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1. 发明申请

WO2018041763A1 7-SUBSTITUTED SULFONIMIDOYLPURINONE COMPOUNDS FOR THE TREATMENT AND PROPHYLAXIS OF VIRUS INFECTION 审中-公开
标题翻译： 7-取代磺胺甲基嘌呤酮化合物治疗和预防病毒感染
公开(公告)号：WO2018041763A1
公开(公告)日：2018-03-08
申请号：PCT/EP2017/071514
申请日：2017-08-28
申请人： F. HOFFMANN-LA ROCHE AG , HOFFMANN-LA ROCHE INC.
发明人： GAO, Lu , LIANG, Chungen , YUN, Hongying , ZHENG, Xiufang , WANG, Jianping , MIAO, Kun , ZHANG, Bo
IPC分类号： C07D473/24 , A61K31/522 , A61P31/00
摘要： The present invention relates to compounds of formula (I), wherein R 1 , R 2 and R 3 are as described herein, and their prodrugs or pharmaceutically acceptable salt, enantiomer or diastereomer thereof, and compositions including the compounds and methods of using the compounds as TLR7 agonists for the treatment of viral infections.
摘要翻译：本发明涉及式（I）的化合物，其中R 1，R 2和R 3如上所定义，如本文所述，及其前药或其药学上可接受的盐，对映异构体或非对映异构体，以及包含所述化合物的组合物和使用所述化合物作为TLR7激动剂治疗病毒感染的方法。

2. 发明申请

WO2007034916A1 新規アデニン化合物审中-公开
标题翻译：新颖的化合物
公开(公告)号：WO2007034916A1
公开(公告)日：2007-03-29
申请号：PCT/JP2006/318854
申请日：2006-09-22
申请人：大日本住友製薬株式会社 , アストラゼネカ・アクチエボラーグ , ミリチップイアン , マキナリートマス , ボナートロジャー
发明人：ミリチップイアン , マキナリートマス , ボナートロジャー
IPC分类号： C07D473/18 , A61K31/522 , A61P11/02 , A61P11/06 , A61P17/00 , A61P27/02 , A61P31/12 , A61P31/18 , A61P35/00 , A61P37/02 , A61P37/08 , A61P43/00 , C07D473/16 , C07D473/24 , C07D473/34
CPC分类号： C07D473/18
摘要： A novel adenine compound represented by the formula (1): (1) [wherein Z represents (un)substituted alkylene, a single bond, etc.; R 1 represents an (un)substituted alkyl, alkenyl, alkynyl, cycloalkyl, aryl, or heteroaryl group; R 2 represents hydrogen or (un)substituted alkyl; R 3 , R 4 , and R 5 each independently represents an (un)substituted alkyl, alkenyl, alkynyl, aryl, or heteroaryl group, provided that R 3 and R 5 may be bonded to each other to form a 3- to 7-membered, saturated carbocycle or heterocycle in cooperation with the adjacent carbon atom; and X represents oxygen, sulfur, SO 2 , NR 6 (R 6 represents hydrogen or alkyl), or a single bond] or a pharmaceutically acceptable salt of the compound. The compound and salt are useful as a medicine.
摘要翻译：由式（1）表示的新颖腺嘌呤化合物：（1）[其中Z表示（un）取代的亚烷基，单键等; R 1表示（未）取代的烷基，烯基，炔基，环烷基，芳基或杂芳基; R 2表示氢或（未）取代的烷基; R 4，R 4和R 5各自独立地表示（未）取代的烷基，烯基，炔基，芳基或杂芳基，条件是R 3和R 5可以彼此键合以与相邻碳原子一起形成3-至7-元饱和碳环或杂环; 和X表示氧，硫，SO 2，NR 6（R 6表示氢或烷基）或单键]或药学上化合物的可接受的盐。化合物和盐可用作药物。

