公开(公告)号：US09181249B2

公开(公告)日：2015-11-10

申请号：US14577480

申请日：2014-12-19

Applicant: Takeda Pharmaceutical Company Limited

Inventor： Jason Brown ,  Steve Hitchcock ,  Maria Hopkins ,  Shota Kikuchi ,  Holger Monenschein ,  Holly Reichard ,  Kristin Schleicher ,  Huikai Sun ,  Todd Macklin

IPC: A61K31/4965 ,  C07D471/04

CPC classification number: C07D471/04

Abstract: The present invention provides compounds of formula I: which are useful as modulators of GPR6, pharmaceutical compositions thereof, methods for treatment of conditions associated with GPR6, processes for making the compounds and intermediates thereof.

Abstract translation: 本发明提供式I化合物：其可用作GPR6的调节剂，其药物组合物，用于治疗与GPR6相关的病症的方法，以及用于制备化合物及其中间体的方法。

公开(公告)号：US09181186B2

公开(公告)日：2015-11-10

申请号：US14377951

申请日：2013-02-12

Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITED

Inventor： Seiji Miwatashi ,  Hideo Suzuki ,  Tomohiro Okawa ,  Yasufumi Miyamoto ,  Takeshi Yamasaki ,  Yuko Hitomi ,  Yasuhiro Hirata

IPC: C07D213/64 ,  C07D405/14 ,  C07D401/12 ,  C07D239/34 ,  C07D213/30 ,  C07D213/68 ,  C07D213/69 ,  C07D213/55 ,  C07D403/12

CPC classification number: C07D213/64 ,  C07D213/30 ,  C07D213/55 ,  C07D213/68 ,  C07D213/69 ,  C07D239/34 ,  C07D401/12 ,  C07D403/12 ,  C07D405/14

Abstract: Provided is an aromatic ring compound having a GPR40 agonist activity. A compound represented by the formula (I): wherein each symbol is as described in the DESCRIPTION, or a salt thereof has a GPR40 agonist activity, and is useful as an agent for the prophylaxis or treatment of diabetes and the like.

Abstract translation: 提供具有GPR40激动剂活性的芳环化合物。 由式（I）表示的化合物：其中每个符号如说明书所述，或其盐具有GPR40激动剂活性，并且可用作预防或治疗糖尿病等的药剂。

公开(公告)号：US09169238B2

公开(公告)日：2015-10-27

申请号：US12737612

申请日：2009-07-29

Applicant: Yutaka Tanoue ,  Junya Nomura

Inventor： Yutaka Tanoue ,  Junya Nomura

IPC: A61K31/4245 ,  A61K31/5415 ,  A61K9/20 ,  A61P9/12 ,  A61P9/00 ,  A61P7/10 ,  C07D413/14

CPC classification number: C07D413/14

Abstract: The present invention relates to a solid preparation containing a compound represented by the formula (I) wherein each symbol is as defined in the specification, or a salt thereof, a pH control agent and a diuretic, which is superior in the stability and dissolution property of the compound represented by the formula (I) and the diuretic.

Abstract translation: 本发明涉及一种固体制剂，其含有式（I）表示的化合物，其中每个符号如说明书中所定义，或其盐，pH控制剂和利尿剂，其稳定性和溶解性优异 的式（I）表示的化合物和利尿剂。

公开(公告)号：US20150274723A1

公开(公告)日：2015-10-01

申请号：US14706876

申请日：2015-05-07

Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITED

Inventor： Mark E. Adams ,  Rongliang Chen ,  Betty Lam ,  Matthew Lardy ,  Srinivasa Reddy Natala ,  Steven James Wilkens ,  Mitsunori Kono ,  Zhe Nie

IPC: C07D471/04 ,  A61K31/519 ,  A61K31/5365 ,  A61K31/4985 ,  A61K31/437 ,  C07D519/00

CPC classification number: C07D471/04 ,  A61K31/4365 ,  A61K31/437 ,  A61K31/4985 ,  A61K31/519 ,  A61K31/5365 ,  A61K31/5383 ,  C07D487/04 ,  C07D495/04 ,  C07D498/04 ,  C07D519/00

Abstract: Disclosed are compounds of Formula 1, and pharmaceutically acceptable salts thereof, wherein G, p, R1, R2, R3a, R4, and R5 are defined in the specification. This disclosure also relates to materials and methods for preparing compounds of Formula 1, to pharmaceutical compositions which contain them, and to their use for treating disorders, diseases, and conditions involving the immune system and inflammation, including rheumatoid arthritis, cancer, and other disorders, diseases, and conditions for which inhibition of SYK is indicated.

