Patents by Inventor Gen Unoki

Gen Unoki 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: 11261182
    Abstract: Provided is a crystal of a novel pyrido[3, 4-d]pyrimidine derivative having excellent CDK 4/6 inhibitory activity. A crystal of a compound represented by formula (I). In the formula, R1 represents a hydrogen atom or a C1-3 alkyl group; R2 represents a hydrogen atom or an oxo group; L represents a single bond or a C1-3 alkylene group; and X represents CH or N.
    Type: Grant
    Filed: November 27, 2017
    Date of Patent: March 1, 2022
    Assignee: Teijin Pharma Limited
    Inventors: Hidetoshi Miyamoto, Tsuyoshi Mizuno, Gen Unoki, Yuki Miyazawa, Naoki Yajima
  • Patent number: 11084814
    Abstract: The purpose of the present invention is to provide a compound that has excellent CDK4/6 inhibitory activity. The present invention is a compound represented by formula (I) or a pharmaceutically acceptable salt of the compound.
    Type: Grant
    Filed: November 27, 2017
    Date of Patent: August 10, 2021
    Assignee: Teijin Pharma Limited
    Inventors: Tsuyoshi Mizuno, Tomohiro Shimada, Gen Unoki, Akinobu Maruyama, Kosuke Sasaki, Takuya Yokosaka, Hiroshi Takahashi, Kyohei Horie, Yuri Sakai
  • Patent number: 10689354
    Abstract: A compound, represented by the following formula or a medically acceptable salt thereof, having an effect of regulating the activity of an androgen receptor. In the formula, X represents S, O; Z represents (Ra)n-A-(CR13R14)0-1—(CR11R12)0-1; A represents aryl, heteroaryl; R1 represents alkyl, cycloalkyl, alkenyl, alkynyl, alkoxyalkyl, aryl, arylalkyl, heterocycle, heterocyclic alkyl; R2 represents hydrogen, halogen, alkyl, cycloalkyl, phenyl; R3 represents hydrogen, halogen, alkyl, cycloalkyl, alkoxyalkyl, alkenyl, alkynyl, cycloalkenyl, aryl, arylalkyl, heterocycle, heterocyclic alkyl, acyl, cycloalkylcarbonyl, benzoyl, spiroalkyl, adamantyl, silyl, R31R32NCO—; R4 and R5 represent hydrogen, halogen, alkyl, phenyl, and cycloalkyl.
    Type: Grant
    Filed: December 9, 2016
    Date of Patent: June 23, 2020
    Assignee: Teijin Pharma Limited
    Inventors: Shinnosuke Hosoda, Gen Unoki, Hidekazu Watanabe, Kosuke Sasaki, Jun Shibata, Emi Yokoyama, Kyohei Horie, Kenichiro Takagi
  • Publication number: 20190367510
    Abstract: The purpose of the present invention is to provide a compound that has excellent CDK4/6 inhibitory activity. The present invention is a compound represented by formula (I) or a pharmaceutically acceptable salt of the compound.
    Type: Application
    Filed: November 27, 2017
    Publication date: December 5, 2019
    Applicant: Teijin Pharma Limited
    Inventors: Tsuyoshi MIZUNO, Tomohiro SHIMADA, Gen UNOKI, Akinobu MARUYAMA, Kosuke SASAKI, Takuya YOKOSAKA, Hiroshi TAKAHASHI, Kyohei HORIE, Yuri SAKAI
  • Publication number: 20190031628
    Abstract: A compound, represented by the following formula or a medically acceptable salt thereof, having an effect of regulating the activity of an androgen receptor. In the formula, X represents S, O; Z represents (Ra)n-A- (CR13R14)0-1—(CR11R12)0-1; A represents aryl, heteroaryl; R1 represents alkyl, cycloalkyl, alkenyl, alkynyl, alkoxyalkyl, aryl, arylalkyl, heterocycle, heterocyclic alkyl; R2 represents hydrogen, halogen, alkyl, cycloalkyl, phenyl; R3 represents hydrogen, halogen, alkyl, cycloalkyl, alkoxyalkyl, alkenyl, alkynyl, cycloalkenyl, aryl, arylalkyl, heterocycle, heterocyclic alkyl, acyl, cycloalkylcarbonyl, benzoyl, spiroalkyl, adamantyl, silyl, R31R32NCO—; R4 and R5 represent hydrogen, halogen, alkyl, phenyl, and cycloalkyl.
