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1. 发明授权

US10710967B2 Pyrimidine derivative 有权
公开(公告)号：US10710967B2
公开(公告)日：2020-07-14
申请号：US15770002
申请日：2016-10-28
申请人： ASKA PHARMACEUTICAL CO., LTD.
发明人： Makoto Okada , Youichi Nakano , Takashi Nose , Takahiro Nishimoto , Satoshi Maeda
IPC分类号： C07D239/36 , C07D401/04 , C07D401/10 , C07D401/12 , C07D401/14 , C07D403/04 , C07D405/14 , C07D409/04 , C07D417/04 , A61K31/506
摘要： A compound represented by the formula (1), or a salt thereof (X represents carbonyl group, or sulfonyl group; R1 represents hydrogen atom, a halogen atom, an alkyl group, an alkanoyl group, cyano group, or carboxyl group; R2 represents an alkyl group, a cyclic carbon group, or a heterocyclic group; R3 represents hydrogen atom, or 1 to 3 substituents; R4 and R5 represents hydrogen atom, a halogen atom, or an alkyl group; and R6 represents an alkyl group, or an alkoxy group), which has an mPGES-1 inhibitory action, and is useful as an active ingredient of a medicament for prophylactic and/or therapeutic treatment of inflammation, pain, rheumatism, and the like.

2. 发明授权

US09643994B2 Crystalline polymorphic form of ulipristal acetate 有权
公开(公告)号：US09643994B2
公开(公告)日：2017-05-09
申请号：US14431357
申请日：2013-09-26
申请人： ASKA PHARMACEUTICAL CO., LTD.
发明人： Shigeki Iwashita , Hiroyuki Hayashi , Koichi Miyazaki
IPC分类号： A61K31/57 , C07J7/00 , C07J41/00
CPC分类号： C07J41/0083 , C07B2200/13
摘要： A novel crystalline polymorphic form of ulipristal acetate useful as an agent for preventing and/or treating uterine leiomyoma and as a contraceptive, and a process for producing the crystalline polymorphic form are provided. The novel crystalline polymorphic form of ulipristal acetate is obtained by crystallization or transition in association with a specified solvent. The solvent comprises at least one member selected from the group consisting of water, an aliphatic hydrocarbon, an aromatic hydrocarbon, a halogenated hydrocarbon, a linear alcohol, an alkyl ether, an acetate ester, an alkyl ketone, an N-alkylacylamide, and an alkanenitrile.

3. 发明授权

US09365553B2 Heterocyclic compound and H1 receptor antagonist 有权
标题翻译：杂环化合物和H1受体拮抗剂
公开(公告)号：US09365553B2
公开(公告)日：2016-06-14
申请号：US13699892
申请日：2011-05-23
申请人： Makoto Okada , Koichi Hasumi , Takahiro Nishimoto , Miwa Yoshida , Kouki Ishitani , Tomoji Aotsuka , Hashime Kanazawa
发明人： Makoto Okada , Koichi Hasumi , Takahiro Nishimoto , Miwa Yoshida , Kouki Ishitani , Tomoji Aotsuka , Hashime Kanazawa
IPC分类号： C07D401/06 , C07D211/46 , C07D405/06 , C07D213/79 , C07D333/40 , C07D407/08 , C07D409/06 , C07D413/06 , C07D417/06
CPC分类号： C07D405/06 , C07D211/46 , C07D213/79 , C07D333/40 , C07D401/06 , C07D407/08 , C07D409/06 , C07D413/06 , C07D417/06
摘要： A heterocyclic compound useful as an antiallergic agent is provided.A compound represented by the following formula (1) or a salt thereof: wherein the ring A is a homocyclic or heterocyclic ring; the ring B is a heterocyclic ring which contains G and nitrogen atom N as constituent atoms thereof, wherein G is CH or N; R1 is a carbonyl group or an alkylene group; R2a and R2b are an alkyl group, a cycloalkyl group, an aryl group, or a heterocyclic group; X is an oxygen atom or a sulfur atom; Z is a hydroxyl group, an alkoxy group, a cycloalkyloxy group, an aryloxy group, an aralkyloxy group, an amino group, or an N-substituted amino group; and n is 0 or 1; with the proviso that when the ring A is a benzene ring or when the ring B is a piperazine ring, R1 is an alkylene group which may have a substituent.
摘要翻译：提供了可用作抗过敏剂的杂环化合物。由下式（1）表示的化合物或其盐：其中环A是稠环或杂环; 环B是含有G和氮原子N作为其构成原子的杂环，其中G是CH或N; R1是羰基或亚烷基; R2a和R2b是烷基，环烷基，芳基或杂环基; X是氧原子或硫原子; Z是羟基，烷氧基，环烷氧基，芳氧基，芳烷氧基，氨基或N-取代氨基; 并且n为0或1; 条件是当环A为苯环时，或当环B为哌嗪环时，R 1为可具有取代基的亚烷基。

