Patents by Inventor Hideo Ishitsuka
Hideo Ishitsuka 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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Publication number: 20030138864Abstract: The present invention relates to a method for identification of enzymes that are preferentially expressed in certain tumor tissue as compared with rapidly growing normal cells or tissue, use of said enzymes for the compound design to generate an active anti-cancer substance selectively in tumor tissue, compounds designed based on said enzymes, their pharmaceutically acceptable salts as well as pharmaceutical composition thereof.Type: ApplicationFiled: November 21, 2002Publication date: July 24, 2003Inventors: Hideo Ishitsuka, Hisafumi Okabe, Nobuo Shimma, Takuo Tsukuda, Isao Umeda
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Patent number: 6211166Abstract: Novel 5′-deoxy-cytidine derivatives represented by the general formula (I) wherein R1 is a hydrogen atom or a group easily hydrolyzable under physiological conditions; R2 is a hydrogen atom, or —CO—OR4 group [wherein R4 is a saturated or unsaturated, straight or branched hydrocarbon group consisting of one to fifteen carbon atoms, or a group of the formula —(CH2)n—Y (in which Y is cyclohexyl or phenyl; n is an integer from 0 to 4)]; R3 is a hydrogen atom, bromo, iodo, cyano, a C1-4 alkyl group [which may be substituted with halogen atom(s)], a vinyl or ethynyl group [which may be substituted with halogen atom(s), C1-4 alkyl, cycloalkyl, aralkyl, or aromatic ring which may have one or more hetero atom(s)], or an aralkyl group which may be substituted for use in medical therapy, especially tumor therapy.Type: GrantFiled: March 24, 2000Date of Patent: April 3, 2001Assignee: Hoffman-La Roche Inc.Inventors: Kazuo Hattori, Tohru Ishikawa, Hideo Ishitsuka, Yasunori Kohchi, Nobuhiro Oikawa, Nobuo Shimma, Hitomi Suda
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Patent number: 6114520Abstract: Novel 5'-deoxy-cytidine derivatives represented by the general formula (I) ##STR1## wherein R.sup.1 is a hydrogen atom or a group easily hydrolyzable under physiological conditions; R.sup.2 is a hydrogen atom, or --CO--OR.sup.4 group [wherein R.sup.4 is a saturated or unsaturated, straight or branched hydrocarbon group consisting of one to fifteen carbon atoms, or a group of the formula --(CH.sub.2).sub.n --Y (in which Y is cyclohexyl or phenyl; n is an integer from 0 to 4)]; R.sup.3 is a hydrogen atom, bromo, iodo, cyano, a C.sub.1-4 alkyl group [which may be substituted with halogen atom(s)], a vinyl or ethynyl group [which may be substituted with halogen atom(s), C.sub.1-4 alkyl, cycloalkyl, aralkyl, or aromatic ring which may have one or more hetero atom(s)], or an aralkyl group which may be substituted for use in medical therapy, especially tumor therapy.Type: GrantFiled: January 14, 2000Date of Patent: September 5, 2000Assignee: Hoffmann-La Roche Inc.Inventors: Kazuo Hattori, Tohru Ishikawa, Hideo Ishitsuka, Yasunori Kohchi, Nobuhiro Oikawa, Nobuo Shimma, Hitomi Suda
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Patent number: 6005098Abstract: Compounds of the formula (I) ##STR1## wherein R.sup.1 is each independently hydrogen or a group easily hydrolyzable under physiological conditions;R.sup.2 is --(CH.sub.2).sub.n -cycloalkyl wherein cycloalkyl contains 3 to 5 carbon atoms and n is an integer from 0 to 4, heteroaryl-(lower-alkyl), (lower-alkoxy)-(lower-alkyl), aryloxy-(lower-alkyl), aralkyloxy-(lower-alkyl), (lower-alkylthio)-(lower-alkyl), arylthio-(lower-alkyl), aralkylthio-(lower-alkyl), oxo-(lower-alkyl), acylamino-(lower-alkyl), cyclic amino-(lower-alkyl), (2-oxocyclic amino)-(lower-alkyl) wherein the alkylene chain is unsubstituted or substituted with one or two lower-alkyl group(s); andR.sup.3 is iodo, or a vinyl or ethynyl group which group is unsubstituted or substituted by one or more substituents selected from the group consisting of halogen, C.sub.1-4 alkyl, cycloalkyl, aralkyl, carbocyclic aromatic ring and heteorcyclic aromatic ring.Type: GrantFiled: January 20, 1999Date of Patent: December 21, 1999Assignee: Hoffmann-La Roche Inc.Inventors: Kazuo Hattori, Tohru Ishikawa, Hideo Ishitsuka, Yasunori Kohchi, Nobuhiro Oikawa, Nobuo Shimma, Hitomi Suda