    Type: Application
    Filed: December 9, 2016
    Publication date: January 31, 2019
    Applicant: Teijin Pharma Limited
    Inventors: Shinnosuke HOSODA, Gen UNOKI, Hidekazu WATANABE, Kosuke SASAKI, Jun SHIBATA, Emi YOKOYAMA, Kyohei HORIE, Kenichiro TAKAGI
  • Patent number: 10124004
    Abstract: The purpose of the present invention is to provide a compound having an excellent CDK4/6 inhibiting activity. The present invention is a compound represented by general formula (I) or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: May 27, 2016
    Date of Patent: November 13, 2018
    Assignee: Teijin Pharma Limited
    Inventors: Tsuyoshi Mizuno, Tomohiro Shimada, Gen Unoki, Masaru Ebisawa, Susumu Takeuchi, Kunio Minamizono, Kosuke Sasaki, Takuya Yokosaka, Junji Igarashi, Akinobu Maruyama, Hiroshi Takahashi, Kyohei Horie, Yuri Sakai
  • Publication number: 20180161329
    Abstract: The purpose of the present invention is to provide a compound having an excellent CDK4/6 inhibiting activity. The present invention is a compound represented by general formula (I) or a pharmaceutically acceptable salt thereof.
    Type: Application
    Filed: May 27, 2016
    Publication date: June 14, 2018
    Applicant: Teijin Pharma Limited
    Inventors: Tsuyoshi MIZUNO, Tomohiro SHIMADA, Gen UNOKI, Masaru EBISAWA, Susumu TAKEUCHI, Kunio MINAMIZONO, Kosuke SASAKI, Takuya YOKOSAKA, Junji IGARASHI, Akinobu MARUYAMA, Hiroshi TAKAHASHI, Kyohei HORIE, Yuri SAKAI
  • Patent number: 7667036
    Abstract: The Pyrazolo[1,5-a]pyrimidine derivatives represented by formula I and their pharmaceutically acceptable salts exhibit excellent MAPKAP-K2 inhibiting activity. Drugs comprising the compounds as effective ingredients are therefore expected to be useful as therapeutic or prophylactic agents for MAPKAP-K2 mediated disorder, such as inflammatory disease, autoimmune disease, destructive bone disorder, cancer and/or tumour growth.
    Type: Grant
    Filed: August 12, 2005
    Date of Patent: February 23, 2010
    Assignee: Teijin Pharma Limited
    Inventors: Tomomi Kosugi, Minoru Imai, Hiroaki Makino, Mika Takakuwa, Gen Unoki, Kenichiro Kataoka, Dale Robert Mitchell, Donald James Simpson, Clifford John Harris, Joelle Le, Yuko Yamakoshi
  • Publication number: 20090291945
    Abstract: To provide a compound having an excellent cysteine protease inhibitory effect, and to provide a drug for treatment or prevention of the disease selected from the group consisting of osteoporosis, osteoarthritis, chronic rheumatoid arthritis, Paget's disease of bone, hypercalcemia, bone metastasis of cancer, and ostealgia. A compound represented by formula (1) or a pharmaceutically acceptable salt thereof, or a drug or pharmaceutical composition containing the same as an effective component.
    Type: Application
    Filed: April 7, 2009
    Publication date: November 26, 2009
    Applicant: Teijin Pharma Limited
    Inventors: Gen Unoki, Takashi Hayamizu, Hiroshi Eguchi, Yumiko Muroga, Toshiyuki Kaneko, Naoki Yajima
  • Patent number: 7557113
    Abstract: A compound having GSK-3 inhibitory activity. A1 and A3 are a single bond, an aliphatic hydrocarbon group; A2 and A4 are a single bond, CO, COO, CONR, O, OCO, NR, NRCO, NRCOO, etc.; G1 is a single bond, an aliphatic hydrocarbon, aromatic hydrocarbon, heterocyclic; G2 is H, an aliphatic hydrocarbon, an alicyclic hydrocarbon, an aromatic hydrocarbon, heterocyclic; A5 is a single bond, NR; R2 is H, halogen, an aliphatic hydrocarbon, alicyclic hydrocarbon, aromatic hydrocarbon, heterocyclic; A6 is a single bond, NR, CO, NRCO, NRCONR, CONR, COO, O, etc.; R3 is H, halogen, nitro, saturated aliphatic hydrocarbon, alicyclic hydrocarbon, aromatic hydrocarbon, heterocyclic; and R3 may be a trimethylsilyl, formyl, acyl, carboxyl, alkoxylcarbonyl, carbamoyl, alkylcarbamoyl, or cyano group when A6 is CR?CR or C?C, wherein R is H or an lower aliphatic hydrocarbon group.
