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1. 发明授权

US11596644B2 Method for treating post-prandial hypoglycemia 有权
公开(公告)号：US11596644B2
公开(公告)日：2023-03-07
申请号：US17041577
申请日：2019-03-28
申请人： AVOLYNT , KISSEI PHARMACEUTICAL CO., LTD.
发明人： William Wilkison , Bentley Cheatham , James T. Green
IPC分类号： A61K31/706 , A61K31/7056 , A61P3/08 , A61K31/702
摘要： Disclosed herein are methods, sodium-dependent glucose transporter (SGLT)1 compounds and compositions for the treatment of postprandial hypoglycemia, postprandial hypoglycemia that occurs as a consequence of gastric surgery.

2. 发明申请

US20210046078A1 USAGE AND DOSAGE OF THERAPEUTIC AGENTS FOR ENDOMETRIOSIS 有权
公开(公告)号：US20210046078A1
公开(公告)日：2021-02-18
申请号：US16843260
申请日：2020-04-08
申请人： KISSEI PHARMACEUTICAL CO., LTD.
发明人： Takuro Dan , Hideomi Takahashi , Yu Kuramochi
IPC分类号： A61K31/519 , A61P15/00 , A61P29/00
摘要： An object of the present invention is to provide pharmaceutical agents that reduce risk for decrease in bone mineral density due to their effect of reducing estrogen levels and exert excellent therapeutic effects on endometriosis. The present invention relates to pharmaceutical compositions for treating endometriosis comprising 3-[2-fluoro-5-(2,3-difluoro-6-methoxybenzyloxy)-4-methoxyphenyl]-2,4-dioxo-1,2,3,4-tetrahydrothieno[3,4-d]pyrimidine-5-carboxylic acid or a pharmaceutically acceptable salt thereof, which are administered orally once a day at a daily dose of between 50 mg and 75 mg calculated as a free form.

3. 发明申请

US20190002414A1 NK1 RECEPTOR ANTAGONIST 审中-公开
公开(公告)号：US20190002414A1
公开(公告)日：2019-01-03
申请号：US15781925
申请日：2016-12-06
申请人： KISSEI PHARMACEUTICAL CO., LTD.
发明人： Takashi Miyagi , Masahiro Kobayashi , Toshihiro Nishimura
IPC分类号： C07D241/04 , C07D211/32 , C07D401/06 , A61P1/08
CPC分类号： C07D241/04 , A61K31/451 , A61K31/495 , A61P1/08 , C07D211/32 , C07D211/62 , C07D401/06
摘要： A problem of the present invention is to provide a new compound which has NK1 receptor antagonist activity, and thus is useful for the prevention or treatment of cancer-chemotherapy-induced nausea and vomiting.A compound represented by the formula (I): wherein W represents a fluorine atom and the like, ring A represents a cycloalkyl and the like, X1 represents CH or N, R represents methyl and the like, Y represents 0 to 2, U1, U2 and U3 each independently represents a single bond and the like, or a pharmaceutically acceptable salt thereof. The compounds of the present invention or pharmaceutically acceptable salts thereof have an excellent NK1 receptor antagonist activity, and thus are also useful as an agent for the prevention or treatment of cancer-chemotherapy-induced nausea and vomiting.

4. 发明申请

US20180312566A1 Fc FUSION HIGH AFFINITY IgE RECEPTOR ALPHA-CHAIN 审中-公开
公开(公告)号：US20180312566A1
公开(公告)日：2018-11-01
申请号：US16034648
申请日：2018-07-13
申请人： Kissei Pharmaceutical Co., Ltd.
发明人： Takashi Sakamoto , Yoichi Inada , Kazumasa Yokoyama
IPC分类号： C07K14/735 , C12N15/09 , A61K38/16 , C07K16/18 , C07K14/705 , C07K19/00
CPC分类号： C07K14/70535 , A61K38/16 , C07K14/705 , C07K16/18 , C07K19/00 , C07K2319/30 , C12N15/09
摘要： Provided is an Fc fusion high affinity IgE receptor α-chain having excellent stability at low pH. An Fc fusion protein comprising: (i) a high affinity IgE receptor α-chain; and (ii) an Fc region of IgG1, wherein a linker fragment region between the (i) and the (ii) is the amino acid sequence shown in SEQ ID NO: 2.

