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1. 发明授权

US10308654B2 Preparation and use of kinase inhibitor 有权
公开(公告)号：US10308654B2
公开(公告)日：2019-06-04
申请号：US15566872
申请日：2016-04-15
申请人： CHANGZHOU LONGTHERA PHARMACEUTICALS INC
发明人： Peng Cheng , Wenjie Cao
IPC分类号： C07D487/04 , A61K31/52 , A61K31/5377 , C07D401/12 , C07D473/28 , C07D473/32 , C07D473/36 , A61P35/02
摘要： Disclosed are a preparation method for a kinase inhibitor and a use thereof. The kinase inhibitor is a compound represented by formula (I) wherein the groups are defined as described in the description. The compound of formula (I) has a kinase inhibitory activity and therefore can be used for the preparation of medicines for treating kinase activity-related diseases.

2. 发明授权

US09132130B2 Purine derivative and antitumor agent using same 有权
标题翻译：嘌呤衍生物和抗肿瘤剂
公开(公告)号：US09132130B2
公开(公告)日：2015-09-15
申请号：US13266681
申请日：2010-04-28
申请人： Toshiaki Suzuki , Hideki Satoh , Toshiyuki Matsuno , Kenichi Saitoh , Soichi Ohta , Manami Masuda , Shinichi Yaguchi , Ichiro Koshimizu , Yuriko Watanabe , Yoshie Minowa , Masayuki Takahashi , Tomoyoshi Kayou
发明人： Toshiaki Suzuki , Hideki Satoh , Toshiyuki Matsuno , Kenichi Saitoh , Soichi Ohta , Manami Masuda , Shinichi Yaguchi , Ichiro Koshimizu , Yuriko Watanabe , Yoshie Minowa , Masayuki Takahashi , Tomoyoshi Kayou
IPC分类号： A61K31/52 , C07D473/36 , C07D487/12 , C07D473/24 , A61K31/5377
CPC分类号： A61K31/52 , A61K31/5377 , C07D473/24
摘要： Disclosed are: a novel purine derivative, a composition thereof, a method for treating tumor using the purine derivative, and an antitumor agent using the purine derivative. Specifically disclosed is a compound represented by formula (I), or a pharmaceutically acceptable salt, solvate or hydrate thereof, or a prodrug thereof.
摘要翻译：公开了一种新型嘌呤衍生物，其组合物，使用嘌呤衍生物治疗肿瘤的方法，以及使用嘌呤衍生物的抗肿瘤剂。具体公开的是由式（I）表示的化合物或其药学上可接受的盐，溶剂合物或水合物或其前药。

3. 发明授权

US07259159B2 Guanidino derivatives as inhibitors of cell adhesion 有权
标题翻译：胍基衍生物作为细胞粘附抑制剂
公开(公告)号：US07259159B2
公开(公告)日：2007-08-21
申请号：US10343173
申请日：2001-07-23
申请人： Anuschirwan Peyman , David Will , Thomas R Gadek , Robert McDowell , Jean Francois Gourvest , Jean-Marie Ruxer , Jochen Knolle
发明人： Anuschirwan Peyman , David Will , Thomas R Gadek , Robert McDowell , Jean Francois Gourvest , Jean-Marie Ruxer , Jochen Knolle
IPC分类号： C07D471/04 , C07D487/04 , C07D473/16 , C07D473/24 , C07D473/28 , C07D473/32 , C07D473/34 , C07D473/36 , C07D473/40 , A61K31/437 , A61K31/519
CPC分类号： C07D473/00 , C07D487/04
摘要： The present invention relates to acylguanidino derivatives of formula (I), in which R1, R2, R3, A, B, X, Y and n have the meanings indicated in claim 1, their physiologically tolerable salts and their prodrugs. The compounds of the formula (I) are valuable pharmaceutically active compounds. They are vitronectin receptor antagonists and inhibitors of cell adhesion and bone resorption by osteoclasts. This renders them suitable, for example, for the therapy and prophylaxis of illness which are based on the interaction between vitronectin receptors and their ligands in cell-cell or cell-matrix interaction processes or which can be prevented, alleviated or cured by influencing such interactions. For example, they can be applied for treating and preventing osteoporosis, or for inhibiting undesired angiogenesis or proliferation of cells of the vascular smooth muscles. The invention furthermore relates to processes for the preparation of compounds of the formula (I), their use, in particular as pharmaceutical active ingredients, and pharmaceutical compositions comprising them
摘要翻译：本发明涉及式（I）的酰基胍基衍生物，其中R 1，R 2，R 3，A，B，X ，Y和n具有权利要求1所述的含义，其生理上可耐受的盐及其前药。式（I）的化合物是有价值的药物活性化合物。它们是玻连蛋白受体拮抗剂和破骨细胞的细胞粘附和骨吸收的抑制剂。这使得它们适合于例如基于玻连蛋白受体及其配体在细胞 - 细胞或细胞 - 基质相互作用过程中的相互作用的疾病的治疗和预防，或通过影响这些相互作用可以预防，缓解或治愈。例如，它们可以用于治疗和预防骨质疏松症，或用于抑制血管平滑肌细胞的不期望的血管生成或增殖。本发明还涉及制备式（I）化合物的方法，其用途，特别是作为药物活性成分，以及包含它们的药物组合物