    Type: Grant
    Filed: August 26, 2004
    Date of Patent: July 7, 2009
    Assignee: Teijin Pharma Limited
    Inventors: Takaharu Tsutsumi, Satoshi Sugiura, Masahiro Koga, Yoshiyuki Matsumoto, Toshihiro Ishii, Akira Nakano, Gen Unoki, Yuri Sakai, Reiko Takarada, Hiroko Ogawa
  • Patent number: 7557110
    Abstract: The Pyrazolo[1,5-a]pyrimidine derivatives represented by formula I and their pharmaceutically acceptable salts exhibit excellent kinase inhibiting activity. Drugs comprising the compounds as effective ingredients are therefore expected to be useful as therapeutic or prophylactic agents for a protein kinase mediated disorder in which kinase is implicated, such as inflammatory disease, autoimmune disease, destructive bone disorder, cancer and/or tumour growth.
    Type: Grant
    Filed: March 1, 2004
    Date of Patent: July 7, 2009
    Assignee: Teijin Pharma Limited
    Inventors: Kenichiro Kataoka, Naotaka Suzuki, Tomomi Kosugi, Minoru Imai, Hiroaki Makino, Mika Takakuwa, Gen Unoki, Aiko Fujino, Yasuhiro Oue, Yuko Yamakoshi, Satoshi Sugiura, Robert Dale Mitchell, James Donald Simpson, John Clifford Harris, Joelle Le
  • Patent number: 7528140
    Abstract: The invention provides pyrrolo[3,2-d]pyrimidine derivatives represented by formula (I), and their medically acceptable salts. The compounds of the invention exhibit GSK-3 inhibiting activity and are therefore expected to be useful as therapeutic or prophylactic agents for conditions in which GSK-3 is implicated, such as diabetes, diabetes complications, Alzheimer's disease, neurodegenerative diseases, manic depression, traumatic encephalopathy, alopecia, inflammatory diseases, cancer and immune deficiency.
    Type: Grant
    Filed: February 24, 2003
    Date of Patent: May 5, 2009
    Assignee: Teijin Limited
    Inventors: Kenichiro Kataoka, Tomomi Kosugi, Toshihiro Ishii, Takahiro Takeuchi, Takaharu Tsutsumi, Akira Nakano, Gen Unoki, Masanori Yamamoto, Yuri Sakai
  • Publication number: 20090054472
    Abstract: A pyrazolopyrimidine derivative represented by formula (1) and pharmaceutically acceptable salt thereof exhibit excellent inhibitory activity against MAPKAP-K2. Accordingly, medicines containing this compound as an active ingredient are expected to be effective for treating diseases mediated by MAPKAP-K2 such as, for example, inflammatory disorder, autoimmune diseases, destructive osteopathy, cancer and/or tumor growth.
    Type: Application
    Filed: September 29, 2008
    Publication date: February 26, 2009
    Applicant: TEIJIN PHARMA LIMITED
    Inventors: Gen UNOKI, Tomomi KOSUGI, Mika TAKAKUWA, Hiroaki MAKINO, Kenichiro KATAOKA, Yuko YAMAKOSHI
  • Patent number: 7473694
    Abstract: A pyrazolopyrimidine derivative represented by formula (1) and pharmaceutically acceptable salt thereof exhibit excellent inhibitory activity against MAPKAP-K2. Accordingly, medicines containing this compound as an active ingredient are expected to be effective for treating diseases mediated by MAPKAP-K2 such as, for example, inflammatory disorder, autoimmune diseases, destructive osteopathy, cancer and/or tumor growth.
    Type: Grant
    Filed: March 17, 2006
    Date of Patent: January 6, 2009
    Assignee: Teijin Pharma Limited
    Inventors: Gen Unoki, Tomomi Kosugi, Mika Takakuwa, Hiroaki Makino, Kenichiro Kataoka, Yuko Yamakoshi
  • Patent number: 7417053
    Abstract: A pyrazolo[1,5-a]pyridine derivative represented by formula (I) and salt thereof exhibit excellent MAPKAP-K2 inhibitory activity. Accordingly, medicines comprising this compound as an active ingredient are expected to be valuable for treating or preventing diseases mediated by MAPKAP-K2 such as inflammatory injury, autoimmune diseases, asteropathia destruens, cancer and/or growth of tumor.
    Type: Grant
    Filed: April 7, 2006
    Date of Patent: August 26, 2008
    Assignee: Teijin Pharma Limited
    Inventors: Gen Unoki, Yoshiyuki Matsumoto, Yohei Matsueda, Tomomi Kosugi, Mika Takakuwa, Hiroaki Makino, Kenichiro Kataoka, Yuko Yamakoshi, Motoko Hamada
  • Publication number: 20070173519
    Abstract: A pyrazolopyrimidine derivative represented by formula (1) and pharmaceutically acceptable salt thereof exhibit excellent inhibitory activity against MAPKAP-K2. Accordingly, medicines containing this compound as an active ingredient are expected to be effective for treating diseases mediated by MAPKAP-K2 such as, for example, inflammatory disorder, autoimmune diseases, destructive osteopathy, cancer and/or tumor growth.
