公开(公告)号：US09688794B2

公开(公告)日：2017-06-27

申请号：US14434719

申请日：2013-10-15

Applicant: Iowa State University Research Foundation, Inc.

Inventor： Jason Shih-Hao Chen ,  Michael Richard Kessler ,  Michael Dennis Zenner

IPC: A01N43/40 ,  C07D401/00 ,  C07D405/00 ,  C08F122/20 ,  C07D493/04 ,  C09J4/00 ,  C08G18/32 ,  C08G18/77 ,  C08L75/08

CPC classification number: C08F122/20 ,  C07D493/04 ,  C08G18/3218 ,  C08G18/771 ,  C08L75/08 ,  C08L2201/50 ,  C09J4/00 ,  C09J135/02

Abstract: The present invention relates to tackifier compounds and methods of using the same. In various embodiments, the present invention provides a tackifier compound including independently substituted or unsubstituted fused rings A and B each independently chosen from (C5-C10)cycloalkyl and (C2-C10)heterocyclyl. Fused ring A is substituted with (R1)1-8 and fused ring B is substituted with —(OC(O)R′C(O)R2)1-8. At each occurrence R′ is independently chosen from (C2-C10)alkanylene, (C2-C10)alkenylene, (C2-C10)alkynylene, C5-C20(arylene), and (C1-C20)heteroarylene, wherein R′ is unsubstituted or substituted. At each occurrence R1 is independently selected from —OH, —OR3, and —OC(O)R′C(O)R2. At each occurrence R2 is independently chosen from —OH, —OR3, —NH2, —NHR3, and —NR32. At each occurrence R3 is independently chosen from (C1-C10)alkanyl, (C2-C10)alkenyl, (C2-C10)alkynyl, C5-C20(aryl), and (C1-C20)heteroaryl, wherein R3 is unsubstituted or substituted.

公开(公告)号：US09611220B2

公开(公告)日：2017-04-04

申请号：US14472059

申请日：2014-08-28

Applicant: Gilead Sciences, Inc.

Inventor： Marc Labelle ,  Thomas Boesen ,  Mukund Mehrotra ,  Qasim Khan ,  Farman Ullah

IPC: A61K31/00 ,  A61K31/497 ,  A61K31/445 ,  A61K31/44 ,  C07D401/00 ,  C07D211/68 ,  C07D211/80 ,  C07D213/02 ,  C07D405/00 ,  C07D211/78 ,  C07D211/90 ,  C07D213/79 ,  C07D401/12 ,  C07D405/12 ,  C07D413/12 ,  A61K31/443 ,  A61K31/4439 ,  A61K31/4545 ,  A61K31/496 ,  C07D401/06 ,  A61K31/444

Abstract: The present application discloses compounds capable of modulating the activity of histone demethylases (HDMEs), which are useful for prevention and/or treatment of diseases in which genomic dysregulation is involved in the pathogenesis, such as e.g. cancer. The present application also discloses pharmaceutical compositions comprising said compounds and the use of such compounds as a medicament. The compounds take the form

公开(公告)号：US09556144B2

公开(公告)日：2017-01-31

申请号：US14408254

申请日：2012-06-15

Applicant: Songzhu An

Inventor： Songzhu An

IPC: A61K31/54 ,  A61K31/50 ,  A61K31/495 ,  A61K31/4965 ,  A61K31/44 ,  A61K31/501 ,  A61K31/497 ,  A61K31/47 ,  C07D217/00 ,  C07D217/22 ,  C07D471/02 ,  C07D471/00 ,  C07D491/00 ,  C07D487/00 ,  C07D495/00 ,  C07D497/00 ,  C07D401/00 ,  C07D403/00 ,  C07D405/00 ,  C07D409/00 ,  C07D411/00 ,  C07D413/00 ,  C07D417/00 ,  C07D419/00 ,  C07D401/14 ,  C07D401/12 ,  C07D471/04

CPC classification number: C07D471/04 ,  C07D217/22 ,  C07D401/12 ,  C07D401/14

Abstract: The present invention relates to a compound having the structure of Formula I as inhibitor of WNT signal transduction pathways, as well as a composition comprising the compound. Further, the present invention relates to the use of the compound and the method of inhibiting the WNT signal transduction pathways.

