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61. 发明申请

US20160082010A1 SALT OF FUSED HETEROCYCLIC DERIVATIVE AND CRYSTAL THEREOF 有权
标题翻译：熔融杂环衍生物和晶体的盐
公开(公告)号：US20160082010A1
公开(公告)日：2016-03-24
申请号：US14867501
申请日：2015-09-28
申请人： KISSEI PHARMACEUTICAL CO., LTD.
发明人： Kazumichi JO , Hideki TAKEUCHI
IPC分类号： A61K31/519 , A61K31/14 , A61K9/00
CPC分类号： A61K31/519 , A61K9/0053 , A61K31/14 , C07B2200/13 , C07D495/04
摘要： An objective of the present invention is to improve the solubility of 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.The present invention provides 3-[2-fluoro-5-(2,3-difluoro-6-methoxybenzyl-oxy)-4-methoxyphenyl]-2,4-dioxo-1,2,3,4-tetrahydrothieno[3,4-d]pyrimidine-5-carboxylic acid choline salt has excellent solubility and storage stability.
摘要翻译：本发明的目的是提高3- [2-氟-5-（2,3-二氟-6-甲氧基苄氧基）-4-甲氧基苯基] -2,4-二氧代-1,2,3,4-四氢 - 4-四氢噻吩并[3,4-d]嘧啶-5-甲酸。本发明提供3- [2-氟-5-（2,3-二氟-6-甲氧基苄氧基）-4-甲氧基苯基] -2,4-二氧代-1,2,3,4-四氢噻吩并[ 4-d]嘧啶-5-羧酸胆碱盐具有优异的溶解性和储存稳定性。

62. 发明授权

US09169266B2 Salt of fused heterocyclic derivative and crystal thereof 有权
标题翻译：稠合杂环衍生物的盐及其结晶
公开(公告)号：US09169266B2
公开(公告)日：2015-10-27
申请号：US13577832
申请日：2011-02-09
申请人： Kazumichi Jo , Hideki Takeuchi
发明人： Kazumichi Jo , Hideki Takeuchi
IPC分类号： C07D495/04 , A61K31/519 , A61P15/08 , A61P15/16 , A61P35/00 , A61P15/18 , A61P5/24
CPC分类号： A61K31/519 , A61K9/0053 , A61K31/14 , C07B2200/13 , C07D495/04
摘要： An objective of the present invention is to improve the solubility of 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.The present invention provides 3-[2-fluoro-5-(2,3-difluoro-6-methoxybenzyl-oxy)-4-methoxyphenyl]-2,4-dioxo-1,2,3,4-tetrahydrothieno[3,4-d]pyrimidine-5-carboxylic acid choline salt has excellent solubility and storage stability.
摘要翻译：本发明的目的是提高3- [2-氟-5-（2,3-二氟-6-甲氧基苄氧基）-4-甲氧基苯基] -2,4-二氧代-1,2,3,4-四氢 - 4-四氢噻吩并[3,4-d]嘧啶-5-甲酸。本发明提供3- [2-氟-5-（2,3-二氟-6-甲氧基苄氧基）-4-甲氧基苯基] -2,4-二氧代-1,2,3,4-四氢噻吩并[ 4-d]嘧啶-5-羧酸胆碱盐具有优异的溶解性和储存稳定性。

