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).
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Patent number: 11261182Abstract: 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: GrantFiled: November 27, 2017Date of Patent: March 1, 2022Assignee: Teijin Pharma LimitedInventors: Hidetoshi Miyamoto, Tsuyoshi Mizuno, Gen Unoki, Yuki Miyazawa, Naoki Yajima
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Patent number: 11084814Abstract: 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: GrantFiled: November 27, 2017Date of Patent: August 10, 2021Assignee: Teijin Pharma LimitedInventors: Tsuyoshi Mizuno, Tomohiro Shimada, Gen Unoki, Akinobu Maruyama, Kosuke Sasaki, Takuya Yokosaka, Hiroshi Takahashi, Kyohei Horie, Yuri Sakai
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Patent number: 10689354Abstract: 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: GrantFiled: December 9, 2016Date of Patent: June 23, 2020Assignee: Teijin Pharma LimitedInventors: Shinnosuke Hosoda, Gen Unoki, Hidekazu Watanabe, Kosuke Sasaki, Jun Shibata, Emi Yokoyama, Kyohei Horie, Kenichiro Takagi
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Publication number: 20190367510Abstract: 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: ApplicationFiled: November 27, 2017Publication date: December 5, 2019Applicant: Teijin Pharma LimitedInventors: Tsuyoshi MIZUNO, Tomohiro SHIMADA, Gen UNOKI, Akinobu MARUYAMA, Kosuke SASAKI, Takuya YOKOSAKA, Hiroshi TAKAHASHI, Kyohei HORIE, Yuri SAKAI
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Publication number: 20190031628Abstract: 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: ApplicationFiled: December 9, 2016Publication date: January 31, 2019Applicant: Teijin Pharma LimitedInventors: Shinnosuke HOSODA, Gen UNOKI, Hidekazu WATANABE, Kosuke SASAKI, Jun SHIBATA, Emi YOKOYAMA, Kyohei HORIE, Kenichiro TAKAGI
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Patent number: 10124004Abstract: 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: GrantFiled: May 27, 2016Date of Patent: November 13, 2018Assignee: Teijin Pharma LimitedInventors: 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
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Publication number: 20180161329Abstract: 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: ApplicationFiled: May 27, 2016Publication date: June 14, 2018Applicant: Teijin Pharma LimitedInventors: 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
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Patent number: 7667036Abstract: 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: GrantFiled: August 12, 2005Date of Patent: February 23, 2010Assignee: Teijin Pharma LimitedInventors: 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
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Publication number: 20090291945Abstract: 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: ApplicationFiled: April 7, 2009Publication date: November 26, 2009Applicant: Teijin Pharma LimitedInventors: Gen Unoki, Takashi Hayamizu, Hiroshi Eguchi, Yumiko Muroga, Toshiyuki Kaneko, Naoki Yajima
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Patent number: 7557113Abstract: 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: GrantFiled: August 26, 2004Date of Patent: July 7, 2009Assignee: Teijin Pharma LimitedInventors: Takaharu Tsutsumi, Satoshi Sugiura, Masahiro Koga, Yoshiyuki Matsumoto, Toshihiro Ishii, Akira Nakano, Gen Unoki, Yuri Sakai, Reiko Takarada, Hiroko Ogawa
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Patent number: 7557110Abstract: 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: GrantFiled: March 1, 2004Date of Patent: July 7, 2009Assignee: Teijin Pharma LimitedInventors: 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
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Patent number: 7528140Abstract: 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: GrantFiled: February 24, 2003Date of Patent: May 5, 2009Assignee: Teijin LimitedInventors: Kenichiro Kataoka, Tomomi Kosugi, Toshihiro Ishii, Takahiro Takeuchi, Takaharu Tsutsumi, Akira Nakano, Gen Unoki, Masanori Yamamoto, Yuri Sakai
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Publication number: 20090054472Abstract: 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: ApplicationFiled: September 29, 2008Publication date: February 26, 2009Applicant: TEIJIN PHARMA LIMITEDInventors: Gen UNOKI, Tomomi KOSUGI, Mika TAKAKUWA, Hiroaki MAKINO, Kenichiro KATAOKA, Yuko YAMAKOSHI
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Patent number: 7473694Abstract: 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: GrantFiled: March 17, 2006Date of Patent: January 6, 2009Assignee: Teijin Pharma LimitedInventors: Gen Unoki, Tomomi Kosugi, Mika Takakuwa, Hiroaki Makino, Kenichiro Kataoka, Yuko Yamakoshi
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Patent number: 7417053Abstract: 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: GrantFiled: April 7, 2006Date of Patent: August 26, 2008Assignee: Teijin Pharma LimitedInventors: Gen Unoki, Yoshiyuki Matsumoto, Yohei Matsueda, Tomomi Kosugi, Mika Takakuwa, Hiroaki Makino, Kenichiro Kataoka, Yuko Yamakoshi, Motoko Hamada
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Publication number: 20070173519Abstract: 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: ApplicationFiled: March 17, 2006Publication date: July 26, 2007Inventors: Gen Unoki, Tomomi Kosugi, Mika Takakuwa, Hiroaki Makino, Kenichiro Kataoka, Yuko Yamakoshi
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Publication number: 20070072898Abstract: 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: ApplicationFiled: April 7, 2006Publication date: March 29, 2007Inventors: Gen Unoki, Yoshiyuki Matsumoto, Yohei Matsueda, Tomomi Kosugi, Mika Takakuwa, Hiroaki Makino, Kenichiro Kataoka, Yuko Yamakoshi, Motoko Hamada
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Publication number: 20060189632Abstract: 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: ApplicationFiled: March 1, 2004Publication date: August 24, 2006Inventors: 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
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Publication number: 20060160831Abstract: 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: ApplicationFiled: August 26, 2004Publication date: July 20, 2006Applicant: TEIJIN PHARMA LIMITEDInventors: Takaharu Tsutsumi, Satoshi Sugiura, Masahiro Koga, Yoshiyuki Matsumoto, Toshihiro Ishii, Akira Nakano, Gen Unoki, Yuri Sakai, Reiko Takarada, Hiroko Ogawa
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Publication number: 20060135514Abstract: 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: ApplicationFiled: August 12, 2005Publication date: June 22, 2006Inventors: Tomomi Kosugi, Minoru Imai, Hiroaki Makino, Mika Takakuwa, Gen Unoki, Kenichiro Kataoka, Dale Mitchell, Donald Simpson, Clifford Harris, Joelle Le, Yuko Yamakoshi