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91. 发明授权

US10703755B2 Substituted purine derivative 有权
公开(公告)号：US10703755B2
公开(公告)日：2020-07-07
申请号：US16095822
申请日：2017-04-25
申请人： SUMITOMO DAINIPPON PHARMA CO., LTD.
发明人： Shingo Tojo , Yoshiaki Isobe , Eiji Ideue , Hiroaki Fujiwara , Daisuke Urabe
IPC分类号： A61K31/52 , A61K31/5377 , A61K45/06 , C07D473/16 , C07D473/18 , C07D473/40 , C07D519/00 , A61P37/06 , C07D473/34 , C07D473/28
摘要： The present invention relates to a substituted purine derivative of formula (1) wherein R1 is alkoxy or the like, R2 is alkyl or the like, Ring Q1 is aryl or the like, W1 is alkylene or the like, Ring Q2 is aromatic carbocyclyl or the like, n is 1-4, R3 is hydrogen atom or the like, X1 is single bond or the like, W2 is alkylene or the like, and R4 is hydrogen atom or the like, or a pharmaceutically acceptable salt thereof, which has a potent inhibitory effect against TLR7, and thereby is useful for treating autoimmune disease.

92. 发明申请

US20190276455A1 CRYSTALLINE FORM OF GNRH RECEPTOR ANTAGONIST AND PREPARATION METHOD THEREFOR 审中-公开
公开(公告)号：US20190276455A1
公开(公告)日：2019-09-12
申请号：US16348932
申请日：2017-11-13
申请人： Jiangsu Hengrui Medicine Co., Ltd. , Suncadia Pharmaceuticals Co., Ltd.
发明人： Quanliang ZHANG , Junlei JIA , Lin BIAN , Xiaohui GAO
IPC分类号： C07D473/28
摘要： Provided are a crystalline form of a GnRH receptor antagonist and a preparation method therefor. Specifically, provided are a crystalline form I of 1-(4-(7-(2,6-difluorobenzyl)-3-((dimethylamino)methyl)-5-(6-methoxypyridazin-3-yl)-4,6-dicarbonyl-4,5,6,7-tetrahydro-2H-pyrazolo[3,4-d]pyrimidin-2-yl)phenyl)-3-methoxy urea (a compound of formula I) and a preparation method, the use of same in a pharmaceutical composition and the use of the crystalline form I and the composition in the preparation of a drug for treating diseases associated with a GnRH receptor antagonist.

93. 发明授权

US10112946B2 Composition 有权
公开(公告)号：US10112946B2
公开(公告)日：2018-10-30
申请号：US14234070
申请日：2012-07-19
申请人： Claire Louise Ambery , Christopher David Edwards
发明人： Claire Louise Ambery , Christopher David Edwards
IPC分类号： C07D473/28 , A61K9/00 , A61K9/12 , A61K31/522
摘要： Compound (I), and pharmaceutically acceptable salts thereof, are inducers of human interferon. Certain discrete and particular dosages of Compound (I) may be particularly useful in the treatment of various disorders, for example the treatment of allergic diseases and other inflammatory conditions, for example allergic rhinitis and allergic asthma.

94. 发明申请

US20180134700A1 TYK2 INHIBITORS AND USES THEREOF 审中-公开
公开(公告)号：US20180134700A1
公开(公告)日：2018-05-17
申请号：US15789588
申请日：2017-10-20
申请人： Nimbus Lakshmi, Inc.
发明人： Jeremy Robert Greenwood , Silvana Marcel Leit de Moradei , Craig E. Masse , Thomas H. McLean , Sayan Mondal
IPC分类号： C07D471/04 , C07D473/36 , C07D473/32 , C07D473/28 , A61P37/00 , A61P35/02 , A61P5/26 , A61P3/10 , A61P25/28
CPC分类号： C07D471/04 , A61P3/10 , A61P5/26 , A61P25/28 , A61P35/02 , A61P37/00 , C07D473/28 , C07D473/32 , C07D473/36
摘要： The present invention provides compounds, compositions thereof, and methods of using the same for the inhibition of TYK2, and the treatment of TYK2-mediated disorders.

95. 发明授权

US09403827B2 Substituted purinone compounds 有权
标题翻译：取代的嘌呤酮化合物
公开(公告)号：US09403827B2
公开(公告)日：2016-08-02
申请号：US14762037
申请日：2014-01-21
申请人： Pascal Furet , Vito Guagnano , Philipp Holzer , Joerg Kallen , Robert Mah , Keiichi Masuya , Achim Schlapbach , Andrea Vaupel
发明人： Pascal Furet , Vito Guagnano , Philipp Holzer , Joerg Kallen , Robert Mah , Keiichi Masuya , Achim Schlapbach , Andrea Vaupel
IPC分类号： A61K31/522 , C07D473/28
CPC分类号： C07D473/28 , A61K31/522
摘要： The invention relates to compounds of formula (I): (I) as described herein, pharmaceutical preparations comprising such compounds, uses and methods of use for such compounds in the treatment of a disorder or a disease mediated by the activity of as MDM2 and/or MDM4, and combinations comprising such compounds.
摘要翻译：本发明涉及式（I）化合物：本文所述的（I）化合物，包含这些化合物的药物制剂，用于治疗由MDM2和/或MDM2的活性介导的病症或疾病的用途和用途的方法，或MDM4，以及包含这些化合物的组合。