4. 发明授权

US09200008B2 Heterocyclic compound and p27Kip1 degradation inhibitor 有权
标题翻译：杂环化合物和p27Kip1降解抑制剂
公开(公告)号：US09200008B2
公开(公告)日：2015-12-01
申请号：US13701896
申请日：2011-07-01
申请人： Hiroshi Uchida , Akira Asagarasu , Teruaki Matsui
发明人： Hiroshi Uchida , Akira Asagarasu , Teruaki Matsui
IPC分类号： C07D471/04 , C07D498/04 , C07D207/34 , C07D231/40 , C07D277/20 , C07D277/42 , C07D307/68 , C07D403/12 , C07D405/14 , C07D409/12 , C07D417/12 , C07D417/14 , C07D487/04 , C07D491/052 , C07F5/02
CPC分类号： C07D498/04 , C07D207/34 , C07D231/40 , C07D277/20 , C07D277/42 , C07D307/68 , C07D403/12 , C07D405/14 , C07D409/12 , C07D417/12 , C07D417/14 , C07D471/04 , C07D487/04 , C07D491/052 , C07F5/025
摘要： A novel heterocyclic compound or a salt thereof useful for selectively inhibiting the degradation of p27Kip1 is provided. The compound or the salt thereof is represented by the following formula (1): wherein A represents an alkyl group, a cycloalkyl group, an aryl group or a heterocyclic group, the group A may have a substituent; the ring B represents a 5- to 8-membered monocyclic heterocyclic ring or a condensed ring containing the monocyclic heterocyclic ring, the ring B may have a substituent; the ring C represents an aromatic ring, the ring C may have a substituent; L represents a linker comprising a main chain having 3 to 5 atoms selected from the group consisting of a carbon atom, a nitrogen atom, an oxygen atom and a sulfur atom, wherein at least one atom in the main chain is a hetero atom selected from the group consisting of a nitrogen atom, an oxygen atom and a sulfur atom, the linker L may have a substituent; and n is 0 or 1.
摘要翻译：提供了可用于选择性抑制p27Kip1降解的新型杂环化合物或其盐。化合物或其盐由下式（1）表示：其中A表示烷基，环烷基，芳基或杂环基，基团A可以具有取代基; 环B表示5至8元单环杂环或含有单环杂环的稠环，环B可以具有取代基; 环C表示芳香环，环C可以具有取代基; L表示包含选自碳原子，氮原子，氧原子和硫原子的3至5个原子的主链的连接体，其中主链中的至少一个原子是选自以下的杂原子由氮原子，氧原子和硫原子组成的基团，连接体L可以具有取代基; n为0或1。

5. 发明授权

US09115344B2 Mesenchymal stem cell and a method of use thereof 有权
标题翻译：间充质干细胞及其使用方法
公开(公告)号：US09115344B2
公开(公告)日：2015-08-25
申请号：US13481180
申请日：2012-05-25
申请人： Osamu Honmou , Kazuo Hashi , Teiji Uede
发明人： Osamu Honmou , Kazuo Hashi , Teiji Uede
IPC分类号： A61K35/12 , C12N5/00 , C12N5/0775 , C12N5/079 , A61K35/28
CPC分类号： C12N5/0676 , A61K9/0019 , A61K35/12 , A61K35/28 , A61K35/51 , A61K2035/124 , C12N5/0622 , C12N5/0662 , C12N5/0663 , C12N5/0664 , C12N5/0665 , C12N5/0666 , C12N5/0667 , C12N5/0668 , C12N2506/1353
摘要： Demyelinated axons were remyelinated in the demyelinated rat model by collecting bone marrow cells from mouse bone marrow and transplanting the mononuclear cell fraction separated from these bone marrow cells.
摘要翻译：脱髓鞘大鼠模型中脱髓鞘的轴突通过从小鼠骨髓中收集骨髓细胞并移植从这些骨髓细胞分离出的单核细胞级分而被髓鞘化。