63. 发明授权

US08796247B2 Indole derivative, and pharmacologically acceptable salt thereof 有权
标题翻译：吲哚衍生物及其药理学上可接受的盐
公开(公告)号：US08796247B2
公开(公告)日：2014-08-05
申请号：US13980599
申请日：2012-01-24
申请人： Kazuya Tatani , Atsushi Kondo , Tatsuhiro Kondo , Naohiro Kawamura , Shigeki Seto , Yasushi Kohno
发明人： Kazuya Tatani , Atsushi Kondo , Tatsuhiro Kondo , Naohiro Kawamura , Shigeki Seto , Yasushi Kohno
IPC分类号： C07D209/08 , A61K31/40 , A61K31/4025 , A61K31/443 , A61K31/4439 , A61K31/444 , A61K45/06 , C07D401/06 , C07D401/14 , C07D405/06 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14 , A61K31/404
CPC分类号： C07D209/08 , A61K31/40 , A61K31/4025 , A61K31/404 , A61K31/443 , A61K31/4439 , A61K31/444 , A61K45/06 , C07D401/06 , C07D401/14 , C07D405/06 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14 , A61K2300/00
摘要： The present invention provides a compound represented by the general formula (I) of the present invention, which has EP1 receptor antagonism: wherein A represents a pyridine ring, a furan ring, or the like; Y1 represents a C1-6 alkylene group; Y2 represents a single bond or the like; R1 represents —C(═O)—NH—SO2R6, an acidic 5-membered hetero ring group, or the like; R2 represents an optionally substituted phenyl group, an optionally substituted 5-membered aromatic heterocyclic group, or the like; R3 represents a halogen atom, a C1-6 alkoxy group, or the like; R4 represents a hydrogen atom, a halogen atom, or the like; R5 represents a hydrogen atom or the like; and R6 represents a C1-6 alkyl group or the like], and a pharmaceutically acceptable salt thereof. Furthermore, the compound (I) of the present invention can be used as an agent for treating or preventing LUTS, in particular, various symptoms of OABs.
摘要翻译：本发明提供了具有EP1受体拮抗作用的本发明通式（I）表示的化合物：其中A表示吡啶环，呋喃环等; Y1表示C1-6亚烷基; Y2表示单键等; R 1表示-C（= O）-NH-SO 2 R 6，酸性5元杂环基等; R 2表示任选取代的苯基，任选取代的5元芳族杂环基等; R3表示卤素原子，C1-6烷氧基等; R 4表示氢原子，卤素原子等; R5表示氢原子等; 和R6表示C1-6烷基等〕及其药学上可接受的盐。此外，本发明的化合物（I）可以用作治疗或预防LUTS，特别是OAB的各种症状的药剂。

64. 发明授权

US08680120B2 Indole derivative or pharmaceutically acceptable salt thereof 失效
标题翻译：吲哚衍生物或其药学上可接受的盐
公开(公告)号：US08680120B2
公开(公告)日：2014-03-25
申请号：US13387266
申请日：2010-07-26
申请人： Kazuya Tatani , Naohiro Kawamura , Tatsuhiro Kondo , Atsushi Kondo
发明人： Kazuya Tatani , Naohiro Kawamura , Tatsuhiro Kondo , Atsushi Kondo
IPC分类号： A61K31/444 , A61K31/4439 , C07D401/14 , C07D401/06 , C07D401/04 , C07D209/08 , C07D209/10 , C07D405/06 , C07D405/14 , C07D405/04
CPC分类号： C07D209/08 , C07D209/10 , C07D209/12 , C07D401/04 , C07D401/06 , C07D401/14 , C07D405/04 , C07D405/06 , C07D405/14 , C07D409/04 , C07D409/06 , C07D409/14 , C07D413/06 , C07D413/14 , C07D417/06 , C07D417/14
摘要： A compound (I) of the present invention, which has an EP1 receptor antagonism: [wherein A represents a benzene ring or the like; Y1 represents a C1-6 alkylene group; Y2 represents a single bond or the like; R1 represents a hydrogen atom, a C1-6 alkyl group or the like; R2 represents a phenyl group which may have a substituent, a 5-membered aromatic heterocyclic ring which may have a substituent, a 6-membered aromatic heterocyclic ring which may have a substituent or the like; R3 represents a halogen atom, a C1-6 alkoxy group or the like; R4 represents a hydrogen atom or the like; and R5 represents a hydrogen atom or the like] or a pharmaceutically acceptable salt thereof is provided. Furthermore, the compound (I) of the present invention can be used as an agent for treating or preventing LUTS, in particular, various symptoms of OABs.
摘要翻译：具有EP1受体拮抗作用的本发明化合物（I）：其中A表示苯环等; Y1表示C1-6亚烷基; Y2表示单键等; R1表示氢原子，C1-6烷基等; R2表示可以具有取代基的苯基，可以具有取代基的5元芳香族杂环，可以具有取代基的6元芳族杂环等; R3表示卤素原子，C1-6烷氧基等; R4表示氢原子等; 并且R5表示氢原子等]或其药学上可接受的盐。此外，本发明的化合物（I）可以用作治疗或预防LUTS，特别是OAB的各种症状的药剂。