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Patent number: 5472949Abstract: The invention relates to N.sup.4 -(substituted-oxycarbonyl)-5'-deoxy-5-fluorocytidine derivatives which are useful as an agent for treating tumors, pharmaceutical compositions including the same, a method of treating tumors and a method of preparing N.sup.4 -(substituted-oxycarbonyl)-5'-deoxy-5-fluorocytidine derivatives for treating tumors.Compounds of formula (I), ##STR1## wherein R.sup.1 is a saturated or unsaturated, straight or branched hydrocarbon radical wherein the number of carbon atoms in the longest straight chain of this hydrocarbon radical ranges from three to seven, or is a radical of the formula --(CH.sub.2)n--.sup.Y wherein Y is a cyclohexyl radical, a C.sub.1 -C.sub.4 alkoxy radical or a phenyl radical and wherein when Y is a cyclohexyl radical n is an integer from 0 to 4, and when Y is C.sub.1 -C.sub.4 alkoxy radical or a phenyl radical n is an integer from 2 to 4, and R.sup.2 is a hydrogen atom or a radical easily hydrolyzable under physiological conditions,or a hydrate or solvate thereof.Type: GrantFiled: December 14, 1993Date of Patent: December 5, 1995Assignee: Hoffmann-La Roche Inc.Inventors: Motohiro Arasaki, Hideo Ishitsuka, Isami Kuruma, Masanori Miwa, Chikako Murasaki, Nobuo Shimma, Isao Umeda
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Patent number: 4966891Abstract: The novel 5'-deoxy-5-fluorocytidine derivatives of formula ##STR1## wherein R.sup.1, R.sup.2 and R.sup.3 are hydrogen or an easily hydrolyzable radical under physiological conditions, with the proviso that, at least one or R.sup.1, R.sup.2 and R.sup.3 is an easily hydrolyzable radical under physiological conditions,as well as hydrates of solvates of these compounds have antitumor properties. They can be prepared from compounds of formula I, wherein R.sup.1 is hydrogen or an amino-protecting radical and R.sup.2 and R.sup.3 are hydrogen or a hydroxy-protecting radical or taken together are a cyclic hydroxy-protecting radical.Type: GrantFiled: November 8, 1988Date of Patent: October 30, 1990Assignee: Hoffmann-La Roche Inc.Inventors: Morio Fujiu, Hideo Ishitsuka, Masanori Miwa, Isao Umeda, Kazuteru Yokose
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Patent number: 4605674Abstract: Antivirally active compounds of the formula ##STR1## wherein R.sup.1 represents hydroxy, acyloxy derived from an aliphatic acid having 2-18 carbon atoms or a heterocyclic carboxylic acid containing nitrogen atom(s), lower alkoxycarbonyloxy, aminoacyloxy or carboxyalkanoyloxy;R.sup.2 represents lower alkoxy;R.sup.3 represents hydrogen or lower alkoxy; andR.sup.4 represents phenyl which may be substituted by one or more substituents selected from the group consisting of lower alkyl, lower alkoxy, benzyloxy, allyloxy, alkylthio, dialkylamino, amino, cyano, hydroxy, halo and alkylenedioxy; or pyridyl, furyl, thienyl or pyrrolyl which may be substituted by lower alkyl,pharmaceutical compositions containing them and a process for the preparation of those compounds of formula I which are novel.Type: GrantFiled: April 24, 1984Date of Patent: August 12, 1986Assignee: Hoffmann-La Roche Inc.Inventors: Morio Fujiu, Yasuji Suhara, Hideo Ishitsuka
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Patent number: 4452782Abstract: A pentadecapeptide and salts thereof with immunopotentiating activity is presented. Also presented is a fermentation process for the preparation of the pentadecapeptide by a microorganism of the genus Streptoverticillium and pharmaceutical preparations containing the peptide or its salts.Type: GrantFiled: August 26, 1982Date of Patent: June 5, 1984Assignee: Hoffmann-La Roche Inc.Inventors: Kenji Takemoto, Yumiko Miyasaka, Hideo Ishitsuka, Yasuji Suhara, Hiromi Maruyama
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Patent number: 4442031Abstract: Novel hexapeptides corresponding to internal fragments of thymosin .alpha..sub.1 are active as agents which restore and stimulate immune function.Type: GrantFiled: April 5, 1983Date of Patent: April 10, 1984Assignee: Hoffmann-La Roche Inc.Inventors: Arthur M. Felix, Hideo Ishitsuka, Johannes A. Meienhofer, Yumiko Ohta
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Patent number: 4352792Abstract: Antiviral compositions containing 3-alkoxyflavone compounds as their active ingredients are disclosed.Type: GrantFiled: April 7, 1980Date of Patent: October 5, 1982Assignee: Hoffmann-La Roche Inc.Inventors: Hideo Ishitsuka, Haruyoshi Shirai, Isao Umeda, Yasuji Suhara
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Patent number: 4327088Abstract: Compounds of the formula: ##STR1## wherein R.sub.1 is hydroxy, phosphonooxy, aminoglycosyloxy, acylaminoglycosyloxy, benzyloxycarbonyloxy, arylcarbonyloxy, trialkylammonio-acyloxy or furoyloxy; R.sub.2 and R.sub.3 each are lower alkoxy; and R.sub.4 is benzimidazolyl, furyl which is unsubstituted or substituted with lower alkyl, thienyl which is unsubstituted or substituted with lower alkyl, or phenyl which is substituted with lower alkyl, lower alkoxy, alkoxyalkoxy, alkylthio, alkylenedioxy, or acyloxy, with the proviso that when R.sub.1 is hydroxy, R.sub.4 is benzimidazolyl or phenyl which is substituted by acyloxy or alkoxyalkoxy, or pharmaceutically acceptable salts thereof useful as antiviral agents.Type: GrantFiled: May 12, 1980Date of Patent: April 27, 1982Assignee: Hoffmann-La Roche Inc.Inventors: Nobuo Shinma, Isao Umeda, Hideo Ishitsuka, Yasuji Suhara