Patents by Inventor Masatoshi Shiga

Masatoshi Shiga 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).

  • Process and diastereomeric salts useful for the optical resolution of racemic alpha-(4-(1, 1-dimethylethyl) phenyl] -4- (hydroxydiphenylmethyl) -1-piperidinebutanol and derivative compounds
    Publication number: 20060014793
    Abstract: A process and diastereomeric salts useful for the optical resolution of racemic ?-[4-(1,1-dimethylethyl)phenyl]-4-(hydroxydiphenylmethyl)-1 -piperidinebutanol, 4-[4-[4-(hydroxydiphenylmethyl)-1 -piperidinyl]-1-hydroxybutyl]-?,?-dimethylbenzeneacetic acid and lower alkyl 4-[4-[4-(hydroxydiphenylmethyl)-1-piperidinyl]-1-hydroxybutyl]-?,?-dimethylbenzeneacetates. The process comprises placing into solution a chiral resolving agent, either (+)/(?)-di-paratoluoyltartaric acid or (?)/(+)-mandelic acid, in an amount equimolar to a compound corresponding to the desired enantiomer of the above compound, precipitating the resulting diastereomeric salt between the chiral resolving agent and the target enantiomer and separating the enantiomer.
    Type: Application
    Filed: September 15, 2005
    Publication date: January 19, 2006
    Applicant: Merrell Pharmaceuticals Inc.
    Inventors: Mitsuo Nakamura, Masatoshi Shiga
  • Process and diastereomeric salts useful for the optical resolution of racemic alpha-(4-(1,1-dimethylethyl)phenyl)-4-(hydroxydiphenylmethyl)-1-piperidinebutanol and derivative compounds
    Publication number: 20040186137
    Abstract: A process and diastereomeric salts useful for the optical resolution of racemic &agr;-[4-(1,1-dimethylethyl)phenyl]-4-(hydroxydiphenylmethyl)-1-piperidinebutanol, 4-[4-[4-(hydroxydiphenylmethyl)-1-piperidinyl]-1-hydroxybutyl]-&agr;,&agr;-dimethylbenzeneacetic acid and lower alkyl 4-[4-[4-(hydroxydiphenylmethyl)-1-piperidinyl]-1-hydroxybutyl]-&agr;,&agr;-dimethylbenzeneacetates. The process comprises placing into solution a chiral resolving agent, either (+)/(−)-di-paratoluoyltartaric acid or (−)/(+)-mandelic acid, in an amount equimolar to a compound corresponding to the desired enantiomer of the above compound, precipitating the resulting diastereomeric salt between the chiral resolving agent and the target enantiomer and separating the enantiomer.
    Type: Application
    Filed: January 29, 2004
    Publication date: September 23, 2004
    Applicant: Merrell Pharmaceuticals Inc.
    Inventors: Mitsuo Nakamura, Masatoshi Shiga
  • Process and diastereomeric salts useful for the optical resolution of racemic a-[4- (1,1-dimethylethy) phenyl) -4- (hydroxydipenylmethyl) -1-piperidinebutanol and derivative compounds
    Publication number: 20030078429
    Abstract: A process and diastereomeric salts useful for the optical resolution of racemic &agr;-[4-(1,1-dimethylethyl)phenyl]-4-(hydroxydiphenylmethyl)-1-piperidinebutanol, 4-[4-[4-(hydroxydiphenylmethyl)-1-piperidinyl]-1-hydroxybutyl]-&agr;,&agr;-dimethylbenzeneacetic acid and lower alkyl 4-[4-[4-(hydroxydiphenylmethyl)-1-piperidinyl]-1-hydroxybutyl]-&agr;,&agr;-dimethylbenzeneacetates. The process comprises placing into solution a chiral resolving agent, either (+)/(−)-di-paratoluoyltartaric acid or (−)/(+)-mandelic acid, in an amount equimolar to a compound corresponding to the desired enantiomer of the above compound, precipitating the resulting diastereomeric salt between the chiral resolving agent and the target enantiomer and separating the enantiomer.
    Type: Application
    Filed: July 10, 2002
    Publication date: April 24, 2003
    Inventors: Mitsuo Nakamura, Masatoshi Shiga
  • 2'-Deoxy-3',5'-di-O-alkylcarbonyl-5-fluorouridine derivatives, a process for the preparation of the derivatives and anti-tumor agents containing the derivatives
    Patent number: 4503045
    Abstract: 2'-Deoxy-3',5'-di-O-alkylcarbonyl-5-fluorouridine derivatives possessing strong anti-tumor activity with weak toxicity and represented by the general formula: ##STR1## wherein R stands for an alkyl group, an alkoxy group or a halogen atom, m for zero or an integer of 1-3, and n for an integer of 1-14, with the proviso that when m is 2 or 3, R's may be the same or different and that when m is 2 and the adjacent two R's are alkoxy groups, the two alkyl moieties of the alkoxy groups may be combined to form together with the two adjacent oxa bridging members an alkylenedioxy group as a whole. These derivatives are prepared by acylating a 2'-deoxy-3',5'-di-O-alkylcarbonyl-5-fluorouridine with corresponding benzoyl halides and are useful as active ingredients for anti-tumor agents, especially for oral administration.
    Type: Grant
    Filed: February 13, 1981
    Date of Patent: March 5, 1985
    Assignee: Funai Yakuhin Kogyo Kabushiki Kaisha
    Inventors: Setsuro Fujii, Bompei Yasui, Tomohisa Miyamoto, Masatoshi Shiga, Kazuko Ando, Iwao Hashimoto, Masahiro Kawasaki, Yoichiro Kawai, Yuji Mino