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: 4866093
    Abstract: 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: Grant
    Filed: March 19, 1984
    Date of Patent: September 12, 1989
    Assignee: Sankyo Company Limited
    Inventors: Akira Terahara, Minoru Tanaka
  • Patent number: 4820865
    Abstract: 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of MB-530B or a corresponding compound in which the 2-methylbutyryloxy group at the 1-position of these compounds has been replaced by another C.sub.2 --C.sub.11 acyloxy group), preferably using a microorganism of the genus Syncephalastrum, Mucor, Rhizopus, Zygorinchus, Circinella,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: Grant
    Filed: September 17, 1986
    Date of Patent: April 11, 1989
    Assignee: Sankyo Company, Limited
    Inventors: Akira Terahara, Minoru Tanaka
  • Patent number: 4695587
    Abstract: 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: Grant
    Filed: April 26, 1984
    Date of Patent: September 22, 1987
    Assignee: Sankyo Company Limited
    Inventors: Akira Terahara, Minoru Tanaka
  • Patent number: 4537859
    Abstract: 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: Grant
    Filed: November 18, 1982
    Date of Patent: August 27, 1985
    Assignee: Sankyo Company, Limited
    Inventors: Akira Terahara, Minoru Tanaka
  • Patent number: 4517373
    Abstract: 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: Grant
    Filed: August 24, 1982
    Date of Patent: May 14, 1985
    Assignee: Sankyo Company, Limited
    Inventors: Akira Terahara, Minoru Tanaka
  • Patent number: 4479965
    Abstract: 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: Grant
    Filed: April 28, 1982
    Date of Patent: October 30, 1984
    Assignee: Sankyo Company, Limited
    Inventors: Akira Terahara, Minoru Tanaka
  • Patent number: 4460765
    Abstract: 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: Grant
    Filed: May 12, 1982
    Date of Patent: July 17, 1984
    Assignee: Sankyo Company Limited
    Inventors: Atsushi Naito, Fumio Nakagawa, Takao Okazaki, Akira Terahara, Seigo Iwado, Mitsuo Yamazaki
  • Patent number: 4451481
    Abstract: 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: Grant
    Filed: May 5, 1982
    Date of Patent: May 29, 1984
    Assignee: Sankyo Company Limited
    Inventors: Akira Terahara, Minoru Tanaka
  • Patent number: 4448979
    Abstract: 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: Grant
    Filed: February 24, 1982
    Date of Patent: May 15, 1984
    Assignee: Sankyo Company, Limited
    Inventors: Akira Terahara, Minoru Tanaka
  • Patent number: 4447626
    Abstract: 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: Grant
    Filed: July 7, 1982
    Date of Patent: May 8, 1984
    Assignee: Sankyo Company Limited
    Inventors: Akira Terahara, Minoru Tanaka
  • Patent number: 4438277
    Abstract: 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: Grant
    Filed: April 15, 1982
    Date of Patent: March 20, 1984
    Assignee: Sankyo Company, Limited
    Inventors: Akira Terahara, Kiyoshi Hamano, Yoshio Tsujita, Minoru Tanaka
  • Patent number: 4410629
    Abstract: 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: Grant
    Filed: February 24, 1982
    Date of Patent: October 18, 1983
    Assignee: Sankyo Company Limited
    Inventors: Akira Terahara, Minoru Tanaka
  • Patent number: 4361515
    Abstract: 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: Grant
    Filed: April 21, 1981
    Date of Patent: November 30, 1982
    Assignee: Sankyo Company, Limited
    Inventors: Akira Terahara, Kiyoshi Hamano, Yoshio Tsujita, Minoru Tanaka
  • Patent number: 4346227
    Abstract: 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: Grant
    Filed: June 5, 1981
    Date of Patent: August 24, 1982
    Assignee: Sankyo Company, Limited
    Inventors: Akira Terahara, Minoru Tanaka
  • Patent number: 4255444
    Abstract: 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: Grant
    Filed: October 26, 1979
    Date of Patent: March 10, 1981
    Assignee: Sankyo Company Limited
    Inventors: Hidehiko Oka, Akira Terahara, Akira Endo
  • Patent number: 4248889
    Abstract: 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: Grant
    Filed: October 26, 1979
    Date of Patent: February 3, 1981
    Assignee: Sankyo Company Limited
    Inventors: Hidehiko Oka, Akira Terahara, Akira Endo
  • Patent number: 4137322
    Abstract: 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: Grant
    Filed: October 31, 1977
    Date of Patent: January 30, 1979
    Assignee: Sankyo Company Limited
    Inventors: Akira Endo, Akira Terahara, Noritoshi Kitano, Akira Ogiso, Seiji Mitsui
  • Patent number: 4049495
    Abstract: 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: Grant
    Filed: December 4, 1975
    Date of Patent: September 20, 1977
    Assignee: Sankyo Company Limited
    Inventors: Akira Endo, Masao Kuroda, Akira Terahara, Yoshio Tsujita, Chihiro Tamura
  • Patent number: 3983140
    Abstract: 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: Grant
    Filed: May 12, 1975
    Date of Patent: September 28, 1976
    Assignee: Sankyo Company Limited
    Inventors: Akira Endo, Masao Kuroda, Akira Terahara, Yoshio Tsujita, Chihiro Tamura