Abstract translation: 公开了式1的化合物及其药学上可接受的盐，其中G，p，R1，R2，R3a，R4和R5在说明书中定义。 本公开还涉及用于制备式1化合物的材料和方法，含有它们的药物组合物及其用于治疗涉及免疫系统和炎症的疾病，疾病和病症的用途，包括类风湿性关节炎，癌症和其它疾病 ，疾病和表示SYK抑制的病症。

公开(公告)号：US20150250728A1

公开(公告)日：2015-09-10

申请号：US14430956

申请日：2013-09-25

Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITED

Inventor： Naoyuki Murata ,  Shigeo Yanai

IPC: A61K9/16 ,  A61K31/24

CPC classification number: A61K9/1688 ,  A61K9/14 ,  A61K31/18 ,  A61K31/24

Abstract: A method of producing crystal of a poorly water-soluble pharmaceutical compound, including mixing a solution of a poorly water-soluble pharmaceutical compound in a good solvent and nanobubble water or an aqueous nanobubble solution to precipitate crystal of the poorly water-soluble pharmaceutical compound. The crystal of a poorly water-soluble pharmaceutical compound obtained by the method is microparticulate and has more uniform particle size distribution, and is superior in the absorbability and sustainability.

Abstract translation: 一种生产水溶性差的药物化合物的方法，包括将难溶于水的药物化合物的溶液与纳米气泡水溶液或纳米气泡水溶液混合，使难溶于水的药物化合物的晶体析出。 通过该方法得到的水溶性差的药物的结晶为微粒状，粒径分布更均匀，吸收性和可持续性优异。

公开(公告)号：US09115139B2

公开(公告)日：2015-08-25

申请号：US13377918

申请日：2010-06-14

Applicant: Shigekazu Sasaki ,  Tomokazu Kusumoto

Inventor： Shigekazu Sasaki ,  Tomokazu Kusumoto

IPC: A61K31/553 ,  C07D498/04 ,  A61K9/20 ,  A61K9/28

CPC classification number: C07D498/04 ,  A61K9/2018 ,  A61K9/2059 ,  A61K9/286 ,  Y02A50/402

Abstract: Provided is a compound having a serotonin 5-HT2c receptor activating action, useful for lower urinary tract conditions, obesity and cancer. A compound represented by the formula (I0): wherein each symbol is as defined in the specification, or a salt thereof.

Abstract translation: 本发明提供具有5-羟色胺5-HT 2C受体激活作用的化合物，其用于下尿路状况，肥胖症和癌症。 由式（I0）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：US09115136B2

公开(公告)日：2015-08-25

申请号：US14059868

申请日：2013-10-22

Applicant: Takeda Pharmaceutical Company Limited

Inventor： Tsuyoshi Maekawa ,  Hideyuki Igawa

IPC: A01N43/90 ,  A61K31/519 ,  C07D487/00 ,  C07D487/04

CPC classification number: C07D487/04 ,  A61K31/519

Abstract: Provided is a novel compound represented by the following formula wherein each symbol is as defined in the specification, or a salt thereof, which has an angiotensin II receptor antagonistic activity and a peroxisome proliferator-activated receptor γ agonistic activity, and is useful as an agent for the prophylaxis or treatment of circulatory diseases such as hypertension and the like and/or metabolic diseases such as diabetes and the like, and the like.

Abstract translation: 本发明提供一种下式表示的新化合物，其中各符号如说明书中所定义，或其盐，其具有血管紧张素II受体拮抗作用和过氧化物酶体增殖物激活受体γ激动活性，可用作试剂 用于预防或治疗诸如高血压等循环系统疾病和/或代谢疾病如糖尿病等。

公开(公告)号：US09108970B2

公开(公告)日：2015-08-18

申请号：US13886032

申请日：2013-05-02

Applicant: Takeda Pharmaceutical Company Limited

Inventor： Yasuyoshi Arikawa ,  Benjamin Jones ,  Betty Lam ,  Christopher Smith ,  Masashi Takahashi ,  Qing Dong ,  Victoria Feher ,  Zhe Nie

IPC: C07D471/04 ,  A61K31/437 ,  A61P11/06 ,  A61P35/00 ,  A61P17/06 ,  A61P29/00 ,  A61P11/08 ,  A61P37/02 ,  A61K31/527 ,  A61K45/06 ,  C07D487/10 ,  C07D519/00 ,  C07D487/04 ,  A61K31/519