6. 发明授权

US08377944B2 Thienopyrimidine derivatives 有权
标题翻译：噻吩并嘧啶衍生物
公开(公告)号：US08377944B2
公开(公告)日：2013-02-19
申请号：US13585060
申请日：2012-08-14
申请人： Kotaro Gotanda , Atsushi Shinbo , Youichi Nakano , Hideo Kobayashi , Makoto Okada , Akira Asagarasu
发明人： Kotaro Gotanda , Atsushi Shinbo , Youichi Nakano , Hideo Kobayashi , Makoto Okada , Akira Asagarasu
IPC分类号： C07D495/04 , A61K31/519 , A61P25/28
CPC分类号： C07D495/04
摘要： This invention provides thienopyrimidine derivatives of the formula, wherein R1 stands for hydrogen atom, an alkyl group or the like; R2 stands for a hydrogen atom, an alkyl or amino group or the like, R3 stands for an alkyl, alkenyl or alkylthio group or the like or a group Y—X—; or R2 and R3 may together form tetramethylene group; X standing for a direct bond or linking group such as CH2, CH(OH), S, O, NH; Y standing for a substituted or unsubstituted aromatic carbocyclic, aromatic heterocylic, cycloalkyl or saturated heterocyclic group or the like; Z stands for S or O, and n is 0 or an integer of 1 to 4, or salts thereof, which exhibit an inhibitory effect on PDE9, and are therefore useful for prevention or treatment of overactive bladder syndrome, pollakiuria, urinary incontinence, dysuria associated with prostatic hyperplasia, urolithiasis, Alzheimer's disease, chronic obstructive pulmonary disease, myocardial infarction, thrombosis, diabetes and the like.
摘要翻译：本发明提供下式的噻吩并嘧啶衍生物，其中R1代表氢原子，烷基等; R2表示氢原子，烷基或氨基等，R3表示烷基，烯基或烷硫基等或Y-X-基团; 或者R 2和R 3可以一起形成四亚甲基; X代表直接键或连接基团如CH 2，CH（OH），S，O，NH; Y代表取代或未取代的芳族碳环，芳香杂环，环烷基或饱和杂环基等; Z代表S或O，n为0或1〜4的整数，或其盐，对PDE9具有抑制作用，因此可用于预防或治疗膀胱过度活动症，尿频尿失禁，排尿困难与前列腺增生，尿石症，阿尔茨海默病，慢性阻塞性肺疾病，心肌梗死，血栓形成，糖尿病等相关。

7. 发明授权

US08309138B2 Pharmaceutical composition comprising microparticle oily suspension 有权
标题翻译：包含微粒油性悬浮液的药物组合物
公开(公告)号：US08309138B2
公开(公告)日：2012-11-13
申请号：US12526825
申请日：2008-02-15
申请人： Yasunori Sato
发明人： Yasunori Sato
IPC分类号： A61K9/14 , A61K31/506
CPC分类号： A61K31/506 , A61K9/0053 , A61K9/145
摘要： A pharmaceutical composition comprising a suspension of medicinally-active ingredient microparticles having a mean particle diameter of 20 μm or smaller in a base oil which can achieve extremely high intestinal absorption and bioavailability especially when the medicinally-active ingredient is hardly water-soluble.
摘要翻译：一种药物组合物，其特征在于，当所述药物活性成分几乎不溶于水时，其特征在于，在基础油中含有平均粒径为20μm以下的药物活性成分微粒的悬浮液，其可以实现极高的肠吸收和生物利用度。

8. 发明申请

US20120021059A1 SOLID PREPARATION 审中-公开
标题翻译：固体制剂
公开(公告)号：US20120021059A1
公开(公告)日：2012-01-26
申请号：US13257400
申请日：2010-03-24
申请人： Youichi Takano , Yusaku Sugiura
发明人： Youichi Takano , Yusaku Sugiura
IPC分类号： A61K9/14
CPC分类号： A61K9/2886 , A61K9/7007
摘要： A solid preparation 1 comprises a drug-containing unit 2 containing a cationic drug, and a gel-forming layer 4, containing an anionic polymer, for covering the drug-containing unit 2 and forming a gel with absorbing water, and optionally an intermediate layer 3 interposed between the drug-containing unit 2 and the gel-forming layer 4. The solid preparation 1 improves the elution property of the drug by incorporating an electrolyte (e.g., calcium chloride) into the intermediate layer 2 and/or the intermediate layer 3. The gel-forming layer 4 may comprise a carboxyvinyl polymer and a polyvalent metal compound. The gel-forming layer 4 may be covered with a surface layer (anti-adhesive layer) 5.
摘要翻译：固体制剂1包含含有阳离子药物的药物含有单元2和含有阴离子聚合物的凝胶形成层4，用于覆盖含药单元2并用吸水形成凝胶，以及任选的中间层 3。固体制剂1通过将电解质（例如氯化钙）并入中间层2和/或中间层3中来改善药物的洗脱性能凝胶形成层4可以包含羧基乙烯基聚合物和多价金属化合物。凝胶形成层4可以用表面层（抗粘合剂层）5覆盖。