4. 发明申请

US20050197328A1 Imidazopyridine derivatives as kinase inhibitors 失效
标题翻译：咪唑并吡啶衍生物作为激酶抑制剂
公开(公告)号：US20050197328A1
公开(公告)日：2005-09-08
申请号：US10508760
申请日：2003-03-21
申请人： Nicholas Bailey , Mark Bamford , Haifeng Cui , Stephen Garland , Krista Goodman , Mark Hilfiker , Dennis Lee , Terence Panchal , Robert Stavenger , David Wilson , Jason Witherington
发明人： Nicholas Bailey , Mark Bamford , Haifeng Cui , Stephen Garland , Krista Goodman , Mark Hilfiker , Dennis Lee , Terence Panchal , Robert Stavenger , David Wilson , Jason Witherington
IPC分类号： C07D473/36 , A61K31/4439 , A61K31/4545 , A61K31/496 , A61K31/52 , A61K31/5377 , A61P1/04 , A61P11/06 , A61P19/10 , A61P25/16 , A61P25/28 , A61P29/00 , A61P35/00 , A61P43/00 , C07D471/04 , A61K31/551 , A61K31/498 , A61K31/503 , C07D473/14 , C07D487/02
CPC分类号： C07D471/04
摘要： A compound of the formula and physiologically acceptable salts and or N-oxides thereof wherein, X1 is N or CR3; X2 is N or CR4; X3 is N or CR5; X4 is N or CR6. with the proviso that at least one but not more than two of X1, X2, X3 and X4 represents N. R1 is a 5-, or 6-membered heterocyclic group selected from group a, b, c or d wherein X5 is a group selected from N or CR7 and X6 is a group selected from O, S or NR8; X7 and X8 which may be the same or different is a group selected from N or CR9; X9 is a group selected from O, S or NR8 and X10 is N or CR10; X11, X12 and X13 may be the same or different and selected from a group N or CR11; processes for their preparation, pharmaceutical compositions containing them and their use in medicine.
摘要翻译：下式的化合物及其生理上可接受的盐和/或其N-氧化物，其中X 1是N或CR 3; X 2是N或CR 4; X 3是N或CR 5; X 4是N或CR 6。条件是X 1，X 2，X 3和X 4中的至少一个但不多于两个， SUB>表示N. R 1是选自a，b，c或d的5-或6-元杂环基，其中X 5是选自 N或CR 7和X 6是选自O，S或NR 8的基团; 可以相同或不同的是选自N或CR 9的基团;其中X 1和X 3可以相同或不同。 X 9是选自O，S或NR 8和X 10的基团是N或CR 10; X 11，X 12和X 13可以相同或不同，选自基团N或CR 13， 11 其制备方法，含有它们的药物组合物及其在医药中的用途。

