Patents by Inventor Akira Terahara
Akira Terahara 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: 4866093Abstract: The dihydro-M-4 and dihydro-IsoM-4 hydroxy carboxylic acids of the formula (II): ##STR1## wherein one of R.sup.1 represents a hydrogen atom and the other represents a hydroxy group and wherein the structure shown as ##STR2## represents a structure of formula ##STR3## and the salts and esters of said acids. The invention also provides pharmaceutical compositions containing said acids, salts and/or esters which are useful for inhibiting cholesterol biosynthesis in the liver.Type: GrantFiled: March 19, 1984Date of Patent: September 12, 1989Assignee: Sankyo Company LimitedInventors: Akira Terahara, Minoru Tanaka
-
Patent number: 4820865Abstract: Compounds of formula (I): ##STR1## wherein R.sup.1 represents a group of formula ##STR2## or a group of formula ##STR3## (wherein R.sup.2 represents a C.sub.1 --C.sub.10 alkyl group) and their corresponding free hydroxy-carboxylic acids and salts and esters of said acids may be prepared by the enzymatic hydroxylation of an MB-530B compound (which may be the lactone, the carboxylic acid or a salt or ester of MB-530B or a corresponding compound in which the 2-methylbutyryloxy group at the 1-position of these compounds has been replaced by another C.sub.2 --C.sub.11 acyloxy group), preferably using a microorganism of the genus Syncephalastrum, Mucor, Rhizopus, Zygorinchus, Circinella, Actinomucor, Gongronella, Phycomyces, Streptomyces, Absidia, Cunninghamella, Mortierella, Pycnoporus or Rhizoctonia, or a cell-free enzyme-containing extract from the microorganism.Type: GrantFiled: September 17, 1986Date of Patent: April 11, 1989Assignee: Sankyo Company, LimitedInventors: Akira Terahara, Minoru Tanaka
-
Patent number: 4695587Abstract: Tetrahydro-M-4 and tetrahydro-IsoM-4 hydroxy carboxylic acids of the formula (II): ##STR1## wherein one of R.sup.1 and R.sup.2 represents a hydrogen atom and the other represents a hydroxy group, and the salts and esters of said acids which are useful for inhibiting chloresterol biosynthesis in the liver. The invention also provides pharmaceutical compositions containing said acid(s).Type: GrantFiled: April 26, 1984Date of Patent: September 22, 1987Assignee: Sankyo Company LimitedInventors: Akira Terahara, Minoru Tanaka
-
Patent number: 4537859Abstract: Compounds of formula (I): ##STR1## (wherein OH represents OH or OH), that is to say M-4 carboxylic acid and M-4' carboxylic acid, as well as pharmaceutically acceptable salts and esters thereof and the corresponding ring-closed lactones may be prepared by contacting an ML-236B compound with a microorganism of the genus Nocardia or a cell-free, enzyme-containing extract thereof and then, if necessary, subjecting the resulting product to one or more of the following reactions: hydrolysis, salification, esterification and lactonisation. The resulting M-4 and M-4' derivatives have the ability to inhibit the biosynthesis of cholesterol and are therefore of value in the therapy and/or prophylaxis of hyperlipaemia and arteriosclerosis.Type: GrantFiled: November 18, 1982Date of Patent: August 27, 1985Assignee: Sankyo Company, LimitedInventors: Akira Terahara, Minoru Tanaka
-
Patent number: 4517373Abstract: The 1-acyloxy-6-hydroxy-IsoMB-530B lactones of the formula (I): ##STR1## wherein R.sup.1 represents a group of the formula ##STR2## wherein R.sup.2 is a C.sub.1 -C.sub.10 alkyl group.Type: GrantFiled: August 24, 1982Date of Patent: May 14, 1985Assignee: Sankyo Company, LimitedInventors: Akira Terahara, Minoru Tanaka
-