    Type: Application
    Filed: March 17, 2006
    Publication date: July 26, 2007
    Inventors: Gen Unoki, Tomomi Kosugi, Mika Takakuwa, Hiroaki Makino, Kenichiro Kataoka, Yuko Yamakoshi
  • Publication number: 20070072898
    Abstract: A pyrazolo[1,5-a]pyridine derivative represented by formula (I) and salt thereof exhibit excellent MAPKAP-K2 inhibitory activity. Accordingly, medicines comprising this compound as an active ingredient are expected to be valuable for treating or preventing diseases mediated by MAPKAP-K2 such as inflammatory injury, autoimmune diseases, asteropathia destruens, cancer and/or growth of tumor.
    Type: Application
    Filed: April 7, 2006
    Publication date: March 29, 2007
    Inventors: Gen Unoki, Yoshiyuki Matsumoto, Yohei Matsueda, Tomomi Kosugi, Mika Takakuwa, Hiroaki Makino, Kenichiro Kataoka, Yuko Yamakoshi, Motoko Hamada
  • Publication number: 20060189632
    Abstract: The Pyrazolo[1,5-a]pyrimidine derivatives represented by formula I and their pharmaceutically acceptable salts exhibit excellent kinase inhibiting activity. Drugs comprising the compounds as effective ingredients are therefore expected to be useful as therapeutic or prophylactic agents for a protein kinase mediated disorder in which kinase is implicated, such as inflammatory disease, autoimmune disease, destructive bone disorder, cancer and/or tumour growth.
    Type: Application
    Filed: March 1, 2004
    Publication date: August 24, 2006
    Inventors: Kenichiro Kataoka, Naotaka Suzuki, Tomomi Kosugi, Minoru Imai, Hiroaki Makino, Mika Takakuwa, Gen Unoki, Aiko Fujino, Yasuhiro Oue, Yuko Yamakoshi, Satoshi Sugiura, Robert Mitchell, James Simpson, John Harris, Joelle Le
  • Publication number: 20060160831
    Abstract: A compound having GSK-3 inhibitory activity. A1 and A3 are a single bond, an aliphatic hydrocarbon group; A2 and A4 are a single bond, CO, COO, CONR, O, OCO, NR, NRCO, NRCOO, etc.; G1 is a single bond, an aliphatic hydrocarbon, aromatic hydrocarbon, heterocyclic; G2 is H, an aliphatic hydrocarbon, an alicyclic hydrocarbon, an aromatic hydrocarbon, heterocyclic; A5 is a single bond, NR; R2 is H, halogen, an aliphatic hydrocarbon, alicyclic hydrocarbon, aromatic hydrocarbon, heterocyclic; A6 is a single bond, NR, CO, NRCO, NRCONR, CONR, COO, O, etc.; R3 is H, halogen, nitro, saturated aliphatic hydrocarbon, alicyclic hydrocarbon, aromatic hydrocarbon, heterocyclic; and R3 may be a trimethylsilyl, formyl, acyl, carboxyl, alkoxylcarbonyl, carbamoyl, alkylcarbamoyl, or cyano group when A6 is CR?CR or C?C, wherein R is H or an lower aliphatic hydrocarbon group.
    Type: Application
    Filed: August 26, 2004
    Publication date: July 20, 2006
    Applicant: TEIJIN PHARMA LIMITED
    Inventors: Takaharu Tsutsumi, Satoshi Sugiura, Masahiro Koga, Yoshiyuki Matsumoto, Toshihiro Ishii, Akira Nakano, Gen Unoki, Yuri Sakai, Reiko Takarada, Hiroko Ogawa
  • Publication number: 20060135514
    Abstract: The Pyrazolo[1,5-a]pyrimidine derivatives represented by formula I and their pharmaceutically acceptable salts exhibit excellent MAPKAP-K2 inhibiting activity. Drugs comprising the compounds as effective ingredients are therefore expected to be useful as therapeutic or prophylactic agents for MAPKAP-K2 mediated disorder, such as inflammatory disease, autoimmune disease, destructive bone disorder, cancer and/or tumour growth.
    Type: Application
    Filed: August 12, 2005
    Publication date: June 22, 2006
    Inventors: Tomomi Kosugi, Minoru Imai, Hiroaki Makino, Mika Takakuwa, Gen Unoki, Kenichiro Kataoka, Dale Mitchell, Donald Simpson, Clifford Harris, Joelle Le, Yuko Yamakoshi