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1. 发明申请

WO2011016576A1 ALANINE DERIVATIVES AS INHIBITORS OF APOPTOSIS PROTEINS 审中-公开
标题翻译：作为APOPTOSIS蛋白的抑制剂的ALANINE衍生物
公开(公告)号：WO2011016576A1
公开(公告)日：2011-02-10
申请号：PCT/JP2010/063447
申请日：2010-08-03
申请人： TAKEDA PHARMACEUTICAL COMPANY LIMITED , HASHIMOTO, Kentaro , ISHIKAWA, Tomoyasu , OGURO, Yuya
发明人： HASHIMOTO, Kentaro , ISHIKAWA, Tomoyasu , OGURO, Yuya
IPC分类号： C07D487/04 , A61K31/498 , A61P35/00
CPC分类号： C07D487/04
摘要： The present invention provides a compound represented by the formula (I) wherein each symbol is as defined in the specification, or a salt thereof. The compound of the present invention shows a strong IAP antagonistic activity.
摘要翻译：本发明提供由式（I）表示的化合物，其中每个符号如说明书中所定义，或其盐。本发明化合物显示出强的IAP拮抗活性。

2. 发明申请

WO2007004749A1 FUSED HETEROCYCLIC DERIVATIVES AND USE THEREOF 审中-公开
标题翻译：熔融杂环衍生物及其用途
公开(公告)号：WO2007004749A1
公开(公告)日：2007-01-11
申请号：PCT/JP2006/313815
申请日：2006-07-05
申请人： TAKEDA PHARMACEUTICAL COMPANY LIMITED , IMAMURA, Shinichi , OGURO, Yuya
发明人： IMAMURA, Shinichi , OGURO, Yuya
IPC分类号： C07D487/04 , A61K31/519 , A61P35/00
CPC分类号： C07D487/04
摘要： The present invention provides a fused heterocyclic derivative showing a potent kinase inhibitory activity and use thereof. A compound represented by the formula: (I) wherein ring A is an optionally substituted pyrrole ring, X is an optionally substituted CH, Y is an optionally substituted CH or nitrogen atom, Z is an optionally substituted divalent hydrocarbon group or optionally substituted divalent heterocyclic group, T is a single bond or an optionally substituted C 1-3 alkylene group, and U is an optionally substituted amido group, an optionally substituted sulfonamido group, an optionally substituted ureido group, an optionally substituted carbamoyl group or an optionally substituted thioureido group, or a salt thereof, and a pharmaceutical agent containing the compound or a prodrug thereof, which is a kinase (VEGFR, VEGFR2, PDGFR, TIE2) inhibitor, an angiogenesis inhibitor, an agent for the prophylaxis or treatment of cancer, an agent for inhibiting growth of cancer or an agent for suppressing metastasis of cancer.
摘要翻译：本发明提供了显示出强的激酶抑制活性的稠合杂环衍生物及其应用。由式（I）表示的化合物，其中环A是任选取代的吡咯环，X是任选取代的CH，Y是任选取代的CH或氮原子，Z是任选取代的二价烃基或任选取代的二价杂环基团，T是单键或任选取代的C 1-3 - 亚烷基，U是任选取代的酰胺基，任选取代的亚磺酰氨基，任选取代的脲基，任选取代的氨基甲酰基基团或任选取代的硫脲基或其盐，以及含有作为激酶（VEGFR，VEGFR2，PDGFR，TIE2）抑制剂的化合物或其前药的药剂，血管发生抑制剂，预防剂或治疗癌症，抑制癌症生长的药剂或抑制癌症转移的药剂。