Patent number: 4479965Abstract: Tetrahydro-M-4 and tetrahydro-IsoM-4 hydroxy carboxylic acids of the formula (I): ##STR1## wherein one of R.sup.1 and R.sup.2 represents a hydrogen atom and the other represents a hydroxy group which are useful for inhibiting chloresterol biosynthesis in the liver. The invention also provides pharmaceutical compositions containing said lactone(s).Type: GrantFiled: April 28, 1982Date of Patent: October 30, 1984Assignee: Sankyo Company, LimitedInventors: Akira Terahara, Minoru Tanaka
-
Patent number: 4460765Abstract: A new compound, named "Griseolic acid", and its salts and can be prepared by the cultivation of Streptomyces griseoaurantiacus SANK 63479 (FERM-P 5223). Griseolic acid and its salts inhibit the activity of the enzyme cyclic adenosine monophosphate phosphodiesterase and, as a result of this, have variety of physiological activities and uses.Type: GrantFiled: May 12, 1982Date of Patent: July 17, 1984Assignee: Sankyo Company LimitedInventors: Atsushi Naito, Fumio Nakagawa, Takao Okazaki, Akira Terahara, Seigo Iwado, Mitsuo Yamazaki
-
Patent number: 4451481Abstract: Dihydro-M-4 and dihydro-IsoM-4 are new compounds which may be prepared by the catalytic hydrogenation of M-4 or IsoM-4 respectively. They, and their salts and esters (which may be prepared by conventional salification or esterification reactions with the parent dihydro-M-4 or dihydro-IsoM-4), are capable of inhibiting cholesterol biosynthesis in the liver and may be formulated, for therapeutic use, with conventional pharmaceutical carriers or diluents.Type: GrantFiled: May 5, 1982Date of Patent: May 29, 1984Assignee: Sankyo Company LimitedInventors: Akira Terahara, Minoru Tanaka
-
Patent number: 4448979Abstract: Compounds of formula (I): ##STR1## (wherein R represents a group of formula ##STR2## and the corresponding ring-closed lactones, salts (especially alkali metal salts) and esters (especially C.sub.1 -C.sub.5 alkyl esters) thereof may be prepared by subjecting ML-236B, or ML-236B carboxylic acid or a salt or ester thereof to enzymatic hydroxylation, which may be effected by means of microorganisms of the genera Mucor, Rhizopus, Zygorynchus, Circinella, Actinomucor, Gongronella, Phycomyces, Martierella, Pycnoporus, Rhizoctonia, Absidia, Cunninghamella, Syncephalastrum and Streptomyces, or cell-free, enzyme-containing extracts from said microorganisms. The compounds are capable of inhibiting biosynthesis of cholesterol and are thus useful in the treatment of hypercholesteraemia.Type: GrantFiled: February 24, 1982Date of Patent: May 15, 1984Assignee: Sankyo Company, LimitedInventors: Akira Terahara, Minoru Tanaka
-
Patent number: 4447626Abstract: A compound of formula (I): ##STR1## (called 6-methoxy-IsoML-236B lactone) and its corresponding free hydroxy-carboxylic acid and salts and esters of said acid may be prepared by the enzymatic alkoxylation of an ML-236B compound, preferably using a microorganism of the genus Syncephalastrum, Absidia or Cunninghamella, e.g. Absidia coerulea, or a cell-free enzyme-containing extract from said microorganism. If desired, the lactone or carboxylic acid may be converted by conventional salification or esterification techniques to the desired salt or ester. These compounds have the ability to inhibit the biosynthesis of cholesterol and are thus of value in the treatment of hypercholesteraemia, for which purpose they may be formulated as compositions in admixture with conventional pharmaceutical carriers or diluents.Type: GrantFiled: July 7, 1982Date of Patent: May 8, 1984Assignee: Sankyo Company LimitedInventors: Akira Terahara, Minoru Tanaka
-