65. 发明授权

US08354382B2 Hemifumarate of a pyrazole derivative 有权
标题翻译：吡唑衍生物的半富马酸盐
公开(公告)号：US08354382B2
公开(公告)日：2013-01-15
申请号：US12988273
申请日：2009-04-13
申请人： Hideki Takeuchi , Eiji Tsuru
发明人： Hideki Takeuchi , Eiji Tsuru
IPC分类号： A01N43/04 , A61K31/70 , C07G3/00 , C07H15/00 , C07H17/00 , C07H17/02 , C07H23/00
CPC分类号： C07H17/02
摘要： The present invention provides a novel form of 3-(3-{4-[3-(β-D-glucopyranosyloxy)-5-isopropyl-1H-pyrazol-4-ylmethyl]-3-methylphenoxy}propylamino)-2,2-dimethylpropionamide with improved storage stability. Since 3-(3-{4-[3-(β-D-glucopyranosyloxy)-5-isopropyl-1H-pyrazol-4-ylmethyl]-3-methylphenoxy}-propylamino)-2,2-dimethylpropionamide hemifumarate dihydrate has extremely excellent storage stability, it is useful as a drug substance. Furthermore, it shows an extremely good crystalline property and can be purified by a convenient method, and therefore is suitable for the industrial preparation.
摘要翻译：本发明提供3-（3- {4- [3-（＆bgr。-D-吡喃葡萄糖氧基）-5-异丙基-1H-吡唑-4-基甲基] -3-甲基苯氧基}丙基氨基）具有改善的储存稳定性的2-二甲基丙酰胺。由于3-（3- {4- [3-（＆bgr。-D-吡喃葡萄糖氧基）-5-异丙基-1H-吡唑-4-基甲基] -3-甲基苯氧基} - 丙基氨基）-2,2-二甲基丙酰胺半富马酸盐二水合物具有极好的储存稳定性，作为药物有用。此外，其显示出非常好的结晶性，并且可以通过方便的方法进行纯化，因此适用于工业制备。

66. 发明申请

US20120064154A1 SOLID DRUG FOR ORAL USE 审中-公开
标题翻译：用于口服使用的固体药物
公开(公告)号：US20120064154A1
公开(公告)日：2012-03-15
申请号：US13288348
申请日：2011-11-03
申请人： Tsuyoshi NAGANUMA , Mitsuo MURAMATSU
发明人： Tsuyoshi NAGANUMA , Mitsuo MURAMATSU
IPC分类号： A61K31/4045 , A61P13/00 , A61K9/48
CPC分类号： A61K9/1623 , A61K9/1652 , A61K9/2018 , A61K9/2054 , A61K9/4866 , A61K31/4045
摘要： The present invention provides a solid oral dosage form pharmaceutical for the treatment of dysuria, which comprises, as an active ingredient, an indoline compound having an α1-adrenoceptor blocking activity and represented by the formula: prodrug, pharmaceutically acceptable salt or pharmaceutically acceptable solvate thereof, wherein said pharmaceutical is prepared to have 85% dissolution time of not more than 60 minutes in a dissolution test according to method 2 (paddle method) of Japanese pharmacopoeia in a condition using water.
摘要翻译：本发明提供了用于治疗排尿困难的固体口服剂型药物，其包含作为活性成分的具有α1-肾上腺素能受体阻断活性的二氢吲哚化合物，由下式表示：前药，药学上可接受的盐或其药学上可接受的溶剂合物其中，所述药物在使用水的条件下，根据日本药典的方法2（桨法）在溶出试验中的85％溶解时间为60分钟以下。

