: GrantFiled: June 17, 1994Date of Patent: August 27, 1996Assignee: Takeda Chemical Industries, Ltd.Inventors: Hirosada Sugihara, Zenichi Terashita, Hideto Fukushi
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Patent number: 5294713Abstract: 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: GrantFiled: August 7, 1992Date of Patent: March 15, 1994Assignee: Takeda Chemical Industries, Ltd.Inventors: Hirosada Sugihara, Zenichi Terashita
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Patent number: 4997836Abstract: 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: GrantFiled: November 9, 1989Date of Patent: March 5, 1991Assignee: Takeda Chemical Industries, Ltd.Inventors: Hirosada Sugihara, Kohei Nishikawa
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Patent number: 4954625Abstract: 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: GrantFiled: August 30, 1989Date of Patent: September 4, 1990Assignee: Takeda Chemical Industries, Ltd.Inventors: Hirosada Sugihara, Kohei Nishikawa, Katsumi Ito
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Patent number: 4937246Abstract: 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: GrantFiled: November 22, 1988Date of Patent: June 26, 1990Assignee: Takeda Chemical Industries, Ltd.Inventors: Hirosada Sugihara, Katsumi Itoh, Kohei Nishikawa
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Patent number: 4880809Abstract: 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: GrantFiled: March 14, 1988Date of Patent: November 14, 1989Assignee: Takeda Chemical Industries, Ltd.Inventors: Hirosada Sugihara, Katsumi Itoh, Kohei Nishikawa
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Patent number: 4871842Abstract: 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: GrantFiled: July 14, 1988Date of Patent: October 3, 1989Assignee: Takeda Chemical Industries, Ltd.Inventors: Hirosada Sugihara, Kohei Nishikawa, Katsumi Ito
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Patent number: 4816466Abstract: 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: GrantFiled: April 12, 1988Date of Patent: March 28, 1989Assignee: Takeda Chemical Industries, Ltd.Inventors: Hirosada Sugihara, Kohei Nishikawa, Katsumi Ito
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Patent number: 4751316Abstract: 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: GrantFiled: April 15, 1987Date of Patent: June 14, 1988Assignee: Takeda Chemical Industries, Ltd.Inventors: Hirosada Sugihara, Minoru Hirata
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Patent number: 4739066Abstract: 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: GrantFiled: August 27, 1986Date of Patent: April 19, 1988Assignee: Takeda Chemical Industries, Ltd.Inventors: Hirosada Sugihara, Kohei Nishikawa, Katsumi Ito
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Patent number: 4736031Abstract: 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: GrantFiled: April 15, 1986Date of Patent: April 5, 1988Assignee: Takeda Chemical Industries, Ltd.Inventors: Hirosada Sugihara, Minoru Hirata
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Patent number: 4672064Abstract: 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: GrantFiled: December 10, 1985Date of Patent: June 9, 1987Assignee: Takeda Chemical Industries, Ltd.Inventors: Hirosada Sugihara, Minoru Hirata
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Patent number: 4638000Abstract: 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: GrantFiled: January 14, 1985Date of Patent: January 20, 1987Assignee: Takeda Chemical Industries, Ltd.Inventors: Hirosada Sugihara, Kohei Nishikawa, Katsumi Ito
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Patent number: 4591458Abstract: 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: GrantFiled: July 26, 1985Date of Patent: May 27, 1986Assignee: Takeda Chemical Industries, Ltd.Inventors: Hirosada Sugihara, Kohei Nishikawa, Katsumi Ito
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Patent number: 4564612Abstract: 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: GrantFiled: April 11, 1984Date of Patent: January 14, 1986Assignee: Takeda Chemical Industries, Ltd.Inventors: Hirosada Sugihara, Kohei Nishikawa, Katsumi Ito
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Patent number: 4558068Abstract: 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: GrantFiled: July 12, 1984Date of Patent: December 10, 1985Assignee: Takeda Chemical Industries, Ltd.Inventors: Hirosada Sugihara, Masazumi Watanabe, Mitsuru Kawada, Isuke Imada
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Patent number: 4548932Abstract: 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: GrantFiled: August 3, 1984Date of Patent: October 22, 1985Assignee: Takeda Chemical Industries, Ltd.Inventors: Hirosada Sugihara, Kohei Nishikawa, Katsumi Ito
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Patent number: 4362740Abstract: 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: GrantFiled: September 19, 1980Date of Patent: December 7, 1982Assignee: Takeda Chemical Industries, Ltd.Inventors: Isuke Imada, Hirosada Sugihara, Mitsuru Kawada
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Patent number: 4342779Abstract: Novel 7-acetylspirobenzofuranone compound of the formula: ##STR1## has gastric secretion inhibitive, antiinflammatory and analgesic activities, and is of value as drugs.Type: GrantFiled: April 17, 1981Date of Patent: August 3, 1982Assignee: Takeda Chemical Industries, Ltd.Inventors: Hirosada Sugihara, Masazumi Watanabe, Mitsuru Kawada, Isuke Imada
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Patent number: 4330554Abstract: Novel spirobenzofuranone compounds of the formula: ##STR1## have gastric secretion inhibitive, antiinflammatory and analgesic activities, and are of value as drugs.Type: GrantFiled: April 17, 1981Date of Patent: May 18, 1982Assignee: Takeda Chemical Industries, Ltd.Inventors: Hirosada Sugihara, Masazumi Watanabe, Mitsuru Kawada, Isuke Imada