5. 发明申请

US20050176701A1 Inhibitors of hepatitis C virus RNA-dependent RNA polymerase, and compositions and treatments using the same 失效
标题翻译：丙型肝炎病毒RNA依赖性RNA聚合酶的抑制剂，以及使用其的组合物和治疗
公开(公告)号：US20050176701A1
公开(公告)日：2005-08-11
申请号：US10718337
申请日：2003-11-19
申请人： Allen Borchardt , Javier Gonzalez , Hui Li , Maria Linton , John Tatlock
发明人： Allen Borchardt , Javier Gonzalez , Hui Li , Maria Linton , John Tatlock
IPC分类号： A61K31/4025 , A61K31/452 , A61K31/496 , A61K31/519 , A61K31/5377 , A61K31/541 , A61P31/14 , C07D263/58 , C07D285/06 , C07D309/32 , C07D405/06 , C07D405/10 , C07D405/12 , C07D405/14 , C07D407/06 , C07D407/10 , C07D407/12 , C07D409/06 , C07D409/10 , C07D413/02 , C07D413/06 , C07D413/10 , C07D413/12 , C07D413/14 , C07D417/02 , C07D417/06 , C07D417/10 , C07D417/12 , C07D471/04 , C07D473/30 , C07D473/36 , C07D487/04 , C07D495/04 , C07D513/04 , C07D45/02
CPC分类号： C07D285/06 , C07D263/58 , C07D309/32 , C07D405/06 , C07D405/10 , C07D405/12 , C07D405/14 , C07D407/06 , C07D407/10 , C07D407/12 , C07D409/06 , C07D409/10 , C07D413/06 , C07D413/10 , C07D413/12 , C07D413/14 , C07D417/06 , C07D417/10 , C07D417/12 , C07D471/04 , C07D473/30 , C07D473/36 , C07D487/04 , C07D495/04 , C07D513/04
摘要： The invention relates to compounds of the formula 1 and to pharmaceutically acceptable salts, solvates, prodrugs and metabolites thereof, wherein W, Z, R1 and R2, are as defined herein. The invention also relates to methods of treating Hepatitis C virus in mammals by administering the compounds of formula 1, and to pharmaceutical compositions for treating such disorders, which contain the compounds of formula 1. The invention also relates to methods of preparing the compounds of formula 1.
摘要翻译：本发明涉及式1的化合物及其药学上可接受的盐，溶剂合物，前药和代谢物，其中W，Z，R 1和R 2定义同上这里。本发明还涉及通过给予式1化合物治疗哺乳动物中的丙型肝炎病毒的方法以及含有式1化合物的用于治疗这种病症的药物组合物。本发明还涉及制备式 1。

6. 发明授权

US09221855B2 Thionation process and a thionating agent 有权
标题翻译：硫化过程和硫化剂
公开(公告)号：US09221855B2
公开(公告)日：2015-12-29
申请号：US13807104
申请日：2012-02-03
申请人： Birgitta Pettersson , Vedran Hasimbegovic , Per H Svensson , Jan Bergman
发明人： Birgitta Pettersson , Vedran Hasimbegovic , Per H Svensson , Jan Bergman
IPC分类号： C07C325/02 , C07C327/48 , C07F9/58 , C07B45/06 , C07B45/04 , C07D207/24 , C07D209/30 , C07D211/72 , C07D211/84 , C07D213/63 , C07D239/93 , C07D213/83 , C07D309/36 , C07D215/36 , C07D311/84 , C07D219/04 , C07D219/08 , C07D223/06 , C07D341/00 , C07D239/58 , C07D241/08 , C07D241/44 , C07D243/22 , C07D245/04 , C07D471/04 , C07D473/36 , C07D487/04 , C07D207/416 , C07D209/08 , C07D209/34 , C07D209/42 , C07D209/88 , C07D213/70 , C07D211/88 , C07D239/70 , C07D243/14 , C07B45/00
CPC分类号： C07F9/58 , C07B45/00 , C07B45/04 , C07C325/02 , C07C327/48 , C07D207/24 , C07D207/416 , C07D209/08 , C07D209/30 , C07D209/34 , C07D209/42 , C07D209/88 , C07D211/72 , C07D211/84 , C07D211/88 , C07D213/63 , C07D213/70 , C07D213/83 , C07D215/36 , C07D219/04 , C07D219/08 , C07D223/06 , C07D239/58 , C07D239/70 , C07D239/93 , C07D241/08 , C07D241/44 , C07D243/14 , C07D243/22 , C07D245/04 , C07D309/36 , C07D311/84 , C07D341/00 , C07D471/04 , C07D473/36 , C07D487/04
摘要： A process for transforming a group >C═O (I) in a compound into a group >C═S (II) or into a tautomeric form of group (II) in a reaction giving a thionated reaction product, by use of crystalline P2S5.2 C5H5N as a thionating agent. A thionating agent which is crystalline P2S5.2 C5H5N.
摘要翻译：在通过使用结晶P2S5的反应中将化合物中的基团> C = O（I）转化为基团> C = S（II）或互变异构形式的基团（II）的方法，得到硫化反应产物 .2 C5H5N作为硫化剂。结晶P2S5.2 C5H5N的硫化剂。