67. 发明申请

US20110207935A1 FUSED-RING DERIVATIVE AND MEDICAL APPLICATION OF SAME 有权
标题翻译：熔融衍生物和医学应用
公开(公告)号：US20110207935A1
公开(公告)日：2011-08-25
申请号：US13124345
申请日：2009-10-14
申请人： Kazuo Shimizu , Masato Iizuka , Hideki Fujikura , Yasushi Takigawa , Masahiro Hiratochi
发明人： Kazuo Shimizu , Masato Iizuka , Hideki Fujikura , Yasushi Takigawa , Masahiro Hiratochi
IPC分类号： C07D215/52 , C07D277/56 , C07D263/34 , C07D275/03 , C07D285/08 , C07D271/06 , C07C255/57 , C07D231/14 , C07D213/79
CPC分类号： C07C255/57 , A61K31/192 , A61K31/415 , A61K31/426 , A61K31/44 , A61K31/47 , C07C255/54 , C07D213/79 , C07D215/50 , C07D231/14 , C07D277/20 , C07D277/56
摘要： The present invention provides compounds useful as agents for the prevention or treatment of a disease associated with abnormal plasma uric acid level and the like. The present invention relates to fused ring derivatives represented by the following formula (I) having xanthine oxidase inhibitory activities and useful as agents for the prevention or treatment of a disease associated with abnormality of plasma uric acid level, prodrugs thereof, salts thereof or the like. In the formula (I), X1 and X2 represent CH or N; ring U represents aryl or heteroaryl; m represents integral number from 0 to 2; n represents integral number from 0 to 3; R1 represents a hydroxy group, amino or C1-6 alkyl; R2 represents C1-6 alkyl, C1-6 alkoxy C1-6 alkyl or the like.
摘要翻译：本发明提供了可用作预防或治疗与异常血浆尿酸水平等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下式（I）表示的稠环衍生物，可用作预防或治疗与血浆尿酸水平异常有关的疾病，其前药，其盐或类似物。在式（I）中，X 1和X 2表示CH或N; 环U表示芳基或杂芳基; m表示0〜2的整数; n表示0〜3的整数; R1表示羟基，氨基或C1-6烷基; R 2表示C 1-6烷基，C 1-6烷氧基C 1-6烷基等。

68. 发明申请

US20110092509A1 Pharmaceutical Composition for Prevention or Treatment of Disease Associated with Tear Reduction 审中-公开
标题翻译：用于预防或治疗与撕裂相关的疾病的药物组合物
公开(公告)号：US20110092509A1
公开(公告)日：2011-04-21
申请号：US12526298
申请日：2009-08-07
申请人： Mamoru Kobayashi , Tetsuya Asari , Mariko Tadachi
发明人： Mamoru Kobayashi , Tetsuya Asari , Mariko Tadachi
IPC分类号： A61K31/5377 , A61K31/165 , A61K31/4453 , A61P27/02
CPC分类号： A61K31/165 , A61K31/4453 , A61K31/5375
摘要： The present invention provides pharmaceutical compositions for the prevention or treatment of diseases associated with decrease in tear.The present invention provides pharmaceutical compositions for the prevention or treatment of diseases associated with decrease in tear such as dry eye, dry disorders of cornea and conjunctiva, disorders of the keratoconjunctival epithelium, syndrome with decrease in tear secretion, xerophthalmia, dry eye due to aging, ophthalmopathy in Stevens-Johnson syndrome, ophthalmopathy in Sjögren's syndrome, keratoconjunctival ulcer, dryness in wearing of contact lens or the like, which comprises as an active ingredient a phenylethanolaminotetralin-carboxamide derivative represented by the general formula (I) wherein A represents a lower alkylene group, B represents an amino group, a di(lower alkyl)amino group or a 3 to 7-membered alicyclic amino group which may have an oxygen atom in the ring, a carbon atom with the mark “*” represents a carbon atom of S-configuration or R-configuration, or a mixture thereof and a carbon atom with (S) represents a carbon atom of S-configuration, or a pharmaceutically acceptable salt thereof.
摘要翻译：本发明提供了用于预防或治疗与泪液减少相关的疾病的药物组合物。本发明提供了用于预防或治疗与泪液减少相关的疾病的药物组合物，例如干眼症，角膜和结膜的干性失调，角膜结膜上皮的病症，泪液分泌减少的综合征，干眼症，老化造成的干眼症，史蒂文森 - 约翰逊综合征中的眼病，西格伦综合征的眼病，角膜结膜溃疡，隐形眼镜等的磨损，其包含作为活性成分的由通式（I）表示的苯基乙酰氨基四氢化萘 - 甲酰胺衍生物，其中A表示低级亚烷基，B表示氨基，二（低级烷基）氨基或在环中可具有氧原子的3〜7元脂环族氨基，具有标记“*”的碳原子表示碳原子的S-构型或R构型，或其混合物和碳原子与（S）表示S-构型的碳原子，或者是Phar 其药学上可接受的盐。

