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1. 发明授权

US09637483B2 Heterocyclic compound 有权
公开(公告)号：US09637483B2
公开(公告)日：2017-05-02
申请号：US14779347
申请日：2014-03-27
申请人： TAKEDA PHARMACEUTICAL COMPANY LIMITED
发明人： Masato Yoshida , Hiroyuki Nagamiya , Yusuke Ohba , Masaki Seto , Takatoshi Yogo , Satoshi Sasaki , Norihito Tokunaga , Kazuyoshi Aso
IPC分类号： A61K31/437 , C07D401/14 , C07D471/04 , C07D519/00
CPC分类号： C07D471/04 , C07D519/00
摘要： Provided is a compound or a salt thereof, which has an excellent JAK inhibitory action, and is useful as a prophylactic or therapeutic agent for autoimmune diseases (rheumatoid arthritis, psoriasis, inflammatory bowel disease, Sjogren's syndrome, Behcet's syndrome, multiple sclerosis, systemic lupus erythematosus, etc.), cancer (leukemia, uterine leiomyosarcoma, prostate cancer, multiple myeloma, cachexia, myelofibrosis, etc.) and the like. The present invention relates to a compound represented by the formula (I) wherein each symbol is as defined in the present specification, or a salt thereof.

2. 发明授权

US09447100B2 Substituted pyrazolo[1,5-A] pyrimidines as calcium receptor modulating agents 有权
标题翻译：取代的吡唑并[1,5-A]嘧啶作为钙受体调节剂
公开(公告)号：US09447100B2
公开(公告)日：2016-09-20
申请号：US14089747
申请日：2013-11-25
申请人： Takeda Pharmaceutical Company Limited
发明人： Tsuneo Yasuma , Akira Mori , Masahiro Kawase , Hiroyuki Kimura , Masato Yoshida , Albert Charles Gyorkos , Scott Alan Pratt , Christopher Peter Corrette
IPC分类号： C07D487/04 , A61K31/519 , A61P19/08 , A61P19/10
CPC分类号： C07D487/04
摘要： There is provided a calcium receptor modulator comprising a compound of the formula (I): wherein ring A is an optionally substituted 5- to 7-membered ring; ring B is an optionally substituted 5- to 7-membered heterocyclic ring; X1 is CR1, CR1R2, N or NR13; X2 is N or NR3; Y is C, CR4 or N, Z is CR5, CR5R6, N or NR7; Ar is an optionally substituted cyclic group; R is H, an optionally substituted hydrocarbon group, etc.; and is a single bond or a double bond; R1, R2, R3, R4, R5, R6, R7 and R13 are independently H, an optionally substituted hydrocarbon group; or a salt thereof or a prodrug thereof. Compounds of the formula (II) and (III): wherein ring A is an optionally substituted 5- to 7-membered ring; Q is C, CR5 or N; R8, R9, R10, R11 and R12 are independently, H, an optionally substituted hydrocarbon group, etc., or a salt thereof are also provided. Also specify X1, R3, R1, Y and X3 in formula (II) and (III) as before.
摘要翻译：也如前所述，在式（II）和（III）中指定X1，R3，R1，Y和X3。

3. 发明授权

US09890145B2 Heterocyclic compound 有权
公开(公告)号：US09890145B2
公开(公告)日：2018-02-13
申请号：US15137161
申请日：2016-04-25
申请人： Takeda Pharmaceutical Company Limited
发明人： Masato Yoshida , Kazuaki Takami , Yusuke Tominari , Zenyu Shiokawa , Akito Shibuya , Yusuke Sasaki , Tony Gibson , Terufumi Takagi
IPC分类号： C07D401/14 , C07D487/04 , C07D417/14 , C07D487/10 , A61P37/00 , C07D403/14 , A61K31/4155 , C07D413/14 , C07D401/04 , C07D409/14 , C07D405/14 , A61K9/06 , A61K9/20 , A61K9/48 , C07D403/04 , C07D471/04 , C07D471/10 , C07D491/107 , C07D495/04
CPC分类号： C07D413/14 , A61K9/06 , A61K9/2018 , A61K9/2054 , A61K9/4858 , C07D401/04 , C07D401/14 , C07D403/04 , C07D403/14 , C07D405/14 , C07D409/14 , C07D417/14 , C07D471/04 , C07D471/10 , C07D487/04 , C07D487/10 , C07D491/107 , C07D495/04
摘要： The present invention provides a heterocyclic compound having an IRAK-4 inhibitory action, which is useful for the prophylaxis or treatment of inflammatory disease, autoimmune disease, osteoarticular degenerative disease, neoplastic disease and the like, and a medicament containing thereof. The present invention relates to a compound represented by the formula (I): wherein each symbol is as defined in the specification, or a salt thereof.