9. 发明申请

US20110152517A1 AGENT FOR PREVENTING AND/OR TREATING FUNCTIONAL GASTROINTESTINAL DISORDER 有权
标题翻译：用于预防和/或治疗功能性胃肠疾病的药剂
公开(公告)号：US20110152517A1
公开(公告)日：2011-06-23
申请号：US13061239
申请日：2009-09-24
申请人： Satoru Tamaoki , Jun Sato , Katsuichi Sudo
发明人： Satoru Tamaoki , Jun Sato , Katsuichi Sudo
IPC分类号： C07D491/22
CPC分类号： A61K31/439 , A61K9/1652 , A61K9/2018 , A61K9/2054
摘要： A preventive and/or therapeutic agent which improves an abnormal bowel function such as an abdominal pain, a diarrhea, or a constipation and is effective for preventing or treating a functional gastrointestinal disorder is provided.A preventive and/or therapeutic agent for a functional gastrointestinal disorder contains refaximin as an effective ingredient. The functional gastrointestinal disorder includes a functional esophageal disorder, a functional gastroduodenal disorder (e.g., a functional dyspepsia), a functional bowel disorder (e.g., a functional bloating, a functional diarrhea), a functional abdominal pain syndrome, a functional gallbladder and Sphincter of Oddi disorder, a functional anorectal disorder (e.g., a functional fecal incontinence, a functional anorectal pain, a functional defecation disorder), a functional disorder in neonates and toddlers (e.g., an infant functional diarrhea), a functional disorder in children and adolescents (e.g., a childhood functional abdominal pain, a childhood nonretentive fecal incontinence), and other diseases.
摘要翻译：提供了改善肠功能异常的预防和/或治疗剂，例如腹痛，腹泻或便秘，并且对于预防或治疗功能性胃肠道疾病是有效的。用于功能性胃肠道疾病的预防和/或治疗剂含有抗纤维蛋白作为有效成分。功能性胃肠道疾病包括功能性食管障碍，功能性胃十二指肠疾病（例如功能性消化不良），功能性肠病（例如功能性腹胀，功能性腹泻），功能性腹痛综合征，功能性胆囊和括约肌 Oddi障碍，功能性肛门直肠疾病（例如，功能性大便失禁，功能性肛门直肠疼痛，功能性排便障碍），新生儿和幼儿中的功能障碍（例如，婴儿功能性腹泻），儿童和青少年功能障碍（例如儿童功能性腹痛，童年无力大便失禁）和其他疾病。

10. 发明申请

US20080248004A1 Cell fractions containing cells capable of differentiating into neural cells 审中-公开
$Cell fractions containing cells capable of differentiating into neural cells$
标题翻译：含有能够分化成神经细胞的细胞的细胞级分
公开(公告)号：US20080248004A1
公开(公告)日：2008-10-09
申请号：US12076092
申请日：2008-03-13
申请人： Osamu Honmou , Kazuo Hashi , Teiji Uede
发明人： Osamu Honmou , Kazuo Hashi , Teiji Uede
IPC分类号： A61K35/12 , C12N5/06 , A61P35/00
CPC分类号： C12N5/0676 , A61K9/0019 , A61K35/12 , A61K35/28 , A61K35/51 , A61K2035/124 , C12N5/0622 , C12N5/0662 , C12N5/0663 , C12N5/0664 , C12N5/0665 , C12N5/0666 , C12N5/0667 , C12N5/0668 , C12N2506/1353
摘要： Demyelinated axons were remyelinated in the demyelinated rat model by collecting bone marrow cells from mouse bone marrow and transplanting the mononuclear cell fraction separated from these bone marrow cells.
摘要翻译：脱髓鞘大鼠模型中脱髓鞘的轴突通过从小鼠骨髓中收集骨髓细胞并移植从这些骨髓细胞分离的单核细胞级分而被髓鞘化。

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