3. 发明申请

WO2008150015A1 HETEROBICYCLIC COMPOUNDS AS KINASE INHIBITORS 审中-公开
标题翻译：异环化合物作为激酶抑制剂
公开(公告)号：WO2008150015A1
公开(公告)日：2008-12-11
申请号：PCT/JP2008/060629
申请日：2008-06-04
申请人： TAKEDA PHARMACEUTICAL COMPANY LIMITED , OGURO, Yuya , IMAMURA, Shinichi , CARY, Douglas, R. , OKANIWA, Masanori
发明人： OGURO, Yuya , IMAMURA, Shinichi , CARY, Douglas, R. , OKANIWA, Masanori
IPC分类号： C07D277/82 , C07D471/04 , C07D471/14 , C07D417/12 , C07D513/04 , A61K31/428 , A61K31/429 , A61K31/437 , A61K31/519 , A61P35/00
CPC分类号： C07D471/04 , C07D417/12 , C07D471/14 , C07D513/04
摘要： A compound represented by the formula (I): wherein Z 1 , Z 2 , Z 3 and Z 4 are the following combination, (Z 1 ,Z 2 ,Z 3 ,Z 4 )=(CR 4 ,N,CR 5 ,C), (N,N,CR 5 ,C), (N,C,CR 5 ,N), (S,C,CR 5 ,C) or (S,C,N,C); R 1 and R 2 are the same or different and each is (1) a hydrogen atom, (2) a halogen atom, (3) a group bonded via a carbon atom, (4) a group bonded via a nitrogen atom, (5) a group bonded via an oxygen atom or (6) a group bonded via a sulfur atom; R 3 is an amino optionally having substituent(s); R 4 and R 5 are the same or different and each is (1) a hydrogen atom, (2) a halogen atom, (3) a group bonded via a carbon atom, (4) a group bonded via a nitrogen atom, (5) a group bonded via an oxygen atom or (6) a group bonded via a sulfur atom; R 3 and R 4 optionally form a ring optionally having substituent(s); and a group represented by the formula (A) is a cyclic group optionally having substituent(s), or a salt thereof.
摘要翻译：由式（I）表示的化合物：其中Z 1，Z 2，Z 3和Z 4是以下组合：（Z 1，Z 2，Z 3，Z 4）=（CR 4，N，CR 5，C），（N，N， C），（N，C，CR5，N），（S，C，CR5，C）或（S，C，N，C） R1和R2相同或不同，分别为（1）氢原子，（2）卤素原子，（3）通过碳原子键合的基团，（4）通过氮原子键合的基团，（5）通过氧原子键合的基团或（6）通过硫原子键合的基团; R3是任选具有取代基的氨基; R4和R5相同或不同，分别为（1）氢原子，（2）卤素原子，（3）通过碳原子键合的基团，（4）通过氮原子键合的基团，（5）通过氧原子键合的基团或（6）通过硫原子键合的基团; R3和R4任选地形成任选具有取代基的环; 由式（A）表示的基团是任选具有取代基的环状基团或其盐。

4. 发明申请

WO2010101302A1 THIENOPYRIMIDINE AS CDC7 KINASE INHIBITORS 审中-公开
标题翻译：三硝基嘧啶作为CDC7激酶抑制剂
公开(公告)号：WO2010101302A1
公开(公告)日：2010-09-10
申请号：PCT/JP2010/054073
申请日：2010-03-04
申请人： TAKEDA PHARMACEUTICAL COMPANY LIMITED , OGURO, Yuya , KURASAWA, Osamu
发明人： OGURO, Yuya , KURASAWA, Osamu
IPC分类号： C07D495/04 , A61K31/519 , A61P35/00
CPC分类号： C07D495/04
摘要： 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, or a prodrug thereof, which is useful for the prophylaxis or treatment of cancer.
摘要翻译：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，或其盐或其前药，其可用于预防或治疗癌症。

5. 发明申请

WO2009107850A2 FUSED HETEROCYCLIC DERIVATIVE AND USE THEREOF 审中-公开
标题翻译：熔融杂环衍生物及其用途
公开(公告)号：WO2009107850A2
公开(公告)日：2009-09-03
申请号：PCT/JP2009/054007
申请日：2009-02-25
申请人： TAKEDA PHARMACEUTICAL COMPANY LIMITED , FUJII, Nobuhiro , OGURO, Yuya , SASAKI, Satoshi , KONDO, Shigeru
发明人： FUJII, Nobuhiro , OGURO, Yuya , SASAKI, Satoshi , KONDO, Shigeru
IPC分类号： C07D471/04 , C07D498/04 , C07D513/04 , A61P35/00
CPC分类号： C07D471/04 , C07D471/14 , C07D498/04 , C07D513/04
摘要： The present invention provides a compound having a superior Smo inhibitory activity and lower toxicity, which is sufficiently satisfactory as a pharmaceutical product.The present invention provides a compound represented by the formula (I) wherein ring A is 5- to 7-membered ring optionally having substituent(s), where substituents are optionally bonded to each other to form a ring; X is O, S or NR 1 (R 1 is a hydrogen atom or a hydrocarbon group optionally having substituent(s)); R 2 is carbamoyl optionally having substituent(s); and R 3 is hydroxy optionally having substituent(s), or a salt thereof.
摘要翻译：本发明提供具有优异的Smo抑制活性和较低毒性的化合物，其作为药物产品足够令人满意。本发明提供式（I）表示的化合物，其中环A为5-至7-元环，具有取代基，其中取代基任选地彼此结合形成环; X是O，S或NR1（R1是氢原子或任选具有取代基的烃基）; R2是任选具有取代基的氨基甲酰基; 和R 3是任选具有取代基的羟基，或其盐。