4. 发明授权

US09085578B2 Heterocyclic compound 有权
标题翻译：杂环化合物
公开(公告)号：US09085578B2
公开(公告)日：2015-07-21
申请号：US14379343
申请日：2013-02-19
申请人： Takeda Pharmaceutical Company Limited
发明人： Hiroyuki Nagamiya , Masato Yoshida , Masaki Seto , Shogo Marui , Tsuneo Oda , Yuji Ishichi , Hideo Suzuki , Tomokazu Kusumoto , Takatoshi Yogo , Chul Yun Rhim , Cheolhwan Yoon , Gil Nam Lee , Hyun Bin Kang , Kwang Ok Kim , Hye Sun Jeon
IPC分类号： C07D401/14 , A61K31/437 , C07D471/04 , C07D519/00
CPC分类号： C07D471/04 , C07D519/00
摘要： The present invention provides an agent for the prophylaxis or treatment of autoimmune diseases (e.g., psoriasis, rheumatoid arthritis, inflammatory bowel disease, Sjogren's syndrome, Behcet's disease, multiple sclerosis, systemic lupus erythematosus etc.) and the like, which has a superior Tyk2 inhibitory action.The present invention relates to a compound represented by the formula wherein each symbol is as defined in the specification, or a salt thereof.
摘要翻译：本发明提供了一种用于预防或治疗自身免疫性疾病（例如牛皮癣，类风湿性关节炎，炎性肠病，干燥综合征，白塞病，多发性硬化，系统性红斑狼疮等）等，其具有优异的Tyk2 抑制作用。本发明涉及由下式表示的化合物，其中每个符号如说明书中所定义，或其盐。

5. 发明申请

US20140155416A1 SUBSTITUTED PYRAZOLO[1,5-A] PYRIMIDINES AS CALCIUM RECEPTOR MODULATING AGENTS 审中-公开
标题翻译：作为钙受体调节剂的取代的吡唑并[1,5-A]嘧啶
公开(公告)号：US20140155416A1
公开(公告)日：2014-06-05
申请号：US14089747
申请日：2013-11-25
申请人： Takeda Pharmaceutical Company Limited
发明人： Tsuneo Yasuma , Akira Mori , Masahiro Kawase , Hiroyuki Kimura , Masato Yoshida , Albert Charles Gyorkos , Scott Alan Pratt , Christopher Peter Corrette
IPC分类号： C07D487/04
CPC分类号： C07D487/04
摘要： There is provided a calcium receptor modulator comprising a compound of the formula (I): wherein ring A is an optionally substituted 5- to 7-membered ring; ring B is an optionally substituted 5- to 7-membered heterocyclic ring; X1 is CR1, CR1R2, N or NR13; X2 is N or NR3; Y is C, CR4 or N, Z is CR5, CR5R6, N or NR7; Ar is an optionally substituted cyclic group; R is H, an optionally substituted hydrocarbon group, etc.; and is a single bond or a double bond; R1, R2, R3, R4, R5, R6, R7 and R13 are independently H, an optionally substituted hydrocarbon group; or a salt thereof or a prodrug thereof. Compounds of the formula (II) and (III): wherein ring A is an optionally substituted 5- to 7-membered ring; Q is C, CR5 or N; R8, R9, R10, R11 and R12 are independently, H, an optionally substituted hydrocarbon group, etc., or a salt thereof are also provided. Also specify X1, R3, R1, Y and X3 in formula (II) and (III) as before.
摘要翻译：提供了包含式（I）化合物的钙受体调节剂：其中环A是任选取代的5-至7-元环; 环B是任选取代的5-至7-元杂环; X1是CR1，CR1R2，N或NR13; X2是N或NR3; Y为C，CR4或N，Z为CR5，CR5R6，N或NR7; Ar是任选取代的环状基团; R是H，任选取代的烃基等; 并且是单键或双键; R 1，R 2，R 3，R 4，R 5，R 6，R 7和R 13独立地为H，任选取代的烃基; 或其盐或其前药。式（II）和（III）的化合物：其中环A是任选取代的5-至7-元环; Q为C，CR5或N; R8，R9，R10，R11和R12独立地为氢，任选取代的烃基等，或其盐。也如前所述，在式（II）和（III）中指定X1，R3，R1，Y和X3。