7. 发明授权

US09115158B2 Thionating agent 有权
公开(公告)号：US09115158B2
公开(公告)日：2015-08-25
申请号：US13936423
申请日：2013-07-08
申请人： VIRONOVA THIONATION AB
发明人： Birgitta Pettersson , Vedran Hasimbegovic , Per H Svensson , Jan Bergman
IPC分类号： C07B45/00 , C07F9/58 , C07B45/04 , C07C325/02 , C07C327/48 , C07D207/24 , C07D209/30 , C07D211/72 , C07D211/84 , C07D213/63 , C07D239/93 , C07D213/83 , C07D309/36 , C07D215/36 , C07D311/84 , C07D219/04 , C07D219/08 , C07D223/06 , C07D341/00 , C07D239/58 , C07D241/08 , C07D241/44 , C07D243/22 , C07D245/04 , C07D471/04 , C07D473/36 , C07D487/04 , C07D207/416 , C07D209/08 , C07D209/34 , C07D209/42 , C07D209/88 , C07D213/70 , C07D211/88 , C07D239/70 , C07D243/14
CPC分类号： C07F9/58 , C07B45/00 , C07B45/04 , C07C325/02 , C07C327/48 , C07D207/24 , C07D207/416 , C07D209/08 , C07D209/30 , C07D209/34 , C07D209/42 , C07D209/88 , C07D211/72 , C07D211/84 , C07D211/88 , C07D213/63 , C07D213/70 , C07D213/83 , C07D215/36 , C07D219/04 , C07D219/08 , C07D223/06 , C07D239/58 , C07D239/70 , C07D239/93 , C07D241/08 , C07D241/44 , C07D243/14 , C07D243/22 , C07D245/04 , C07D309/36 , C07D311/84 , C07D341/00 , C07D471/04 , C07D473/36 , C07D487/04
摘要： A process for transforming a group >C═O (I) in a compound into a group >C═S (II) or into a tautomeric form of group (II) in a reaction giving a thionated reaction product, by use of crystalline P2S5.2C5H5N as a thionating agent. A thionating agent which is crystalline P2S5.2C5H5N.
摘要翻译：在通过使用结晶P2S5的反应中将化合物中的基团> C = O（I）转化为基团> C = S（II）或互变异构形式的基团（II）的方法，得到硫化反应产物 .2C5H5N作为硫化剂。结晶P2S5.2C5H5N的硫化剂。

8. 发明授权

US5866702A Purine inhibitors of cyclin dependent kinase 2 失效
标题翻译：细胞周期蛋白依赖性激酶2的嘌呤抑制剂
公开(公告)号：US5866702A
公开(公告)日：1999-02-02
申请号：US692012
申请日：1996-08-02
申请人： Richard Mackman , Robert T. Lum , Steven R. Schow , Michael M. Wick
发明人： Richard Mackman , Robert T. Lum , Steven R. Schow , Michael M. Wick
IPC分类号： C07D473/00 , A61K31/52 , A61P3/10 , A61P9/00 , A61P13/12 , A61P19/06 , A61P25/00 , A61P31/10 , A61P35/00 , C07D233/00 , C07D239/00 , C07D473/04 , C07D473/16 , C07D473/18 , C07D473/20 , C07D473/22 , C07D473/24 , C07D473/30 , C07D473/32 , C07D473/34 , C07D473/36 , C07D473/38 , C07D473/40
CPC分类号： C07D473/16 , C07D473/40
摘要： A 2,6,9-trisubstituted purine composition having the following formula: ##STR1## where X is a amino, oxo, thio, of sulfone moiety, R.sub.1 is a lower alkyl, substituted lower alkyl, cycloalkyl, substituted cycloalkyl, cycloheteroalkyl, substituted cycloheteroalkyl, aryl, substituted aryl, heterocycle, hetaryl, substituted hetaryl, aralkyl, heteroaralkyl, heteroalkyl, alkyl alkenyl, alkyl alkynyl, alkyl cycloalkyl, or alkyl cycloheteroalkyl, each having from 1 to 20 carbon atoms; R.sub.2 is hydrogen, lower alkyl, substituted lower alkyl, cycloalkyl, substituted cycloalkyl, aryl, substituted aryl, heterocycle, hetaryl, substituted hetaryl, aralkyl, heteroaralkyl, heteroalkyl, alkyl alkenyl, alkyl alkynyl, alkyl cycloalkyl, or alkyl cycloheteroalkyl; and R.sub.3 is halogen, hydroxyl, thio, alkoxy, alkylthio, lower alkyl, --NR.sub.4 R.sub.5 or a component having the formula: ##STR2## wherein when R.sub.3 is 2-hydroxyethylamino and R.sub.2 is methyl, R.sub.1 -X is not amino, 3-methyl-2-butenylamino, benzylamino, or m-hydroxybenzyl-amino, when R.sub.3 is 2-hydroxyethylamino and R.sub.2 is isopropyl, R.sub.1 -X is not benzylamino, m-hydroxybenzylamino, or 3-methylbutylamino, when R.sub.3 is 2-hydroxyethylamino and R.sub.2 is 2-hydroxyethyl, R.sub.1 -X is not benzylamino and when R.sub.3 is selected from the group consisting of 2-propanol-2-methylamino and 2-dimethylaminoethylamino and R.sub.2 is methyl, then R.sub.1 -X is not benzylamino.
摘要翻译：具有下式的2,6,9-三取代嘌呤组合物：其中X是砜部分的氨基，氧代，硫代，R1是低级烷基，取代的低级烷基，环烷基，取代的环烷基，环杂烷基，取代的杂环烷基，芳基，取代的芳基，杂环，杂芳基，取代的杂芳基，芳烷基，杂芳烷基，杂烷基，烷基烯基，烷基炔基，烷基环烷基或烷基环杂烷基，各自具有1至20个碳原子; R 2是氢，低级烷基，取代的低级烷基，环烷基，取代的环烷基，芳基，取代的芳基，杂环，杂芳基，取代的杂芳基，芳烷基，杂芳烷基，杂烷基，烷基烯基，烷基炔基，烷基环烷基或烷基环杂烷基。 R 3为卤素，羟基，硫代，烷氧基，烷硫基，低级烷基，-NR 4 R 5或具有下式的组分：其中当R 3为2-羟基乙基氨基且R 2为甲基时，R 1 -X不为氨基， -2-丁烯基氨基，苄基氨基或间羟基苄基 - 氨基，当R 3为2-羟基乙基氨基且R 2为异丙基时，当R 3为2-羟基乙基氨基时，R 1 -X为苄基氨基，间羟基苄基氨基或3-甲基丁基氨基， 2-羟乙基，R1-X不是苄基氨基，当R3选自2-丙醇-2-甲基氨基和2-二甲基氨基乙基氨基，R2是甲基时，则R1-X不是苄基氨基。