3. 发明申请

WO01058902A1 PYRIMIDINE COMPOUNDS AND THEIR USE AS MODULATORS OF CHEMOKINE RECEPTOR ACTIVITY 审中-公开
标题翻译：吡嗪类化合物及其作为化合物受体活性的调节剂
公开(公告)号：WO01058902A1
公开(公告)日：2001-08-16
申请号：PCT/SE2001/000245
申请日：2001-02-07
IPC分类号： A61K31/522 , A61P1/04 , A61P3/10 , A61P5/14 , A61P7/04 , A61P9/10 , A61P9/14 , A61P11/00 , A61P11/02 , A61P11/06 , A61P13/12 , A61P15/00 , A61P17/00 , A61P17/02 , A61P17/04 , A61P17/06 , A61P17/14 , A61P19/02 , A61P25/00 , A61P25/06 , A61P25/14 , A61P25/28 , A61P27/02 , A61P29/00 , A61P31/04 , A61P31/08 , A61P31/18 , A61P35/00 , A61P35/04 , A61P37/02 , A61P37/06 , A61P37/08 , A61P41/00 , A61P43/00 , C07D473/24 , C07D487/04 , A61K31/519
CPC分类号： C07D473/24
摘要： The invention provides certain heterocyclic compounds, processes and intermediates used in their preparation, pharmaceutical compositions containing them and their use in therapy; in formula (I), A is a group of formula (a) or (b).
摘要翻译：本发明提供某些杂环化合物，其制备中使用的方法和中间体，含有它们的药物组合物及其在治疗中的用途; 在式（I）中，A是式（a）或（b）的基团。

4. 发明申请

WO01009134A1 PURINE DERIVATIVES INHIBITORS OF TYROSINE PROTEIN KINASE SYK 审中-公开
标题翻译：酪氨酸蛋白激酶SYK的嘌呤衍生物抑制剂
公开(公告)号：WO01009134A1
公开(公告)日：2001-02-08
申请号：PCT/EP2000/007311
申请日：2000-07-28
IPC分类号： A61K31/52 , A61K31/522 , A61K31/5377 , A61P9/14 , A61P11/00 , A61P11/02 , A61P17/00 , A61P17/02 , A61P17/06 , A61P17/14 , A61P29/00 , A61P37/08 , A61P43/00 , C07D473/16 , C07D473/18 , C07D473/24
CPC分类号： C07D473/24 , A61K31/52 , C07D473/16 , C07D473/18
摘要： Compounds of formula (I) in free or salt form, where X, R , R , R and R are as defined in the specification, their preparation and their use as pharmaceuticals, particularly for the treatment of inflammatory or obstructive airways disease.
摘要翻译：游离或盐形式的式（I）化合物，其中X，R 1，R 2，R 3和R 4如说明书中所定义，它们的制备及其作为药物的用途，特别是用于治疗炎性或阻塞性气道疾病。

5. 发明申请

WO00071543A1 PURINE DERIVATIVES, PREPARATION METHOD AND PHARMACEUTICAL COMPOSITIONS CONTAINING SAME 审中-公开
标题翻译：嘌呤衍生物，制备方法和含有其的药物组合物
公开(公告)号：WO00071543A1
公开(公告)日：2000-11-30
申请号：PCT/FR2000/001335
申请日：2000-05-18
IPC分类号： C07D473/16 , A61K31/52 , A61P17/06 , A61P25/28 , A61P31/04 , A61P33/00 , A61P35/00 , A61P43/00 , C07D473/00 , C07D473/18 , C07D473/24 , C07D473/40
CPC分类号： C07D473/00 , A61K31/52
摘要： The invention concerns novel products of formula (I), wherein: Z represents -CH2-, -SO2-, -CO-, -COO-, -CONH- or -(CH2)2-NR3-; n represents 0 or 1; R1 represents hydrogen, aryl, -CH2-aryl, -SO2-aryl, -CO-aryl, heterocyclic, -CH2- heterocyclic, alkyl and -SO2-alkyl; R2 represents alkyl, cycloalkyl or heterocycle containing oxygen, sulphur or NR3; Y represents oxygen, sulphur or NR3; D1 and D2 are either selected among hydrogen, hydroxyl, alkyl, alkoxy and NHR5, or form =O, or =N-OR4; R3 represents hydrogen, alkyl or cycloalkyl; R4 represents hydrogen, alkyl, cycloalkyl or aryl; R5 represents hydrogen, alkyl, cycloalkyl or -COOtbu; R6 represents hydrogen, halogen, hydroxyl, alkyl, alkoxy or NHR3; said products being all in isomeric forms and their salts, as medicines.
摘要翻译：本发明涉及式（I）的新产物，其中：Z表示-CH 2 - ， - SO 2 - ， - CO - ， - COO - ， - CONH-或 - （CH 2）2 -NR 3 - n表示0或1; R 1表示氢，芳基，-CH 2 - 芳基，-SO 2 - 芳基，-CO-芳基，杂环，-CH 2 - 杂环，烷基和-SO 2 - 烷基; R 2表示含有氧，硫或NR 3的烷基，环烷基或杂环; Y表示氧，硫或NR 3; D1和D2选自氢，羟基，烷基，烷氧基和NHR5，或形式= O或= N-OR4; R3代表氢，烷基或环烷基; R4表示氢，烷基，环烷基或芳基; R5代表氢，烷基，环烷基或-COOtbu; R6表示氢，卤素，羟基，烷基，烷氧基或NHR3; 所述产品全部为异构体形式及其盐，作为药物。