Patent number: 4438277Abstract: Compounds of formula (I): ##STR1## (in which: Z represents a group of formula ##STR2## A represents a group of formula ##STR3## B represents a group of formula ##STR4## R.sup.1 represents a hydrogen atom or a methyl group; R.sup.2, R.sup.3, R.sup.4 and R.sup.6 are the same or different and each represents a hydrogen atom or an acyl group;R.sup.5 represents a carboxy group;R.sup.7 represents a hydrogen atom, an alkyl group or an acyl group;X represents a halogen atom; andthe bond represents a double bond)and salts and esters of the carboxy group represented by R.sup.5 have useful anti-hypercholesteraemic activity and may be prepared from certain natural products obtainable by cultivation of microorganisms of the genera Penicillium or Monascus.Type: GrantFiled: April 15, 1982Date of Patent: March 20, 1984Assignee: Sankyo Company, LimitedInventors: Akira Terahara, Kiyoshi Hamano, Yoshio Tsujita, Minoru Tanaka
-
Patent number: 4410629Abstract: Compounds of formula (I): ##STR1## (wherein R represents a group of formula ##STR2## and the corresponding ring-closed lactones, salts (especially alkali metal salts) and esters (especially C.sub.1 -C.sub.5 alkyl esters) thereof may be prepared by subjecting ML-236B, or ML-236B carboxylic acid or a salt or ester thereof to enzymatic hydroxylation, which may be effected by means of microorganisms of the genera Mucor, Rhizopus, Zygorynchus, Circinella, Actinomucor, Gongornella, Phycomyces, Martierella, Pycnoporus, Rhizoctonia, Absidia, Cunninghamella, Syncephalastrum and Streptomyces, or cell-free, enzyme-containing extracts from said microorganisms. The compounds are capable of inhibiting biosynthesis of cholesterol and are thus useful in the treatment of hypercholesteraemia.Type: GrantFiled: February 24, 1982Date of Patent: October 18, 1983Assignee: Sankyo Company LimitedInventors: Akira Terahara, Minoru Tanaka
-
Patent number: 4361515Abstract: Compounds of formula (I): ##STR1## (in which: Z represents a group of formula ##STR2## A represents a group of formula ##STR3## B represents a group of formula ##STR4## R.sup.1 represents a hydrogen atom or a methyl group; R.sup.2, R.sup.3, R.sup.4 and R.sup.6 are the same or different and each represents a hydrogen atom or an acyl group;R.sup.5 represents a carboxy group;R.sup.7 represents a hydrogen atom, an alkyl group or an acyl group;X represents a halogen atom; andthe bond represents a double bond)and salts and esters of the carboxy group represented byR.sup.5 and compounds of formula (II): ##STR5## (in which R.sup.1, is as defined above and R.sup.2 represents an .alpha.-methylbutyryl group; and R.sup.4 represents a hydrogen atom) have useful anti-hypercholesteraemic activity and may be prepared from certain natural products obtainable by cultivation of microorganisms of the genera Penicillium or Monascus.Type: GrantFiled: April 21, 1981Date of Patent: November 30, 1982Assignee: Sankyo Company, LimitedInventors: Akira Terahara, Kiyoshi Hamano, Yoshio Tsujita, Minoru Tanaka
-
Patent number: 4346227Abstract: Compounds of formula (I): ##STR1## (wherein R represents a group of formula ##STR2## and the corresponding ring-closed lactones, salts (especially alkali metal salts) and esters (especially C.sub.1 -C.sub.5 alkyl esters) thereof may be prepared by subjecting ML-236B, or ML-236B carboxylic acid or a salt or ester thereof to enzymatic hydroxylation, which may be effected by means of microorganisms of the genera Mucor, Rhizopus, Zygorynchus, Circinella, Actinomucor, Gongronella, Phycomyces, Martierella, Pycnoporus, Rhizoctonia, Absidia, Cunninghamella, Syncephalastrum and Streptomyces, or cell-free, enzyme-containing extracts from said microorganisms. The compounds are capable of inhibiting biosynthesis of cholesterol and are thus useful in the treatment of hypercholesteraemia.Type: GrantFiled: June 5, 1981Date of Patent: August 24, 1982Assignee: Sankyo Company, LimitedInventors: Akira Terahara, Minoru Tanaka