5. 发明申请

US20170320821A1 NOVEL ANILINE DERIVATIVE, PHARMACEUTICAL COMPOSITION CONTAINING SAME, AND USE THEREOF 有权
公开(公告)号：US20170320821A1
公开(公告)日：2017-11-09
申请号：US15659760
申请日：2017-07-26
申请人： KISSEI PHARMACEUTICAL CO., LTD.
发明人： Hitoshi Inoue , Kohsuke Ohno , Tetsuya Nakamura , Yusuke Ohsawa
IPC分类号： C07D205/04
CPC分类号： C07D205/04
摘要： [Problem] The present invention provides a novel compound having an S1P1 receptor antagonistic activity.[Solution] The present invention provides a compound represented by the general formula (I): (in the formula, Rl, R2 and R3 are each a hydrogen atom, a halogen atom, a C1-6 alkyl group, a halo C1-6 alkyl group or the like, R4 is a C1-6 alkyl group or the like, R5 is a C1-6 alkyl group or the like, R6 is a C1-6 alkyl group or the like, R7 is a hydrogen atom, a halogen atom, a C1-6 alkyl group or the like, R8 is a halogen atom, a C1-6 alkyl group, a halo C1-6 alkyl group, a C1-6 alkoxy group or the like, and R9 is a hydrogen atom or a C1-6 alkyl group.) or a pharmaceutically acceptable salt thereof, a pharmaceutical compositions containing same, and use thereof. The compounds of the present invention have an excellent S1P1 receptor antagonistic activity and therefore are useful as an agent for the treatment or prevention of antoimmune diseases and the like.

6. 发明申请

US20160129031A1 PYRAZOLE DERIVATIVE AND USE THEREOF FOR MEDICAL PURPOSES 有权
公开(公告)号：US20160129031A1
公开(公告)日：2016-05-12
申请号：US14995489
申请日：2016-01-14
申请人： Masayuki Isaji , Masaaki Takemura , Hidetoshi Isawa , Yukihiko Hotei , Itaru Miyashita
发明人： Masayuki Isaji , Masaaki Takemura , Hidetoshi Isawa , Yukihiko Hotei , Itaru Miyashita
IPC分类号： A61K31/7056
CPC分类号： A61K31/7056 , C07H17/02
摘要： The present invention provides pyrazole derivatives, uses thereof for medical purposes and so on. More particularly, the present invention relates to pharmaceuticals useful for the prevention or treatment of constipation, which comprise as an active ingredient 3-(3-{4-[3-(β-D-glucopyranosyloxy)-5-isopropyl-1H-pyrazol-4-ylmethyl]-3-methylphenoxy}propylamino)-2,2-dimethylpropionamide, or a pharmaceutically acceptable salt thereof. The pharmaceuticals of the present invention exert an effect of increasing the frequency of bowel movement or the like, and are useful for the prevention or treatment of constipation.

7. 发明授权

US09023882B2 5-membered nitrogen containing heterocyclic derivatives and pharmaceutical compositions comprising the same 有权
标题翻译： 5元含氮杂环衍生物和包含它们的药物组合物
公开(公告)号：US09023882B2
公开(公告)日：2015-05-05
申请号：US13494380
申请日：2012-06-12
申请人： Kazuo Shimizu , Yasushi Takigawa , Hideki Fujikura , Masato Iizuka , Masahiro Hiratochi , Norihiko Kikuchi
发明人： Kazuo Shimizu , Yasushi Takigawa , Hideki Fujikura , Masato Iizuka , Masahiro Hiratochi , Norihiko Kikuchi
IPC分类号： A61K31/4025 , C07D231/10 , C07D207/30 , A61K31/4155 , C07D403/04 , A61K31/402 , A61K31/165 , A61K31/404 , A61K31/415 , A61K31/427 , A61K31/4439 , A61K31/454 , A61K31/5377 , A61K45/06 , C07D207/34 , C07D231/14 , C07D231/16 , C07D231/20 , C07D231/38 , C07D231/40 , C07D401/04 , C07D405/04 , C07D405/06 , C07D409/04 , C07D409/12 , C07D417/04
CPC分类号： A61K31/402 , A61K31/165 , A61K31/404 , A61K31/415 , A61K31/4155 , A61K31/427 , A61K31/4439 , A61K31/454 , A61K31/5377 , A61K45/06 , C07D207/34 , C07D231/14 , C07D231/16 , C07D231/20 , C07D231/38 , C07D231/40 , C07D401/04 , C07D403/04 , C07D405/04 , C07D405/06 , C07D409/04 , C07D409/12 , C07D417/04 , A61K2300/00
摘要： 5-membered heterocyclic derivatives represented by general formula (I) having xanthine oxidase inhibitory activities and useful as agents for the prevention or treatment of a disease associated with abnormality of serum uric acid level, prodrugs thereof, or salts thereof. In the formula (I), T represents nitro, cyano and the like; ring J represents aryl or heteroaryl; Q represents carboxy, 5-tetazolyl and the like; Y represents H, OH, NH2, halogen, haloalkyl and the like; X1 and X2 independently represent CR2 or N; R2 represents H, alkyl and the like; R1 represents halogen, cyano, haloalkyl, A-D-E-G-L-M, —N(-D-L-M)2 and the like, A represents a single bond, O, S and the like; D, G and M independently represent optionally substituted alkylene, cycloalkylene, heterocycloalkylene, arylene, heteroarylene and the like; E and L independently represent a single bond, O, S, COO, SO2 and the like.
摘要翻译：具有黄嘌呤氧化酶抑制活性的通式（I）表示的5元杂环衍生物，可用作预防或治疗与血清尿酸水平异常有关的疾病或其前药或其盐的药剂。在式（I）中，T表示硝基，氰基等; 环J表示芳基或杂芳基; Q表示羧基，5-四唑基等; Y表示H，OH，NH 2，卤素，卤代烷基等; X1和X2独立地表示CR2或N; R2代表H，烷基等; R 1表示卤素，氰基，卤代烷基，A-D-E-G-L-M，-N（-D-L-M）2等，A表示单键O，S等; D，G和M独立地表示任选取代的亚烷基，亚环烷基，亚杂环亚烷基，亚芳基，杂亚芳基等; E和L独立地表示单键O，S，COO，SO 2等。