6. 发明申请

WO99002162A1 CYCLIN DEPENDENT KINASE INHIBITING PURINE DERIVATIVES 审中-公开
标题翻译： CYCLIN依赖性激酶抑制嘌呤衍生物
公开(公告)号：WO99002162A1
公开(公告)日：1999-01-21
申请号：PCT/GB1998/002025
申请日：1998-07-10
IPC分类号： A61K31/52 , A61K31/522 , A61K31/7042 , A61K31/7052 , A61K31/7076 , A61P35/00 , A61P43/00 , C07D473/18 , C07D473/24 , C07D473/26 , C07D473/30 , C07D473/40 , C07H15/26 , C07H17/02 , A61K31/70
CPC分类号： C07H15/26 , C07D473/18 , C07D473/30 , C07D473/40
摘要： A range is disclosed of purine derivatives (I) which can act as inhibitors of cyclin dependent kinases (CDKs) and which thereby c an provide useful therapeutic compounds for use in treatment of tumours or other cell proliferation disorders. The compounds of this invention bind to CDK molecules in a manner that appears to be different to that of known CDK inhibitors such as olomoucine and roscovitine. In formula (I), in preferred embodiments: X is O, S or CHRx where Rx is H or C1-4 alkyl; D is H, halo or NZ1Z2 where Z1 and Z2 are each independently H or C1-4 alkyl or C1-4 hydroxyalkyl; A is selected from H, C1-4 alkyl, C1-4 alkoxy, hydroxy, CH2(CH2)nOH (n=1-4), and NRa1Ra2 where Ra1 and Ra2 are each independently H or C1-4 alkyl; B is selected from H, C1-4 alkyl, C1-4 alkoxy, CF3, an optionally substituted aryl (e.g. phenyl) or an optionally substituted aralkyl (e.g. benzyl), and an hydroxy group that provides a C=O tautomer; and Y is or includes an optionally substituted 4- to 8-membered carbocyclic or heterocyclic ring; or comprises an optionally substituted linear or branched hydrocarbon chain.
摘要翻译：公开了可作为细胞周期蛋白依赖性激酶（CDK）抑制剂的嘌呤衍生物（I）的范围，由此可以提供用于治疗肿瘤或其它细胞增殖病症的有用的治疗化合物。本发明的化合物以与已知的CDK抑制剂例如奥洛莫斯和罗斯考维胺似乎不同的方式结合CDK分子。在式（I）中，在优选的实施方案中：X是O，S或CHR x，其中Rx是H或C 1-4烷基; D是H，卤素或NZ 1 Z 2，其中Z 1和Z 2各自独立地为H或C 1-4烷基或C 1-4羟基烷基; A选自H，C 1-4烷基，C 1-4烷氧基，羟基，CH 2（CH 2）n OH（n = 1-4）和NR a R a 2，其中R 1a和R 2a各自独立地为H或C 1-4烷基; B选自H，C 1-4烷基，C 1-4烷氧基，CF 3，任选取代的芳基（如苯基）或任选取代的芳烷基（如苄基）和提供C = O互变异构体的羟基; 并且Y是或包括任选取代的4-至8-元碳环或杂环; 或包含任选取代的直链或支链烃链。