-
Patent number: 4255444Abstract: 4-Hydroxy-2-pyrone derivatives of formula (I): ##STR1## (wherein A represents an alkylene group which is optionally alkyl-substituted or an alkenylene group, and Z represents a substituted or unsubstituted aryl or aryloxy group) may be prepared by cyclizing an ester of formula (II): ##STR2## (wherein A and Z are as defined above and R represents an organic group) and have valuable antilipaemic activities.Type: GrantFiled: October 26, 1979Date of Patent: March 10, 1981Assignee: Sankyo Company LimitedInventors: Hidehiko Oka, Akira Terahara, Akira Endo
-
Patent number: 4248889Abstract: 3,5-Dihydroxypentanoic ester derivatives of formula (I): ##STR1## wherein: A represents an alkylene group which is optionally substituted by one or more alkyl groups, or an alkenylene group;Z represents a substituted or unsubstituted aryl or aryloxy group; andR represents a C.sub.1 -C.sub.4 alkyl group) may be prepared by reacting a dianion of an acetoacetic ester with an aldehyde of formula Z-A-CHO (wherein A and Z are as defined above) and then reducing the resulting compound. These 3,5-dihydroxypentanoic ester derivatives have antihyperlipaemic activity and are thus valuable pharmaceuticals.Type: GrantFiled: October 26, 1979Date of Patent: February 3, 1981Assignee: Sankyo Company LimitedInventors: Hidehiko Oka, Akira Terahara, Akira Endo
-
Patent number: 4137322Abstract: ML-236B carboxylic acid derivatives having the formula ##STR1## wherein R represents an alkyl group, a benzyl group optionally substituted with alkyl, alkoxy or halogen or a phenacyl group optionally substituted with alkyl, alkoxy or halogen; a group of 1/n M in which M represents a metal and n represents a valency of said metal; or a group of AH.sup.+ in which A represents an amino acid. These derivatives are derived from ML-236B by conventional procedures and have an antihyperlipemic activity.Type: GrantFiled: October 31, 1977Date of Patent: January 30, 1979Assignee: Sankyo Company LimitedInventors: Akira Endo, Akira Terahara, Noritoshi Kitano, Akira Ogiso, Seiji Mitsui
-
Patent number: 4049495Abstract: Physiologically active substances ML-236 of the formula ##STR1## wherein R is hydrogen atom, hydroxy group or 2-methyl-butyryloxy group having cholesterol- and lipid-lowering effects in blood and liver and thus utility as hypocholesteremic and hypolipemic medicaments. They are obtained by cultivation of an ML-236-producing micro-organism belonging to the genus Penicillium in a culture medium and subsequent recovery thereof from a cultured broth.Type: GrantFiled: December 4, 1975Date of Patent: September 20, 1977Assignee: Sankyo Company LimitedInventors: Akira Endo, Masao Kuroda, Akira Terahara, Yoshio Tsujita, Chihiro Tamura
-
Patent number: 3983140Abstract: Physiologically active substances ML-236 of the formula ##SPC1##Wherein R is hydrogen atom, hydroxy group or 2-methylbutyryloxy group having cholesterol- and lipid-lowering effects in blood and liver and thus utility as hypocholesteremic and hypolipemic medicaments. They are obtained by cultivation of an ML-236-producing microorganism belonging to the genus Penicillium in a culture medium and subsequent recovery thereof from a cultured broth.Type: GrantFiled: May 12, 1975Date of Patent: September 28, 1976Assignee: Sankyo Company LimitedInventors: Akira Endo, Masao Kuroda, Akira Terahara, Yoshio Tsujita, Chihiro Tamura