8. 发明申请

US20130252955A1 (AZA)INDOLE DERIVATIVE AND USE THEREOF FOR MEDICAL PURPOSES 有权
标题翻译：（AZA）INDOLE DERIVATIVE及其用于医疗用途
公开(公告)号：US20130252955A1
公开(公告)日：2013-09-26
申请号：US13895634
申请日：2013-05-16
申请人： Kissei Pharmaceutical Co., Ltd.
发明人： Kazuo Shimizu , Yasushi Takigawa , Hideki Fujikura , Masato Iizuka , Masahiro Hiratochi , Norihiko Kikuchi
IPC分类号： A61K31/404 , C07D405/10 , A61K45/06 , A61K31/4439 , A61K31/5377 , C07D209/42 , C07D401/04
CPC分类号： C07D209/30 , A61K31/165 , A61K31/404 , A61K31/407 , A61K31/427 , A61K31/437 , A61K31/4439 , A61K31/5377 , A61K45/06 , C07D209/42 , C07D401/04 , C07D405/04 , C07D405/10 , C07D409/12 , C07D417/04 , C07D471/04 , C07D491/056 , A61K2300/00
摘要： The present invention provides compounds useful as agents for the prevention or treatment of a disease associated with abnormal serum uric acid level which has a uricosuric activity or the like. The present invention relates to (aza)indole derivatives represented by the following general formula (I) having xanthine oxidase inhibitory activities and useful as agents for the prevention or treatment of a disease associated with abnormality of serum uric acid level, prodrugs thereof, or salts thereof. In the formula (I), T represents nitro or cyano and the like; ring J represents aryl or heteroaryl and the like; Q represents carboxy or 5-tetazolyl and the like; Y represents H, OH, NH2, halogen, nitro, alkyl, alkoxy and the like; X1, X2 and X3 independently represent CR2 or N; R1 and R2 independently represent halogen, cyano, haloalkyl, A-D-E-G, —N(-D-E-G)2 and the like, in the formula, A represents a single bond, O, S and the like; D and G independently represent optionally substituted alkylene, cycloalkylene, heterocycloalkylene, arylene, heteroarylene and the like; E represents a single bond, O, S, COO, SO2 and the like.
摘要翻译：本发明提供可用作预防或治疗与具有尿酸活性等的异常血清尿酸水平相关的疾病的药剂的化合物。本发明涉及具有黄嘌呤氧化酶抑制活性的由以下通式（I）表示的（aza）吲哚衍生物，可用作预防或治疗与血清尿酸水平异常有关的疾病，其前药或盐其中。在式（I）中，T表示硝基或氰基等; 环J表示芳基或杂芳基等; Q表示羧基或5-四唑基等; Y表示H，OH，NH 2，卤素，硝基，烷基，烷氧基等; X1，X2和X3独立地表示CR2或N; R 1和R 2独立地表示卤素，氰基，卤代烷基，A-D-E-G，-N（-D-E-G）2等，式中，A表示单键O，S等; D和G独立地表示任选取代的亚烷基，亚环烷基，亚杂环亚烷基，亚芳基，杂亚芳基等; E表示单键O，S，COO，SO 2等。