9. 发明授权

US5369098A Hydroxymethyl cyclobutyl purines 失效
标题翻译：羟甲基环丁基嘌呤
公开(公告)号：US5369098A
公开(公告)日：1994-11-29
申请号：US367167
申请日：1989-06-16
申请人： William A. Slusarchyk
发明人： William A. Slusarchyk
IPC分类号： C07D239/47 , A61K31/505 , A61K31/52 , A61K31/522 , A61P31/12 , C07C31/44 , C07C35/04 , C07C69/013 , C07C309/66 , C07C309/73 , C07D239/46 , C07D239/54 , C07D473/00 , C07D473/16 , C07D473/18 , C07D473/30 , C07D473/34 , C07D473/36 , C07D473/40 , C07F7/18 , C07F9/6512 , C07F9/6561 , A61K31/675
CPC分类号： C07D239/47 , C07C309/66 , C07C309/73 , C07C31/44 , C07C35/04 , C07D239/54 , C07D473/00
摘要： Antiviral activity is exhibited by compounds having the formula ##STR1## and their pharmaceutically acceptable salts. R.sub.1 is ##STR2## R.sub.2 is hydrogen, --PO.sub.3 H.sub.2, ##STR3## wherein R.sub.3 is hydrogen, alkyl, substituted alkyl, or aryl, and R.sub.4 is alkyl.
摘要翻译：抗病毒活性由具有式“IMAGE”1的化合物及其药学上可接受的盐显示。 R 1是氢，-PO 3 H 2，其中R 3是氢，烷基，取代的烷基或芳基，且R 4是烷基。

10. 发明授权

US5049566A Imidazole [4,5-c] pyridine derivatives having gastric acid antisecretory activity and pharmaceutical compositions containing them 失效
标题翻译：具有胃酸抗分泌活性的咪唑[4,5-c]吡啶衍生物和含有它们的药物组合物
公开(公告)号：US5049566A
公开(公告)日：1991-09-17
申请号：US493957
申请日：1990-03-14
申请人： Paolo Chiesi , Vittorino Servadio , Roberta Rassetti
发明人： Paolo Chiesi , Vittorino Servadio , Roberta Rassetti
IPC分类号： A61K31/415 , A61K31/4184 , A61K31/435 , A61K31/44 , A61K31/4427 , A61K31/47 , A61K31/496 , A61K31/52 , A61P1/04 , C07D233/84 , C07D235/10 , C07D401/12 , C07D403/12 , C07D471/04 , C07D473/00 , C07D473/36 , C07D473/38 , C07D495/04
CPC分类号： C07D401/12 , C07D233/84 , C07D403/12 , C07D471/04 , C07D473/36 , C07D473/38 , C07D495/04
摘要： Imidazo[4,5-c] pyridine compounds and physiologically acceptable salts thereof having antiulcer and gastric acid antisecretory activities and pharmaceutical compositions containing them.

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