Patents by Inventor Hiroaki Shirahase

Hiroaki Shirahase 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: 11013728
    Abstract: The present invention aims to provide a novel cyclin-dependent kinase 8 and/or 19 inhibitor useful as an anti-cancer agent. The present invention relates to a cyclin-dependent kinase 8 and/or 19 inhibitor containing a compound represented by the formula (I): [wherein each symbol is as defined in the DESCRIPTION] or a pharmaceutically acceptable salt thereof as an active ingredient, and use thereof as an agent for preventing and/or treating cancer.
    Type: Grant
    Filed: April 2, 2018
    Date of Patent: May 25, 2021
    Assignee: Kyoto Pharmaceutical Industries, Ltd.
    Inventors: Tatsuya Kitao, Shigemitsu Takeda, Yoshimichi Shoji, Hiroaki Shirahase
  • Publication number: 20210100783
    Abstract: The present invention aims to provide a novel cyclin-dependent kinase 8 and/or 19 inhibitor useful as an anti-cancer agent. The present invention relates to a cyclin-dependent kinase 8 and/or 19 inhibitor containing a compound represented by the formula (I): [wherein each symbol is as defined in the DESCRIPTION] or a pharmaceutically acceptable salt thereof as an active ingredient, and use thereof as an agent for preventing and/or treating cancer.
    Type: Application
    Filed: April 2, 2018
    Publication date: April 8, 2021
    Applicant: Kyoto Pharmaceutical Industries, Ltd.
    Inventors: Tatsuya KITAO, Shigemitsu TAKEDA, Yoshimichi SHOJI, Hiroaki SHIRAHASE
  • Patent number: 10059663
    Abstract: Provided is a compound showing a bone formation promoting action (and/or bone resorption suppressive action). A compound of the formula (I) or a pharmacologically acceptable salt: [wherein each substituent is as defined in the DESCRIPTION], has low toxicity, shows good pharmacokinetics, has an action to promote bone formation, and is useful for the prophylaxis or treatment of metabolic bone diseases (osteoporosis, fibrous osteitis (hyperparathyroidism), osteomalacia, Paget's disease that influences the systemic bone metabolism parameter etc.) associated with a decrease in the bone formation ability as compared to the bone resorption capacity.
    Type: Grant
    Filed: August 29, 2014
    Date of Patent: August 28, 2018
    Assignee: KYOTO PHARMACEUTICAL INDUSTRIES, LTD.
    Inventors: Hiroaki Shirahase, Kenji Takahashi, Yoshimichi Shoji, Shigemitsu Takeda
  • Publication number: 20160207883
    Abstract: Provided is a compound showing a bone formation promoting action (and/or bone resorption suppressive action). A compound of the formula (I) or a pharmacologically acceptable salt: [wherein each substituent is as defined in the DESCRIPTION], has low toxicity, shows good pharmacokinetics, has an action to promote bone formation, and is useful for the prophylaxis or To treatment of metabolic bone diseases (osteoporosis, fibrous osteitis (hyperparathyroidism), osteomalacia, Paget's disease that influences the systemic bone metabolism parameter etc.) associated with a decrease in the bone formation ability as compared to the bone resorption capacity.
    Type: Application
    Filed: August 29, 2014
    Publication date: July 21, 2016
    Applicant: Kyoto Pharmaceutical Industries, Ltd.
    Inventors: Hiroaki SHIRAHASE, Kenji TAKAHASHI, Yoshimichi SHOJI, Shigemitsu TAKEDA
  • Publication number: 20100022582
    Abstract: The present invention provide a tetrahydroisoquinoline compound having a superior ACAT-inhibitory activity and/or anti-oxidation action, particularly, novel compound represented by the formula (I) (wherein each symbol is as described in the specification) and a pharmaceutically acceptable salt thereof.