CPC classification number: C07D487/04 ,  A61K31/437 ,  A61K31/519 ,  A61K31/527 ,  A61K45/06 ,  C07D471/04 ,  C07D487/10 ,  C07D519/00

Abstract: Disclosed are compounds of Formula 1, and pharmaceutically acceptable salts thereof, wherein G, L1, L2, R1, R2, R3, and R4 are defined in the specification. This disclosure also relates to materials and methods for preparing compounds of Formula 1, pharmaceutical compositions containing them, and their use for treating disorders, diseases, and conditions involving the immune system and inflammation, including rheumatoid arthritis, hematological malignancies, epithelial cancers (i.e., carcinomas), and other disorders, diseases, and conditions for which inhibition of SYK is indicated.

Abstract translation: 公开了式1的化合物及其药学上可接受的盐，其中G，L1，L2，R1，R2，R3和R4在说明书中定义。 本公开还涉及用于制备式1化合物的材料和方法，含有它们的药物组合物及其用于治疗涉及免疫系统和炎症的疾病，疾病和病症的用途，包括类风湿性关节炎，血液恶性肿瘤，上皮癌（即， 癌症）以及其它疾病，疾病和表示SYK抑制的病症。

公开(公告)号：US09056873B2

公开(公告)日：2015-06-16

申请号：US14128576

申请日：2012-06-20

Applicant: Mitsunori Kono ,  Zhe Nie

Inventor： Mitsunori Kono ,  Zhe Nie

IPC: A61K31/437 ,  C07D471/04 ,  C07D498/04 ,  C07D519/00 ,  A61K31/4365 ,  A61K31/4985 ,  A61K31/519 ,  A61K31/5383 ,  C07D487/04 ,  C07D495/04

CPC classification number: C07D471/04 ,  A61K31/4365 ,  A61K31/437 ,  A61K31/4985 ,  A61K31/519 ,  A61K31/5365 ,  A61K31/5383 ,  C07D487/04 ,  C07D495/04 ,  C07D498/04 ,  C07D519/00

Abstract: Disclosed are compounds of Formula 1, and pharmaceutically acceptable salts thereof, wherein G, p, R1, R2, R3a, R4, and R5 are defined in the specification. This disclosure also relates to materials and methods for preparing compounds of Formula 1, to pharmaceutical compositions which contain them, and to their use for treating disorders, diseases, and conditions involving the immune system and inflammation, including rheumatoid arthritis, cancer, and other disorders, diseases, and conditions for which inhibition of SYK is indicated.

Abstract translation: 公开了式1的化合物及其药学上可接受的盐，其中G，p，R1，R2，R3a，R4和R5在说明书中定义。 本公开还涉及用于制备式1化合物的材料和方法，含有它们的药物组合物及其用于治疗涉及免疫系统和炎症的疾病，疾病和病症的用途，包括类风湿性关节炎，癌症和其它疾病 ，疾病和表示SYK抑制的病症。

公开(公告)号：US20150132379A1

公开(公告)日：2015-05-14

申请号：US14405310

申请日：2013-05-28

Applicant: Takeda Pharmaceutical Company Limited

Inventor： Tetsuya Kawano

IPC: A61K9/20

CPC classification number: A61K9/2072 ,  A61K9/2013 ,  A61K9/2027 ,  A61K9/2054 ,  A61K9/2059 ,  A61K9/2077 ,  A61K9/2086 ,  A61K9/2095 ,  A61K9/2846 ,  A61K9/2866 ,  A61K31/4439 ,  A61K31/616

Abstract: A dry-coated tablet 1 comprises an inner core 2 which contains an active component and an outer layer 3 which contains powdery solid components and coats the inner core 2. Openings 8c and 9c are formed in circular surfaces 2a and 2b respectively of the inner core 2, wherein each of the openings is larger than the average particle size of a component the average particle size of which is the smallest of the powdery solid components contained in the outer layer 3, and the inner surface 3a of the outer layer 3 penetrates in the openings 8c and 9c.

Abstract translation: 干涂片1包括含有活性组分的内芯2和含有粉末固体组分并涂覆内芯2的外层3.开口8c和9c分别形成在内芯的圆形表面2a和2b中 如图2所示，其中每个开口大于其平均粒径是外层3中包含的粉末状固体成分中最小的成分的平均粒径，并且外层3的内表面3a渗入 开口8c和9c。