69. 发明授权

US07888382B2 Combined pharmaceutical preparation for treatment of type 2 diabetes 失效
标题翻译：联合用于治疗2型糖尿病的药物制剂
公开(公告)号：US07888382B2
公开(公告)日：2011-02-15
申请号：US11918654
申请日：2006-04-18
申请人： Yuji Kiyono , Yoshio Okubo , Katsumi Hontani , Imao Mikoshiba , Kazuma Ojima
发明人： Yuji Kiyono , Yoshio Okubo , Katsumi Hontani , Imao Mikoshiba , Kazuma Ojima
IPC分类号： A01N43/38 , A01N33/02
CPC分类号： C07D209/44 , A61K31/133 , A61K31/33 , A61K31/4035 , A61K45/06 , A61K2300/00
摘要： For controlling the condition of type 2 diabetes, a pharmaceutical including a combination of mitiglinide, a pharmacologically acceptable salt thereof or a hydrate thereof and an α-glucosidase inhibitor such as voglibose or acarbose, and a therapeutic method using the pharmaceutical are provided. The pharmaceutical according to the present invention has an extremely strong effect of decreasing a morning fasting blood glucose level, a postprandial blood glucose level and HbA1C of a patient with type 2 diabetes, and can improve glucose spike, insulin resistance and lipid metabolism.
摘要翻译：为了控制2型糖尿病的病症，提供了包括米格列奈，其药理学上可接受的盐或其水合物和α-葡糖苷酶抑制剂如伏格列波糖或阿卡波糖的组合药物和使用该药物的治疗方法。根据本发明的药物具有降低早晨空腹血糖水平，餐后血糖水平和2型糖尿病患者的HbA1C的极强作用，并且可以改善葡萄糖刺激，胰岛素抵抗和脂质代谢。

70. 发明授权

US07847107B2 Asymmetric reduction method 失效
标题翻译：不对称还原法
公开(公告)号：US07847107B2
公开(公告)日：2010-12-07
申请号：US12087092
申请日：2006-12-26
申请人： Yoshinori Matsumoto , Yuki Takeuchi , Hiroyuki Yamamoto
发明人： Yoshinori Matsumoto , Yuki Takeuchi , Hiroyuki Yamamoto
IPC分类号： C07D209/44
CPC分类号： C07B53/00 , C07D209/44
摘要： The present invention is to provide a novel method for producing (2S)-2-benzyl-3-(cis-hexahydro-2-isoindolinylcarbonyl)propionic acid which is useful as a therapeutic agent for diabetes. The present invention relates to a method for producing (2S)-2-benzyl-3-(cis-hexahydro-2-isoindolinylcarbonyl)propionic acid, which is characterized in that 2-benzylidene-3-(cis-hexahydro-2-isoindolinylcarbonyl)propionic acid is subjected to a catalytic reduction reaction in the presence of an asymmetric catalyst prepared from a pyrrolidinebisphosphine compound (I) represented by the following general formula (I): wherein, R1 represents a linear or branched alkyl group having 1-10 carbon atoms, cycloalkyl group, aralkyl group or aryl group which may respectively have a substituent; and R2 and R3 independently represent an optionally substituted aryl group. The * mark in the pyrrolidine ring shows that the carbon atom at that position has the S configuration, and a rhodium compound.
摘要翻译：本发明提供可用作糖尿病治疗剂的（2S）-2-苄基-3-（顺式 - 六氢-2-异吲哚基羰基）丙酸的新方法。本发明涉及（2S）-2-苄基-3-（顺 - 六氢-2-异二氢吲哚基羰基）丙酸的制备方法，其特征在于2-亚苄基-3-（顺式 - 六氢-2-异吲哚基羰基））丙酸在由以下通式（I）表示的吡咯烷二膦化合物（I）制备的不对称催化剂存在下进行催化还原反应：其中，R1表示具有1-10个碳原子的直链或支链烷基原子，环烷基，芳烷基或可分别具有取代基的芳基; 并且R 2和R 3独立地表示任选取代的芳基。吡咯烷环中的*标记表示该位置的碳原子具有S构型和铑化合物。

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