    Type: Application
    Filed: March 10, 2006
    Publication date: January 28, 2010
    Inventors: Kenji Takahashi, Hiroaki Shirahase, Kazuyoshi Kunishiro, Masayasu Kasai
  • Patent number: 7557123
    Abstract: The novel heterocyclic compound of the present invention is a novel heterocyclic compound having the formula (I) Y: R15—C(R14)?N—O— wherein R1 is H or C1-6 alkyl, R2 is H, —CO—C(R4)?C(R4)—R5 wherein R4 is H or C1-4 alkyl, and R5 is C4-8 alkyl, C2-8 alkenyl and the like, and the like, Y is the following group wherein X is O or S, R7 is the same as R4, R8 is R10—C(R9)?C(R9)— wherein R9 is the same as R4, R10 is C3-6 alkyl and the like, and the like, R14 is the same as R4, and R15 is aryl and the like, Y—(CH2)n-O— is bonded to the 6- or 7-position of the tetrahydroisoquinoline skeleton, and n is an integer of 1 to 4, or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: May 27, 2002
    Date of Patent: July 7, 2009
    Assignee: Kyoto Pharmaceutical Industries, Ltd.
    Inventors: Hiroshi Matsui, Hideo Kobayashi, Satoru Azukizawa, Masayasu Kasai, Akihisa Yoshimi, Hiroaki Shirahase
  • Patent number: 7429612
    Abstract: The present invention provides an indoline compound represented by the formula (I) wherein each symbol is as defined in the DESCRIPTION, or a pharmaceutically acceptable salt thereof, and a pharmaceutical composition containing this indoline compound or a pharmaceutically acceptable salt thereof. The compound of the present invention shows superior ACAT inhibitory effect and superior lipoperoxidation inhibitory effect and is useful as an ACAT inhibitor or a lipoperoxidation inhibitor.
    Type: Grant
    Filed: July 16, 2003
    Date of Patent: September 30, 2008
    Assignee: Kyoto Pharmaceutical Industries, Ltd.
    Inventors: Shouji Kamiya, Miho Ikai, Kenji Takahash, Tadatsugu Tarumi, Masayasu Kasai, Akihisa Yoshimi, Hiroaki Shirahase
  • Publication number: 20060128787
    Abstract: The present invention provides an indoline compound represented by the formula (I) wherein each symbol is as defined in the DESCRIPTION, or a pharmaceutically acceptable salt thereof, and a pharmaceutical composition containing this indoline compound or a pharmaceutically acceptable salt thereof. The compound of the present invention shows superior ACAT inhibitory effect and superior lipoperoxidation inhibitory effect and is useful as an ACAT inhibitor or a lipoperoxidation inhibitor.
    Type: Application
    Filed: July 16, 2003
    Publication date: June 15, 2006
    Inventors: Shouji Kamiya, Miho Ikai, Kenji Takahash, Tadatsugu Tarumi, Masayasu Kasai, Akihisa Yoshimi, Hiroaki Shirahase
  • Patent number: 6872732
    Abstract: The novel heterocyclic derivative of the present invention is a novel heterocyclic derivative having the formula (I?) wherein R1 is a hydrogen atom or C1-6 alkyl, R2 is —CO—C(R4)?C(R4)—R5 wherein R4 is a hydrogen atom or C1-4 alkyl, and R5 is C4-8 alkyl, C2-8 alkenyl, aryl or aromatic heterocycle, —CO—C?C—R6 wherein R6 is C1-8 alkyl and the like, R3 is a hydrogen atom or C1-4 alkyl, X is an oxygen atom or a sulfur atom, R20 is optionally substituted phenyl, and n is an integer of 1 to 4, or a pharmaceutically acceptable salt thereof. The compound (I?) of the present invention is useful as a hypoglycemic agent, a hypolipidemic agent, an insulin resistance improver, a therapeutic agent of diabetes, a therapeutic agent of diabetic complications, a glucose tolerance improver, an anti-arteriosclerosis agent, an anti-obesity agent, an antiinflammatory agent, an agent for the prophylaxis or treatment of PPAR-mediated diseases and an agent for the prophylaxis or treatment of syndrome X.
    Type: Grant
    Filed: May 27, 2002
    Date of Patent: March 29, 2005
    Assignee: Kyoto Pharmaceutical Industries, Ltd.