7. 发明申请

WO2016147185A1 ADENOSINE THIOPHOSPHATE DERIVATIVES AND USES THEREOF 审中-公开
标题翻译：腺嘌呤硫代磷酸酯衍生物及其用途
公开(公告)号：WO2016147185A1
公开(公告)日：2016-09-22
申请号：PCT/IL2016/050288
申请日：2016-03-16
申请人： BAR-ILAN UNIVERSITY , RAMOT AT TEL-AVIV UNIVERSITY LTD.
发明人： FISCHER, Bilha , OFFEN, Daniel
IPC分类号： C07D405/14 , C07D473/24 , C07D473/34 , C07D473/40 , C07D473/16 , A61K31/66 , A61K31/52 , A61P25/28 , A61P39/00 , A61P39/04 , C07H19/167 , C07H19/20 , C07H21/02 , C07F9/02 , A61K31/7076
CPC分类号： C07H19/20 , A61K31/7076 , C07F9/65616
摘要： Novel adenosine 5'-thiophosphate derivatives, represented by Formulae (I) or (I*), and salts thereof, represented by Formulae (Ia) and (I*a), as defined in the specification, and uses thereof as antioxidants and/or P2Y 1 -R agonists, and/or in the treatment of medical conditions associated with oxidative stress and/or neurodegeneration, and in the treatment of Alzheimer's Disease in particular, are disclosed.
摘要翻译：由式（I）或（I *）表示的新型腺苷5'-硫代磷酸酯衍生物及其盐，其如本说明书中所定义的式（Ia）和（I * a）表示，及其用作抗氧化剂和/ 或P2Y1-R激动剂，和/或治疗与氧化应激和/或神经变性相关的医学病症，特别是治疗阿尔茨海默病。

8. 发明申请

WO2010090491A2 아데포비어 디피복실의 신규한 염 및 그의 제조방법 审中-公开
标题翻译： ADEFOVIR DIPIVOXIL的新型盐及其制备方法
公开(公告)号：WO2010090491A2
公开(公告)日：2010-08-12
申请号：PCT/KR2010/000771
申请日：2010-02-09
申请人： 주식회사 한독약품 , 신동성 , 김동욱 , 원권연
发明人： 신동성 , 김동욱 , 원권연
IPC分类号： C07D473/24 , C07D473/16
CPC分类号： C07D473/24 , C07D473/16 , C07D473/34
摘要： 본 발명은 아데포비어 디피복실(Adefovir dipivoxil)의 신규한 염 및 그의 제조방법에 관한 것으로, 구체적으로는 아데포비어 디피복실을 약제학적으로 허용가능한 지방산과 반응시켜 용해도, 비흡습성, 생체이용율, 분체흐름성 등을 개선시킨 우수한 결정성 산부가염 및 그의 제조방법에 관한 것이다. 본 발명의 제조방법으로 제조한 아데포비어 디피복실의 신규한 염은 기존의 아데포비어 디피복실 또는 그의 염에 비하여 물리화학적, 약학적으로 안정하고 우수한 성질을 나타낸다.
摘要翻译：本发明涉及阿德福韦酯的新型盐及其制备方法。更具体地说，本发明涉及高品质结晶酸加成盐及其制备方法，其中结晶酸加成盐通过使阿德福韦酯与药学上可接受的脂肪酸反应而具有改善的溶解性，非吸湿性，生物利用度和粉末流动性。根据本发明制备的阿德福韦酯的新型盐在物理化学和药学上是稳定的，并且比现有的阿德福韦酯或其盐显示出改进的性能。