6. 发明申请

WO2017172565A1 CRYSTALLINE FORMS OF 2-[(2S)-1-AZABICYCLO[2.2.2]OCT-2-YL]-6-(3-METHYL-1H- PYRAZOL-4-YL)THIENO[3,2-D]PYRIMIDIN-4(3H)-ONE HEMIHYDRATE 审中-公开
标题翻译： 2 - [（2S）-1-氮杂环十二烷[2.2.2] OCT-2-yL] -6-（3-甲基-1H-吡唑-4-基）噻吩并[3,2-d]嘧啶-2 4（3H） - 酮酸血红蛋白
公开(公告)号：WO2017172565A1
公开(公告)日：2017-10-05
申请号：PCT/US2017/024226
申请日：2017-03-27
申请人： TAKEDA PHARMACEUTICAL COMPANY LIMITED
发明人： IWATA, Kentaro , MIZUNO, Masahiro , MAEDA, Kazuhiro , YASUMA, Tsuneo , HOMMA, Misaki , OGURO, Yuya , TAYA, Naohiro , ZHU, Lei , BAILEY, John, Daniel , LANGSTON, Marianne , PATIL, Siddhesh, Dinanath , GOUR, Shruti , ROY, Lilly
IPC分类号： C07D495/04
摘要： The present disclosure relates to crystalline forms of 2-[(2S)-1-azabicyclo[2.2.2]oct-2-yl]-6-(3-methyl-1H-pyrazol-4-yl)thieno[3,2-d]pyrimidin-4(3H)-one hemihydrate (Compound 1) and/or tautomers thereof, wherein Compound 1 has the structure: (I) ⋅ 0.5 H 2 O; processes for preparing crystalline forms of Compound 1 and/or tautomers thereof; pharmaceutical compositions comprising the crystalline forms; methods of inhibiting a cell division cycle 7 in a mammal comprising administering the crystalline forms; and methods of treating a cell division cycle 7 mediated cancer in a mammal comprising administering the crystalline forms or a pharmaceutical composition comprising the crystalline forms.
摘要翻译：本发明涉及2 - [（2S）-1-氮杂双环[2.2.2]辛-2-基] -6-（3-甲基-1H-吡唑-4 - 基）噻吩并[3,2-d]嘧啶-4（3H） - 酮半水合物（化合物1）和/或其互变异构体，其中化合物1具有以下结构：（I）·0.5H 2 / > O; 制备化合物1和/或其互变异构体的结晶形式的方法; 包含晶型的药物组合物; 在哺乳动物中抑制细胞分裂周期7的方法，其包括施用所述晶体形式; 以及在哺乳动物中治疗细胞分裂周期介导的癌症的方法，包括给予所述晶型或包含所述晶型的药物组合物。

7. 发明申请

WO2021094832A8 HETEROCYCLIC NMDA ANTAGONISTS 审中-公开
公开(公告)号：WO2021094832A8
公开(公告)日：2021-05-20
申请号：PCT/IB2020/000962
申请日：2020-11-12
申请人： TAKEDA PHARMACEUTICAL COMPANY LIMITED
发明人： IKEDA, Shuhei , KAMATA, Makoto , OGURO, Yuya , AIDA, Jumpei , TAWARAISHI, Taisuke , WAKABAYASHI, Takeshi , OYABU, Norio , OCHIDA, Atsuko , IWANAGA, Kouichi , YAMAMOTO, Satoshi , MURAKAMI, Masataka , NAKAMURA, Minoru , YAMAGUCHI, Fumie , YUKAWA, Takafumi
IPC分类号： C07D207/263 , C07D401/06 , C07D403/06 , C07D413/06 , A61P25/28 , A61P25/06 , A61K31/4015
摘要： A compound of formula (I), or a salt thereof that may have an antagonistic action against an NMDA receptor that includes an NR2B subunit and may be useful as a prophylactic or therapeutic agent for depression, bipolar disorder, migraine, pain, a symptom peripheral to dementia, or the like.