    Inventors: Hiroshi Matsui, Hideo Kobayashi, Satoru Azukizawa, Masayasu Kasai, Akihisa Yoshimi, Hiroaki Shirahase
  • Publication number: 20040220215
    Abstract: The novel heterocyclic compound of the present invention is a novel heterocyclic compound having the formula (I) 1
    Type: Application
    Filed: November 25, 2003
    Publication date: November 4, 2004
    Inventors: Hiroshi Matsui, Hideo Kobayashi, Satoru Azukizawa, Masayasu Kasai, Akihisa Yoshimi, Hiroaki Shirahase
  • Publication number: 20040180924
    Abstract: The novel heterocyclic derivative of the present invention is a novel heterocyclic derivative having the formula (I′) 1
    Type: Application
    Filed: November 25, 2003
    Publication date: September 16, 2004
    Inventors: Hiroshi Matsui, Hideo Kobayashi, Satoru Azukizawa, Masayasu Kasai, Akihisa Yoshimi, Hiroaki Shirahase
  • Patent number: 6589963
    Abstract: A heterocyclic compound of the formula [I] wherein R1 is hydrogen atom or lower alkyl, R2 is hydrogen atom, alkyl optionally having a substituent and the like, R3 is hydrogen atom, lower alkyl and the like, A is a single bond or >N—R5 wherein R5 is hydrogen atom or lower alkyl, B is lower alkylene, and Y is aryl optionally having a substituent and the like, and a pharmaceutically acceptable salt thereof show a hypoglycemic action, a blood hypolipidemic action, an insulin resistance-improving action and a PPAR activating action, and are useful as a hypoglycemic agent, a hypolipidemic agent, an insulin resistance improver, a therapeutic agent of diabetes, a therapeutic agent of diabetic complication, a glucose tolerance improver, an anti-atherosclerosis agent, an anti-obesity agent, an antiinflammatory agent, an agent for the prophylaxis or treatment of PPAR-mediated disease and an agent for the prophylaxis or treatment of syndrome X.
    Type: Grant
    Filed: May 31, 2002
    Date of Patent: July 8, 2003
    Assignee: Kyoto Pharmaceutical Industries, Ltd.
    Inventors: Hiroshi Matsui, Hideo Kobayashi, Satoru Azukizawa, Masayasu Kasai, Akihisa Yoshimi, Hiroaki Shirahase
  • Publication number: 20030027836
    Abstract: A heterocyclic compound of the formula [I] 1
    Type: Application
    Filed: May 31, 2002
    Publication date: February 6, 2003
    Inventors: Hiroshi Matsui, Hideo Kobayashi, Satoru Azukizawa, Masayasu Kasai, Akihisa Yoshimi, Hiroaki Shirahase
  • Patent number: 6414012
    Abstract: Heterocyclic derivatives of the formula (I) wherein each symbol is as defined in the specification, pharmaceutically acceptable salts thereof and method of producing them. Pharmaceutical compositions containing the heterocyclic derivative or a pharmaceutically acceptable salt thereof, particularly, ACAT inhibitors and lipoperoxidation inhibitors. The heterocyclic derivatives and pharmaceutically acceptable salts thereof of the present invention show superior ACAT inhibitory activity and lipoperoxidation inhibitory activity, and are useful as ACAT inhibitors and hyperlipemia inhibitors. To be specific, they are useful for the prevention and treatment of arteriosclerotic lesions of arteriosclerosis, hyperlipemia and diabetes, as well as ischemic diseases of brain, heart and the like.
    Type: Grant
    Filed: August 12, 1999
    Date of Patent: July 2, 2002
    Assignee: Sankyo Company, Limited
    Inventors: Hiroshi Matsui, Shoji Kamiya, Hiroaki Shirahase, Shohei Nakamura, Katsuo Wada
  • Patent number: 6262108
    Abstract: The cromoglycic acid compound of the formula (I) has an antirheumatic action, an antiinflammatory action and an immunomodulating action. This compound is effective for the inhibition of the symptoms of chronic rheumatoid arthritis and is associated with fewer side effects. Therefore, the antirheumatic agent of the present invention can be used beneficially for the treatment of rheumatoid arthritis. In addition, this compound has anti-type I and anti-type IV allergic activities. Therefore, the compound can be used beneficially mainly for the treatment of allergic dermatitis, in which a type IV allergic reaction is involved, such as contact dermatitis, in which a type IV allergic reaction is involved, atopic dermatitis, in which type I and type IV allergic reactions are involved and the like.
    Type: Grant
    Filed: July 28, 2000
    Date of Patent: July 17, 2001
    Assignee: Kyoto Pharmaceutical Industries, Ltd.