96. 发明授权

US09271962B2 Inhibitors of fatty acid amide hydrolase and monoacylglycerol lipase for modulation of cannabinoid receptors 有权
标题翻译：脂肪酸酰胺水解酶和单酰基甘油脂肪酶抑制剂用于调节大麻素受体
公开(公告)号：US09271962B2
公开(公告)日：2016-03-01
申请号：US12933322
申请日：2009-03-17
申请人： Alexandros Makriyannis , Lakshmipathi Pandarinathan , Nikolai Zvonok , Teija Parkkari , Lauren Chapman
发明人： Alexandros Makriyannis , Lakshmipathi Pandarinathan , Nikolai Zvonok , Teija Parkkari , Lauren Chapman
IPC分类号： C07D233/90 , A61K31/41 , A61K31/415 , C07D231/12 , C07D233/56 , C07D235/08 , C07D249/08 , C07D249/18 , C07D263/22 , C07D401/12 , C07D471/04 , C07D473/00 , C07D473/28 , G01N21/64
CPC分类号： G01N33/9406 , A61K31/41 , A61K31/415 , C07D231/12 , C07D233/56 , C07D235/08 , C07D249/08 , C07D249/18 , C07D263/22 , C07D401/12 , C07D471/04 , C07D473/00 , C07D473/28 , G01N21/6428 , G01N2333/70571 , G01N2333/92 , G01N2333/98 , G01N2500/02 , G01N2500/20
摘要： Disclosed are compounds and compositions that inhibit the action of fatty acid amide hydrolase (FAAH) and monoacylglycerol lipase (MGL), methods of inhibiting FAAH and MGL, methods of modulating cannabinoid receptors, and methods of treating various disorders related to modulation of cannabinoid receptors.
摘要翻译：公开了抑制脂肪酰胺水解酶（FAAH）和单酰基甘油脂肪酶（MGL）的作用的化合物和组合物，抑制FAAH和MGL的方法，调节大麻素受体的方法，以及治疗与大麻素受体调节有关的各种疾病的方法。

97. 发明授权

US09133186B2 Hetero ring-fused imidazole derivative having AMPK activating effect 有权
标题翻译：具有AMPK活化作用的异环烯基咪唑衍生物
公开(公告)号：US09133186B2
公开(公告)日：2015-09-15
申请号：US13822189
申请日：2011-09-08
申请人： Keisuke Tonogaki , Akira Ino , Eiichi Kojima , Manabu Katou , Masafumi Iwatsu , Nobuyuki Tanaka , Masahiko Fujioka
发明人： Keisuke Tonogaki , Akira Ino , Eiichi Kojima , Manabu Katou , Masafumi Iwatsu , Nobuyuki Tanaka , Masahiko Fujioka
IPC分类号： C07D487/04 , C07D471/04 , C07D473/00 , C07D473/06 , C07D473/28 , C07D491/048 , C07D495/04 , C07D513/04 , C07D473/30 , C07D491/08 , C07D519/00
CPC分类号： C07D471/04 , C07D473/00 , C07D473/06 , C07D473/28 , C07D473/30 , C07D487/04 , C07D491/048 , C07D491/08 , C07D495/04 , C07D513/04 , C07D519/00
摘要： Disclosed is a compound which is useful as an AMPK activator. A compound represented by the formula: its pharmaceutically acceptable salt, or a solvate thereof, wherein a group represented by the formula: is a group represented by the formula: R1 is each independently halogen, hydroxy, cyano, nitro, carboxy, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl or the like; m is an integer of 0 to 3; R2 is hydrogen, or substituted or unsubstituted alkyl; X is —O—; and Y is substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl.
摘要翻译：公开了可用作AMPK活化剂的化合物。由下式表示的化合物：其药学上可接受的盐或其溶剂合物，其中由下式表示的基团是由下式表示的基团：R 1各自独立地为卤素，羟基，氰基，硝基，羧基，取代或未取代的烷基，取代或未取代的链烯基等; m为0〜3的整数。 R2是氢或取代或未取代的烷基; X是-O-; 并且Y是取代或未取代的芳基，或取代或未取代的杂芳基。