8. 发明申请

WO2019189945A1 HETEROCYCLIC COMPOUND AND USE THEREOF 审中-公开
公开(公告)号：WO2019189945A1
公开(公告)日：2019-10-03
申请号：PCT/JP2019/014901
申请日：2019-03-27
申请人： TAKEDA PHARMACEUTICAL COMPANY LIMITED
发明人： OGURO, Yuya , MATSUMOTO, Shigemitsu , WAKABAYASHI, Takeshi , TOKUNAGA, Norihito , KAMEI, Taku , ITO, Mitsuhiro , MIKAMI, Satoshi , SETO, Masaki , MORIMOTO, Shinji , NAKAMURA, Shinji , TAKASHIMA, Sachie , MURAKAMI, Masataka , DAINI, Masaki , KAMATA, Makoto , NAKAMURA, Minoru , WADA, Yasufumi , KAKEI, Hiroyuki , TAKAMI, Kazuaki , TAWARAISHI, Taisuke , AIDA, Jumpei , HIWANAGA, Kouichi , YAMAMOTO, Satoshi
IPC分类号： C07D471/04 , C07D487/04 , A61P25/00 , A61K31/437 , A61K31/4162
摘要： The present invention provides a heterocyclic compound having an antagonistic action on an NMDA receptor containing the NR2B subunit, and expected to be useful as an agent for the prophylaxis or treatment of major depression, bipolar disorder, migraine, pain, behavioral and psychological symptoms of dementia and the like. The present invention relates to a compound represented by the formula (I): wherein each symbol is as described in the description, or a salt thereof.

9. 发明申请

WO2021234451A1 3-((1H-PYRAZOL-4-YL)METHYL)-6'-(PHENYL)-2H-(1,2'-BIPYRIDIN)-2-ONE DERIVATIVES AND RELATED COMPOUNDS AS GPR139 ANTAGONISTS FOR USE IN A METHOD OF TREATMENT OF E.G. DEPRESSION 审中-公开
公开(公告)号：WO2021234451A1
公开(公告)日：2021-11-25
申请号：PCT/IB2021/000337
申请日：2021-05-20
申请人： TAKEDA PHARMACEUTICAL COMPANY LIMITED
发明人： HASUI, Tomoaki , MIKAMI, Satoshi , YAMASHITA, Toru , NAKAMURA, Shinji , MORIMOTO, Shinji , IMAEDA, Toshihiro , TAKAMI, Kazuaki , DAINI, Masaki , KAKEI, Hiroyuki , NAKAMURA, Minoru , YAMAGUCHI, Fumie , WANG, Chunxiang , TAKASHIMA, Sachie , KAMATA, Makoto , OGURO, Yuya , IKEDA, Shuhei
IPC分类号： C07D401/14 , C07D413/14 , C07D405/14 , A61K31/444 , A61K31/4155 , A61K31/5377 , A61K31/506 , A61K31/351 , A61K31/4545 , A61K31/4439 , A61P25/00 , A61P25/04 , A61P25/18 , A61P25/20 , A61P25/24 , A61P25/28 , A61P25/30 , A61P25/36
摘要： The present invention refers to compounds of formula (I). The present invention also relates to compounds of formula (I) for use as G Protein coupled Receptor 139 (GPR139) antagonists in methods of medical treatment of e.g. depression, Alzheimer's disease, schizophrenia, drug addiction, sleep disorders, pain, and attention deficit hyperactivity disorder. Exemplary compounds are e.g. 3-((1H-pyrazol-4-yl)methyl)-6'-( phenyl) -2H-(1,2'-bipyridin)-2-one derivatives and related compounds. The present description discloses the synthesis and characterisation of exemplary compounds, pharmacological data thereof, as well as exemplary tablet formulations comprising the compounds of the invention (e.g. page 83 to page 110; examples 1 to 33; reference example 1; test examples 1 and 2; tables 1 to 4).

10. 发明申请

WO2021059017A1 HETEROCYCLIC COMPOUND AND USE THEREOF 审中-公开
公开(公告)号：WO2021059017A1
公开(公告)日：2021-04-01
申请号：PCT/IB2020/000772
申请日：2020-09-25
申请人： TAKEDA PHARMACEUTICAL COMPANY LIMITED
发明人： OGURO, Yuya , KAMATA, Makoto , IKEDA, Shuhei , WAKABAYSAHI, Takeshi , TOKUNAGA, Norihito , KAMEI, Taku , ITO, Mitsuhiro , MATSUMOTO, Shigemitsu , KAMITANI, Hirotaka , HIRAYAMA, Takaharu , TANAKA, Toshio , BANNO, Hiroshi , TAKAKURA, Nobuyuki , YONEMORI, Jinichi , FUJIMOTO, Takuya
IPC分类号： A61P43/00 , C07D213/61 , C07D213/65 , C07D213/68 , C07D221/04 , C07D239/34 , C07D333/38 , C07D401/12 , A61K31/495 , A61K31/444 , A61P25/00 , A61P29/00
摘要： Provided is a heterocyclic compound that can have an antagonistic action on an NMD A receptor containing the NR2B subunit and that is expected to be useful as a prophylactic or therapeutic agent for depression, bipolar disorder, migraine, pain, peripheral symptoms of dementia and the like. A compound represented by the formula (I), wherein each symbol is as defined in the DESCRIPTION, or a salt thereof.

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