    Inventors: Hiroaki Shirahase, Akihisa Yoshimi, Shohei Nakamura, Mamoru Kanda, Fumio Fukata
  • Patent number: 6204392
    Abstract: Heterocyclic derivatives of the formula (I) wherein each symbol is as defined in the specification, pharmaceutically acceptable salts thereof and method of producing them. Pharmaceutical compositions containing the heterocyclic derivative or a pharmaceutically acceptable salt thereof, particularly, ACAT inhibitors and lipoperoxidation inhibitors. The heterocyclic derivatives and pharmaceutically acceptable salts thereof of the present invention show superior ACAT inhibitory activity and lipoperoxidation inhibitory activity, and are useful as ACAT inhibitors and hyperlipemia inhibitors. To be specific, they are useful for the prevention and treatment of arteriosclerotic lesions of arteriosclerosis, hyperlipemia and diabetes, as well as ischemic diseases of brain, heart and the like.
    Type: Grant
    Filed: April 1, 1999
    Date of Patent: March 20, 2001
    Assignee: Sankyo Company, Limited
    Inventors: Hiroshi Matsui, Shoji Kamiya, Hiroaki Shirahase, Shohei Nakamura
  • Patent number: 6201011
    Abstract: A therapeutic agent for allergic dermatitis caused by type IV allergic reaction, which contains diethyl L-lysylcromoglycate of the formula: or a nontoxic salt thereof as an active ingredient. This therapeutic agent for allergic dermatitis is effective for the treatment of allergic dermatitis caused by type IV allergic reaction, such as contact dermatitis mainly induced by type IV allergic reaction and atopic dermatitis induced by type I and type IV allergic reactions.
    Type: Grant
    Filed: February 26, 1999
    Date of Patent: March 13, 2001
    Assignee: Kyoto Pharmaceutical Industries, Ltd.
    Inventors: Hiroaki Shirahase, Akihisa Yoshimi, Shohei Nakamura, Mamoru Kanda
  • Patent number: 6200988
    Abstract: A heterocyclic derivative of the formula (I) wherein each symbol is as defined in the specification, and pharmaceutically acceptable salts thereof. The compound (I) of the present invention and pharmaceutically acceptable salts thereof exhibit superior ACAT inhibitory activity and lipoperoxidation inhibitory activity in mammals, and are useful as ACAT inhibitors and lipoperoxidation inhibitors. Specifically, they are useful for the prophylaxis and treatment of arteriosclerosis, hyperlipemia, arteriosclerosis in diabetes, and cerebrovascular and cardiovascular ischemic diseases.
    Type: Grant
    Filed: February 18, 2000
    Date of Patent: March 13, 2001
    Assignee: Kyoto Pharmaceutical Industries, Ltd.
    Inventors: Shoji Kamiya, Hiroaki Shirahase, Hiroshi Matsui, Shohei Nakamura, Katsuo Wada
  • Patent number: 6149923
    Abstract: An antirheumatic agent comprising diethyl L-lysylcromoglycate of the following formula ##STR1## or a nontoxic salt thereof as an active ingredient. This compound has an anti-inflammatory action and immunomodulating action, is absorbed by oral administration to be delivered efficiently to local sites, and is associated with fewer side effects, so that it serves well as an antirheumatic agent that can be administered orally.
    Type: Grant
    Filed: December 10, 1998
    Date of Patent: November 21, 2000
    Assignee: Kyoto Pharmaceutical Industries, Ltd.
    Inventors: Hiroaki Shirahase, Akihisa Yoshimi, Fumio Fukata, Hideki Okunishi, Yuta Kobayashi
  • Patent number: RE38970
    Abstract: A heterocyclic derivative of the formula (I) wherein each symbol is as defined in the specification, and pharmaceutically acceptable salts thereof. The compound (I) of the present invention and pharmaceutically acceptable salts thereof exhibit superior ACAT inhibitory activity and lipoperoxidation inhibitory activity in mammals, and are useful as ACAT inhibitors and lipoperoxidation inhibitors. Specifically, they are useful for the prophylaxis and treatment of arteriosclerosis, hyperlipemia, arteriosclerosis in diabetes, and cerebrovascular and cardiovascular ischemic diseases.
    Type: Grant
    Filed: September 30, 1996
    Date of Patent: February 7, 2006
    Assignee: Kyoto Pharmaceutical Industries, Ltd.
    Inventors: Shoji Kamiya, Hiroaki Shirahase, Hiroshi Matsui, Shohei Nakamura, Katsuo Wada