98. 发明授权

US08907086B2 Fused bicyclic heterocycles useful as dipeptidyl peptidase-IV inhibitors 有权
标题翻译：用作二肽基肽酶-IV抑制剂的稠合双环杂环
公开(公告)号：US08907086B2
公开(公告)日：2014-12-09
申请号：US14000641
申请日：2012-03-01
申请人： Chad E. Bennett , Duane A. Burnett , Hongmei Li , Yonggang Chen , Troy McCracken , Monica Vicarel
发明人： Chad E. Bennett , Duane A. Burnett , Hongmei Li , Yonggang Chen , Troy McCracken , Monica Vicarel
IPC分类号： C07D239/70 , C07D401/04 , C07D487/04 , A61K31/4523 , A61K31/517 , A61K31/52 , A61P3/10 , A61K45/06 , A61K31/155 , A61K31/427 , A61K31/519 , A61K31/64 , A61K31/522 , C07D473/28
CPC分类号： C07D487/04 , A61K31/155 , A61K31/427 , A61K31/519 , A61K31/522 , A61K31/64 , A61K45/06 , C07D473/18 , C07D473/28 , A61K2300/00
摘要： The present invention is directed to novel bicyclic heterocycles of structural formula (I) which are inhibitors of the dipeptidyl peptidase-IV enzyme and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly Type 2 diabetes. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the dipeptidyl peptidase-IV enzyme is involved.
摘要翻译：本发明涉及结构式（I）的新型双环杂环，其是二肽基肽酶-IV酶的抑制剂，其可用于治疗或预防涉及二肽基肽酶-IV酶的疾病，例如糖尿病特别是2型糖尿病。本发明还涉及包含这些化合物的药物组合物以及这些化合物和组合物在预防或治疗涉及二肽基肽酶-IV酶的疾病中的用途。

99. 发明申请

US20140288099A1 COMPOSITION 审中-公开
标题翻译：组成
公开(公告)号：US20140288099A1
公开(公告)日：2014-09-25
申请号：US14234070
申请日：2012-07-19
申请人： Claire Louise Ambery , Christopher David Edwards
发明人： Claire Louise Ambery , Christopher David Edwards
IPC分类号： C07D473/28
CPC分类号： C07D473/28 , A61K9/0043 , A61K9/0073 , A61K9/12 , A61K31/522
摘要： Compound (I), and pharmaceutically acceptable salts thereof, are inducers of human interferon. Certain discrete and particular dosages of Compound (I) may be particularly useful in the treatment of various disorders, for example the treatment of allergic diseases and other inflammatory conditions, for example allergic rhinitis and allergic asthma.
摘要翻译：化合物（I）及其药学上可接受的盐是人类干扰素的诱导剂。化合物（I）的某些离散和特定剂量可能特别可用于治疗各种疾病，例如治疗过敏性疾病和其它炎性病症，例如过敏性鼻炎和过敏性哮喘。

100. 发明申请

US20110009607A1 METHOD FOR PREPARING DNA FRAGMENT HAVING STICKY END 审中-公开
标题翻译：用于制备具有末端的DNA片段的方法
公开(公告)号：US20110009607A1
公开(公告)日：2011-01-13
申请号：US12921930
申请日：2009-03-10
申请人： Makoto Komiyama , Akinori Kuzuya , Keita Tanaka
发明人： Makoto Komiyama , Akinori Kuzuya , Keita Tanaka
IPC分类号： C12P19/34 , C07H21/04 , C07C205/06 , C07D239/54 , C07D473/28 , C07H19/09 , C07H19/19
CPC分类号： C12N15/64 , C12N15/66 , C12Q1/686 , C12Q2565/519 , C12Q2525/117
摘要： The present invention provides a method for preparing a DNA fragment, in which a desired double-stranded DNA fragment having a sticky end is directly and easily obtained from an amplification product (an amplified fragment) after PCR without a restriction enzyme digestion. The method for preparing a DNA fragment having a sticky end of the present invention comprises: (i) a step of performing a PCR reaction using a template DNA and specific primers to obtain an amplified DNA fragment; and (ii) a step of performing a prescribed treatment on the amplified DNA fragment to dissociate a protecting group from the fragment. Herein, the above-mentioned specific primers are composed of a complementary DNA portion consisting of a nucleotide sequence complementarily binding to an amplification target region in a template DNA and a non-complementary DNA portion consisting of a nucleotide sequence that links to the 5′ end of the complementary DNA portion but does not complementarily bind to the amplification target sequence, and at least a base corresponding to the 3′ end in the nucleotide sequence of the non-complementary DNA portion is modified with a protecting group capable of terminating the progression of DNA replication catalyzed by a DNA polymerase.
摘要翻译：本发明提供了一种制备DNA片段的方法，其中在没有限制酶消化的PCR之后，从扩增产物（扩增片段）直接容易地获得具有粘性末端的所需双链DNA片段。制备本发明粘性末端的DNA片段的方法包括：（i）使用模板DNA和特异性引物进行PCR反应以获得扩增的DNA片段的步骤; 和（ii）对扩增的DNA片段进行规定的处理以从保护基离解的步骤。本文中，上述特异性引物由与模板DNA中的扩增对象区域互补结合的核苷酸序列和与5'末端连接的核苷酸序列组成的非互补DNA部分构成的互补DNA部分构成的互补DNA部分，但不与扩增靶序列互补结合，并且至少对应于非互补DNA部分的核苷酸序列中3'端的碱基用能够终止进展的保护基进行修饰由DNA聚合酶催化的DNA复制。

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