9. 发明申请

WO2007134298A3 THERAPEUTIC COMPOUNDS AND THEIR USE IN CANCER 审中-公开
标题翻译：治疗化合物及其在癌症中的应用
公开(公告)号：WO2007134298A3
公开(公告)日：2008-07-31
申请号：PCT/US2007068899
申请日：2007-05-14
申请人： MYRIAD GENETICS INC , BAJJI ASHOK C , KIM SE-HO , MARKOVITZ BENJAMIN , TROVATO RICHARD , TANGALLAPALLY RAJENDRA , ANDERSON MARK B , WETTSTEIN DANIEL , SHENDEROVICH MARK , VANECKO JOHN A
发明人： BAJJI ASHOK C , KIM SE-HO , MARKOVITZ BENJAMIN , TROVATO RICHARD , TANGALLAPALLY RAJENDRA , ANDERSON MARK B , WETTSTEIN DANIEL , SHENDEROVICH MARK , VANECKO JOHN A
IPC分类号： C07D473/34 , A61K31/52 , A61K31/522 , A61P35/00 , C07D473/24 , C07D473/30 , C07D473/40
CPC分类号： A61K31/52 , A61K31/522 , C07D473/34
摘要： Compounds of the formula (I) (II) (III) in which A is chosen from a substituted or unsubstituted aryl, heteroaryl, heterocyclic, or carbocyclic group! B is chosen from a substituted or unsubstituted aryl, heteroaryl, heterocyclic, or carbocyclic group Rl is chosen from hydro, alkyl, aryl, heteroaryl, amino, halo, sulfur, and thioalkyl.
摘要翻译：式（I）（II）（III）的化合物，其中A选自取代或未取代的芳基，杂芳基，杂环或碳环基团！ B选自取代或未取代的芳基，杂芳基，杂环或碳环基R1选自氢，烷基，芳基，杂芳基，氨基，卤素，硫和硫代烷基。

10. 发明申请

WO2006014325A3 C-MET MODULATORS AND METHOD OF USE 审中-公开
标题翻译： C-MET调制器及其使用方法
公开(公告)号：WO2006014325A3
公开(公告)日：2007-03-01
申请号：PCT/US2005023364
申请日：2005-07-01
申请人： EXELIXIS INC , BANNEN LYNNE CANNE , CHAN DIVA SZE-MING , DALRYMPLE LISA ESTHER , JAMMALAMADAKA VASU , KHOURY RICHARD GEORGE , LEAHY JAMES WILLIAM , MAC MORRISON B , MANN GRACE , MANN LARRY W , NUSS JOHN M , PARKS JASON JEVIOUS , WANG YONG , XU WEI
发明人： BANNEN LYNNE CANNE , CHAN DIVA SZE-MING , DALRYMPLE LISA ESTHER , JAMMALAMADAKA VASU , KHOURY RICHARD GEORGE , LEAHY JAMES WILLIAM , MAC MORRISON B , MANN GRACE , MANN LARRY W , NUSS JOHN M , PARKS JASON JEVIOUS , WANG YONG , XU WEI
IPC分类号： C07D471/04 , A61K31/4355 , A61K31/4365 , A61K31/437 , A61K31/519 , A61K31/52 , A61K31/522 , A61P35/00 , C07D473/06 , C07D473/16 , C07D473/18 , C07D473/22 , C07D473/24 , C07D473/30 , C07D473/34 , C07D473/38 , C07D473/40 , C07D487/04 , C07D491/04 , C07D495/04
CPC分类号： C07D487/04 , C07D209/52 , C07D471/04 , C07D473/30 , C07D473/32 , C07D493/04 , C07D493/14 , C07D493/20 , C07D498/04
摘要： The present invention provides compounds for modulating protein kinase enzymatic activity for modulating cellular activities such as proliferation, differentiation, programmed cell death, migration and chemoinvasion. More specifically, the invention provides appropriately functionalized 5,6-fused bicyclics which inhibit, regulate and/or modulate kinase receptor, particularly c-Met, KDR, and flt-3, signal transduction pathways related to the changes in cellular activities as mentioned above, compositions which contain these compounds, and methods of using them to treat kinase-dependent diseases and conditions.
摘要翻译：本发明提供用于调节蛋白激酶酶活性以调节细胞活性如增殖，分化，程序性细胞死亡，迁移和化学侵蚀的化合物。更具体地，本发明提供了适当的功能化的5,6融合双链体，其抑制，调节和/或调节与上述细胞活性变化相关的激酶受体，特别是c-Met，KDR和flt-3信号转导途径，含有这些化合物的组合物，以及使用它们治疗激酶依赖性疾病和病症的方法。

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