公开(公告)号：US09238639B2

公开(公告)日：2016-01-19

申请号：US14380215

申请日：2013-02-22

Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITED

Inventor： Nobuyuki Takakura ,  Yoshihiro Banno ,  Yoshito Terao ,  Atsuko Ochida ,  Sachie Morimoto ,  Tsuneo Yasuma ,  Minoru Ikoma ,  Kei Masuda

IPC: C07D333/60 ,  C07D417/12 ,  C07D495/04 ,  C07D333/54 ,  C07D405/04 ,  C07D405/12 ,  C07D409/06 ,  C07D409/12 ,  C07D307/79 ,  C07D307/80 ,  C07D307/81 ,  C07D307/84 ,  C07D333/64 ,  C07D333/70

CPC classification number: C07D333/60 ,  C07D307/79 ,  C07D307/80 ,  C07D307/81 ,  C07D307/84 ,  C07D333/54 ,  C07D333/64 ,  C07D333/70 ,  C07D405/04 ,  C07D405/12 ,  C07D409/06 ,  C07D409/12 ,  C07D417/12 ,  C07D495/04

Abstract: The present invention provides a compound having a GOAT inhibitory action, which is useful for the prophylaxis or treatment of obesity and the like, and has superior efficacy. The present invention is a compound represented by the formula (I): wherein each symbol is as defined in the specification, or a salt thereof.

Abstract translation: 本发明提供具有GOAT抑制作用的化合物，其可用于预防或治疗肥胖症等，并且具有优异的疗效。 本发明是由式（I）表示的化合物：其中各符号如说明书中所定义，或其盐。

公开(公告)号：US20140155416A1

公开(公告)日：2014-06-05

申请号：US14089747

申请日：2013-11-25

Applicant: Takeda Pharmaceutical Company Limited

Inventor： Tsuneo Yasuma ,  Akira Mori ,  Masahiro Kawase ,  Hiroyuki Kimura ,  Masato Yoshida ,  Albert Charles Gyorkos ,  Scott Alan Pratt ,  Christopher Peter Corrette

IPC: C07D487/04

CPC classification number: C07D487/04

Abstract: 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.

Abstract translation: 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。

公开(公告)号：US20210101897A1

公开(公告)日：2021-04-08

申请号：US17044366

申请日：2019-04-01

Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITED

Inventor： Lei Zhu ,  John Daniel Bailey ,  Landon Durak ,  Joshua David Waetzig ,  Masahiro Mizuno ,  Kazuhiro Maeda ,  Tsuneo Yasuma ,  Hiroshi Yamaguchi ,  Koichiro Fukuoka ,  Kazuyuki Akiyama

IPC: C07D453/02 ,  C07D409/04

Abstract: The present invention provides processes and synthetic intermediates for the synthesis 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 or a salt, hydrate, or tautomer thereof, or any combination thereof, which are Cdc7 kinase inhibitors, and are useful for the treatment of disorders of cell proliferation, particularly cancer, and other disorders associated with Cdc7 activity.

公开(公告)号：US11746109B2

公开(公告)日：2023-09-05

申请号：US16088096

申请日：2017-03-27

Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITED

Inventor： Kentaro Iwata ,  Masahiro Mizuno ,  Kazuhiro Maeda ,  Tsuneo Yasuma ,  Misaki Homma ,  Yuya Oguro ,  Naohiro Taya ,  Lei Zhu ,  John Daniel Bailey ,  Marianne Langston ,  Siddhesh Dinanath Patil ,  Shruti Gour ,  Lilly Roy

IPC: C07D471/08 ,  A61K9/48

CPC classification number: C07D471/08 ,  A61K9/485 ,  A61K9/4858 ,  C07B2200/13

Abstract: 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)·0.5H2O; 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.

公开(公告)号：US10730904B2

公开(公告)日：2020-08-04

申请号：US16240677

申请日：2019-01-04

Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITED

Inventor： Mitsuru Nonogawa ,  Toshiaki Nagata ,  Hideki Saito ,  Tsuneo Yasuma

IPC: C07H19/207 ,  C07H19/06 ,  C07H19/16 ,  C07H19/067 ,  C07H19/073 ,  C07H21/04 ,  C07H21/00 ,  C07H1/00 ,  C07H19/167

Abstract: In this method, an oligonucleotide represented by formula (II) [wherein Y1, Q, Base, r and r′ are each as defined in claim 1] is prepared by using, as a synthesis unit, a novel nucleoside monomer compound represented by formula (I) [wherein X, R1, Y, Base, Z, Ar, R2, R3 and n are each as defined in claim 1]. The novel nucleoside monomer compound is a nucleoside, the base moiety of which is substituted with an aromatic-hydrocarbon-ring-carbonyl or -thiocarbonyl group having at least one hydrophobic group. The method can dispense with column-chromatographic purification in every reaction, and enables base elongation not only in the 3′-direction but also in the 5′-direction, thus attaining efficient liquid-phase mass synthesis of an oligonucleotide.