6. 发明授权

US10786506B2 Medicament for treating heart failure 有权
公开(公告)号：US10786506B2
公开(公告)日：2020-09-29
申请号：US16065362
申请日：2016-12-21
申请人： TAKEDA PHARMACEUTICAL COMPANY LIMITED
发明人： Takahisa Matsuda , Takashi Motoyaji , Shuji Kitamura , Masato Yoshida
IPC分类号： A61K31/517 , A61K31/519 , A61P9/04
摘要： The present invention provides a medicament for preventing or treating heart failure. More specifically, the present invention provides a medicament for preventing or treating heart failure, comprising a compound selected from the group consisting of (5R)—N-[1-ethyl-1-(4-ethylphenyl)propyl]-2,7,7-trimethyl-5-phenyl-4,5,6,7-tetrahydropyrazolo[1,5-a]pyrimidine-3-carboxamide, (5R)—N-[1-ethyl-1-(4-methoxyphenyl)propyl]-2,7,7-trimethyl-5-phenyl-4,5,6,7-tetrahydropyrazolo[1,5-a]pyrimidine-3-carboxamide, (5R)—N-[1-ethyl-1-(4-ethylphenyl)propyl]-5-(2-fluorophenyl)-2,7,7-trimethyl-4,5,6,7-tetrahydropyrazolo[1,5-a]pyrimidine-3-carboxamide and salts thereof.

7. 发明申请

US20200054637A1 MEDICINE 审中-公开
公开(公告)号：US20200054637A1
公开(公告)日：2020-02-20
申请号：US16065362
申请日：2016-12-21
申请人： TAKEDA PHARMACEUTICAL COMPANY LIMITED
发明人： Takahisa Matsuda , Takashi Motoyaji , Shuji Kitamura , Masato Yoshida
IPC分类号： A61K31/519 , A61P9/04
摘要： The present invention provides a medicament for preventing or treating heart failure. More specifically, the present invention provides a medicament for preventing or treating heart failure, comprising a compound selected from the group consisting of (5R)—N-[1-ethyl-1-(4-ethylphenyl)propyl]-2,7,7-trimethyl-5-phenyl-4,5,6,7-tetrahydropyrazolo[1,5-a]pyrimidine-3-carboxamide, (5R)—N-[1-ethyl-1-(4-methoxyphenyl)propyl]-2,7,7-trimethyl-5-phenyl-4,5,6,7-tetrahydropyrazolo[1,5-a]pyrimidine-3-carboxamide, (5R)—N-[1-ethyl-1-(4-ethylphenyl)propyl]-5-(2-fluorophenyl)-2,7,7-trimethyl-4,5,6,7-tetrahydropyrazolo[1,5-a]pyrimidine-3-carboxamide and salts thereof.