9. 发明申请

US20130217878A1 (AZA)INDOLIZINE DERIVATIVE AND PHARMACEUTICAL USE THEREOF 有权
标题翻译：（AZA）吲哚衍生物及其药物用途
公开(公告)号：US20130217878A1
公开(公告)日：2013-08-22
申请号：US13824147
申请日：2011-09-28
申请人： Masato Iizuka , Kazuo Shimizu
发明人： Masato Iizuka , Kazuo Shimizu
IPC分类号： C07D487/04 , C07D471/04
CPC分类号： C07D487/04 , C07D471/04
摘要： (Aza)indolizine derivatives represented by Formula (I) having xanthine oxidase inhibitory activities and useful as agents for the prevention or treatment of a disease associated with abnormality of serum uric acid level, prodrugs thereof, salts thereof or the like. In Formula (I), 0 to 2 of X1, X2, X3 and X4 are a nitrogen atom and the others are CR1; one of T1 and T2 represents cyano and the other represents a group represented by Formula (A), with the proviso that when T1 is cyano, at least one of X1 to X4 is a nitrogen atom; R1 independently represents a hydrogen atom, a halogen atom, a hydroxy group, C1-6 alkyl, C1-6 alkoxy or the like; ring U represents a benzene ring or the like; m represents integral number from 0 to 2; R2 independently represents a fluorine atom, a hydroxy group or the like.
摘要翻译：具有黄嘌呤氧化酶抑制活性的式（I）表示的（Aza）中氮茚衍生物，可用作预防或治疗与血清尿酸水平异常相关的疾病，其前药，其盐等的药剂。在式（I）中，X 1，X 2，X 3和X 4的0〜2为氮原子，其余为CR 1; T1和T2之一表示氰基，另一个表示由式（A）表示的基团，条件是当T1为氰基时，X 1至X 4中的至少一个为氮原子; R1独立地表示氢原子，卤素原子，羟基，C1-6烷基，C1-6烷氧基等; 环U表示苯环等; m表示0〜2的整数; R2独立地表示氟原子，羟基等。

10. 发明授权

US08217069B2 Nitrogenated fused ring derivative, pharmaceutical composition comprising the same, and use of the same for medical purposes 有权
标题翻译：氮化稠环衍生物，包含其的药物组合物，以及其用于医疗目的
公开(公告)号：US08217069B2
公开(公告)日：2012-07-10
申请号：US12596313
申请日：2008-04-16
申请人： Shigeru Yonekubo , Takashi Miyagi , Kohsuke Ohno , Mikie Kambara , Nobuhiko Fushimi
发明人： Shigeru Yonekubo , Takashi Miyagi , Kohsuke Ohno , Mikie Kambara , Nobuhiko Fushimi
IPC分类号： A61K31/415 , C07D233/00
CPC分类号： C07D471/04 , A61K31/437 , A61K31/52 , C07D473/00 , C07D473/04 , C07D473/30 , C07D473/36 , C07D473/40 , C07D487/04
摘要： [Purpose] The present invention provides compounds useful as agents for the prevention or treatment of a sex hormone-dependent disease or the like.[Solution] The present invention provides nitrogen-containing fused ring derivatives represented by the following general formula (I) which has a GnRH antagonistic activity, prodrugs, salts, pharmaceutical compositions containing the same, medicinal uses thereof and the like. In the formula (I), rings A and B are independently aryl or heteroaryl; RA and RB are independently halogen, cyano, alkyl, alkylsulfonyl, —OW1, —SW1, —COW2, —NW3W4, —SO2NW3W4, aryl, etc.; RC is H or alkyl; E is oxygen atom, etc.; U is single bond or alkylene; and X is Y, —CO—Y, —SO2—Y, —S-(alkylene)-Y, —O-(alkylene)-Y, —SO2-(alkylene)-Y, etc.; Y is Z or amino, etc.; and Z is cycloalkyl, heterocycloalkyl, aryl, heteroaryl, etc.
摘要翻译： [目的]本发明提供可用作预防或治疗性激素依赖性疾病等的药剂的化合物。 [溶液]本发明提供了具有GnRH拮抗活性的下述通式（I）表示的含氮稠环衍生物，前药，盐，含有它们的药物组合物，其药用用途等。在式（I）中，环A和B独立地为芳基或杂芳基; RA和RB独立地是卤素，氰基，烷基，烷基磺酰基，-OW1，-SW1，-COW2，-NW3W4，-SO2NW3W4，芳基等; RC是H或烷基; E是氧原子等; U是单键或亚烷基; 并且X是Y，-CO-Y，-SO 2 -Y，-S-（亚烷基）-Y，-O-（亚烷基）-Y，-SO 2 - （亚烷基）-Y等; Y是Z或氨基等; Z是环烷基，杂环烷基，芳基，杂芳基等。

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