公开(公告)号：US10214555B2

公开(公告)日：2019-02-26

申请号：US14442601

申请日：2013-11-13

Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITED

Inventor： Mitsuru Nonogawa ,  Toshiaki Nagata ,  Hideki Saito ,  Tsuneo Yasuma

IPC: C07H1/00 ,  C07H21/00 ,  C07H21/04 ,  C07H19/06 ,  C07H19/16 ,  C07H19/067 ,  C07H19/073 ,  C07H19/167 ,  C07H19/207

Abstract: In this method, an oligonucleotide is prepared by using, as a synthesis unit, a novel nucleoside monomer compound represented by formula (I) [wherein X, R1, Y, Base, Z, Ar, R2, R3 and n are each as defined in Claim 1]. The novel nucleoside monomer compound is a nucleoside, the base moiety of which is substituted with an aromatic-hydrocarbon-ring-carbonyl or -thiocarbonyl group having at least one hydrophobic group. The method cars dispense with column-chromatographic purification in every reaction, and enables base elongation not only in the 3′-direction but also in the 5′-direction, thus attaining efficient liquid-phase mass synthesis of an oligonucleotide.

公开(公告)号：US09447100B2

公开(公告)日：2016-09-20

申请号：US14089747

申请日：2013-11-25

Applicant: Takeda Pharmaceutical Company Limited

Inventor： Tsuneo Yasuma ,  Akira Mori ,  Masahiro Kawase ,  Hiroyuki Kimura ,  Masato Yoshida ,  Albert Charles Gyorkos ,  Scott Alan Pratt ,  Christopher Peter Corrette

IPC: C07D487/04 ,  A61K31/519 ,  A61P19/08 ,  A61P19/10

CPC classification number: C07D487/04

Abstract: 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.

Abstract translation: 也如前所述，在式（II）和（III）中指定X1，R3，R1，Y和X3。

公开(公告)号：US20140243310A1

公开(公告)日：2014-08-28

申请号：US14353622

申请日：2012-10-23

Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITED

Inventor： Tohru Yamashita ,  Takuya Fujimoto ,  Ryo Mizojiri ,  Kazuko Yonemori ,  Hideki Hirose ,  Zenichi Ikeda ,  Ikuo Fujimori ,  Kyoko Toyofuku ,  Tsuneo Yasuma ,  Nobuyuki Matsunaga

IPC: C07D231/56 ,  C07D498/04 ,  C07D307/80 ,  C07D413/04 ,  C07D263/57 ,  C07D235/18

CPC classification number: C07D231/56 ,  A61K31/343 ,  A61K31/416 ,  A61K31/4184 ,  A61K31/422 ,  A61K31/423 ,  A61K31/437 ,  A61K31/4439 ,  C07D235/18 ,  C07D263/57 ,  C07D307/80 ,  C07D413/04 ,  C07D498/04 ,  C07D513/04

Abstract: The present invention provides a compound represented by the formula (I): wherein each symbol is as defined in the specification, or a salt thereof.

Abstract translation: 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。

公开(公告)号：US08598226B2

公开(公告)日：2013-12-03

申请号：US13910374

申请日：2013-06-05

Applicant: Takeda Pharmaceutical Company Limited

Inventor： Tsuneo Yasuma ,  Nobuyuki Negoro

IPC: A61K31/343

CPC classification number: C07D409/12 ,  C07D307/80

Abstract: The present invention provides a compound represented by the formula (I): wherein each symbol is as defined in the description, or a salt thereof. The compound or a salt thereof or a prodrug thereof has a GPR40 receptor function modulating action and is useful as an insulin secretagogue or an agent for the prophylaxis or treatment of diabetes and the like.

Abstract translation: 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。 化合物或其盐或其前药具有GPR40受体功能调节作用，并且可用作胰岛素促分泌素或用于预防或治疗糖尿病等的药剂。

公开(公告)号：US11524957B2

公开(公告)日：2022-12-13

申请号：US17044366

申请日：2019-04-01

Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITED

Inventor： Lei Zhu ,  John Daniel Bailey ,  Landon Durak ,  Joshua David Waetzig ,  Masahiro Mizuno ,  Kazuhiro Maeda ,  Tsuneo Yasuma ,  Hiroshi Yamaguchi ,  Koichiro Fukuoka ,  Kazuyuki Akiyama

IPC: C07D453/02 ,  C07D409/04

Abstract: The present invention provides processes and synthetic intermediates for the synthesis 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 or a salt, hydrate, or tautomer thereof, or any combination thereof, which are Cdc7 kinase inhibitors, and are useful for the treatment of disorders of cell proliferation, particularly cancer, and other disorders associated with Cdc7 activity.