8. 发明授权

US10849902B2 Medicament for treating heart failure 有权
公开(公告)号：US10849902B2
公开(公告)日：2020-12-01
申请号：US16065362
申请日：2016-12-21
申请人： TAKEDA PHARMACEUTICAL COMPANY LIMITED
发明人： Takahisa Matsuda , Takashi Motoyaji , Shuji Kitamura , Masato Yoshida
IPC分类号： A61K31/517 , A61K31/519 , A61P9/04
摘要： The present invention provides a medicament for preventing or treating heart failure. More specifically, the present invention provides a medicament for preventing or treating heart failure, comprising a compound selected from the group consisting of (5R)—N-[1-ethyl-1-(4-ethylphenyl)propyl]-2,7,7-trimethyl-5-phenyl-4,5,6,7-tetrahydropyrazolo[1,5-a]pyrimidine-3-carboxamide, (5R)—N-[1-ethyl-1-(4-methoxyphenyl)propyl]-2,7,7-trimethyl-5-phenyl-4,5,6,7-tetrahydropyrazolo[1,5-a]pyrimidine-3-carboxamide, (5R)—N-[1-ethyl-1-(4-ethylphenyl)propyl]-5-(2-fluorophenyl)-2,7,7-trimethyl-4,5,6,7-tetrahydropyrazolo[1,5-a]pyrimidine-3-carboxamide and salts thereof.

9. 发明授权

US10800754B2 Heterocyclic amide compound 有权
公开(公告)号：US10800754B2
公开(公告)日：2020-10-13
申请号：US16332993
申请日：2017-09-14
申请人： TAKEDA PHARMACEUTICAL COMPANY LIMITED
发明人： Takaharu Hirayama , Yasuhiro Hirata , Yusuke Tominari , Naoki Iwamura , Yusuke Sasaki , Moriteru Asano , Terufumi Takagi , Masanori Okaniwa , Masato Yoshida , Shinichi Imamura
IPC分类号： C07D401/04 , C07D401/14 , C07D407/14 , C07D409/14 , C07D417/14 , A61P35/00
摘要： Provided is a heterocyclic amide compound that may have a PRS inhibitory action and is expected to be useful as a prophylactic or therapeutic agent for PRS associated diseases and the like including cancer. A compound represented by the following formula (I): wherein each symbol is as described in the DESCRIPTION, or a salt thereof.

10. 发明授权

US09321757B2 Heterocyclic compound 有权
标题翻译：杂环化合物
公开(公告)号：US09321757B2
公开(公告)日：2016-04-26
申请号：US14533326
申请日：2014-11-05
申请人： Takeda Pharmaceutical Company Limited
发明人： Masato Yoshida , Kazuaki Takami , Yusuke Tominari , Zenyu Shiokawa , Akito Shibuya , Yusuke Sasaki , Tony Gibson , Terufumi Takagi
IPC分类号： C07D401/14 , C07D487/04 , C07D417/14 , C07D487/10 , A61P37/00 , C07D403/14 , A61K31/4155 , C07D413/14 , C07D409/14 , C07D405/14 , C07D401/04 , A61K9/06 , A61K9/20 , A61K9/48
CPC分类号： C07D413/14 , A61K9/06 , A61K9/2018 , A61K9/2054 , A61K9/4858 , C07D401/04 , C07D401/14 , C07D403/04 , C07D403/14 , C07D405/14 , C07D409/14 , C07D417/14 , C07D471/04 , C07D471/10 , C07D487/04 , C07D487/10 , C07D491/107 , C07D495/04
摘要： The present invention provides a heterocyclic compound having an IRAK-4 inhibitory action, which is useful for the prophylaxis or treatment of inflammatory disease, autoimmune disease, osteoarticular degenerative disease, neoplastic disease and the like, and a medicament containing thereof. The present invention relates to a compound represented by the formula (I): wherein each symbol is as defined in the specification, or a salt thereof.
摘要翻译：本发明提供具有IRAK-4抑制作用的杂环化合物，其可用于预防或治疗炎性疾病，自身免疫性疾病，骨关节炎性退行性疾病，肿瘤性疾病等，以及含有它们的药物。本发明涉及由式（I）表示的化合物：其中每个符号如说明书中所定义，或其盐。

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