Abstract translation: 本发明涉及具有式I结构的化合物作为WNT信号转导途径的抑制剂，以及包含该化合物的组合物。 此外，本发明涉及该化合物的用途和抑制WNT信号转导途径的方法。

公开(公告)号：US09512089B2

公开(公告)日：2016-12-06

申请号：US14459143

申请日：2014-08-13

Applicant: Roche Palo Alto LLC

Inventor： Li Chen ,  Michael Patrick Dillon ,  Lichun Feng ,  Ronald Charles Hawley ,  Minmin Yang

IPC: A01N43/64 ,  A61K31/41 ,  C07D401/00 ,  C07D403/00 ,  C07D405/00 ,  C07D409/00 ,  C07D257/04 ,  C07D401/10 ,  C07D401/14 ,  C07D405/12 ,  C07D409/14 ,  C07D471/04 ,  C07D413/12

CPC classification number: C07D257/04 ,  C07D401/10 ,  C07D401/14 ,  C07D405/12 ,  C07D409/14 ,  C07D413/12 ,  C07D471/04

Abstract: Compounds of the formula I: or a pharmaceutically acceptable salt thereof, wherein, R1 is optionally substituted tetrazolyl, R2 is optionally substituted phenyl, optionally substituted pyridinyl or optionally substituted thienyl, and R3, R4, R5, R6 R7 and R8 are as defined herein. Also provided are methods of using the compounds for treating diseases associated with the P2X3 and/or a P2X2/3 receptor antagonist and methods of making the compounds.

公开(公告)号：US09320803B2

公开(公告)日：2016-04-26

申请号：US14001387

申请日：2012-02-24

Applicant: Felix Kratz ,  Katrin Hochdoerffer

Inventor： Felix Kratz ,  Katrin Hochdoerffer

IPC: A61K38/00 ,  A61K47/00 ,  A01N43/04 ,  A61K31/70 ,  A01N43/00 ,  A61K31/33 ,  A01N43/64 ,  A61K31/41 ,  A01N43/36 ,  A61K31/40 ,  A01N43/16 ,  A61K31/35 ,  C07H15/24 ,  C07D345/00 ,  A61K47/48 ,  C07K5/062 ,  C07K5/078 ,  C07D405/00 ,  C07H15/252 ,  A61K31/704 ,  A61P19/08 ,  A61P35/00

CPC classification number: A61K47/48084 ,  A61K31/35 ,  A61K31/40 ,  A61K31/704 ,  A61K38/00 ,  A61K47/48338 ,  A61K47/548 ,  A61K47/65 ,  C07D405/00 ,  C07H15/252 ,  C07K5/06026 ,  C07K5/06052 ,  C07K5/06139

Abstract: The present invention relates to a prodrug, comprising a pharmaceutically and/or diagnostically active compound, and one or more bisphosphonate groups, to a process for producing such a prodrug, and to a pharmaceutical composition comprising said prodrug, to be used for the treatment of bone-related disorders such as bone cancer.

Abstract translation: 本发明涉及包含药学和/或诊断活性化合物和一种或多种二膦酸酯基团的前体药物，以及制备这种前药的方法，以及包含所述前药的药物组合物，用于治疗 骨相关疾病如骨癌。

公开(公告)号：US09173424B2

公开(公告)日：2015-11-03

申请号：US13381393

申请日：2010-07-10

Applicant: Yili Wang ,  Andrew Daniher ,  Adri De Klerk ,  Cornelis Winkel

Inventor： Yili Wang ,  Andrew Daniher ,  Adri De Klerk ,  Cornelis Winkel

IPC: A23L1/226 ,  C07D405/00 ,  C07D213/46 ,  A23L1/22 ,  C07D213/50 ,  C07D405/06 ,  C07D405/10

CPC classification number: A23L1/22678 ,  A23L27/2024 ,  A23L27/203 ,  A23L27/2052 ,  A23L27/2054 ,  A23L27/70 ,  C07D213/46 ,  C07D213/50 ,  C07D405/00 ,  C07D405/06 ,  C07D405/10

Abstract: A compound (including salts thereof) according to Formula I in which R1 is H, methyl or ethyl; R2 is H, OH, fluorine, C1-C4 linear or branched alkyl, C1-C6 alkoxy wherein the alkyl group is linear or branched, or a C3-C5 cycloalkyl moiety; R3 is H, methoxy, methyl or ethyl; or R2 and R3 together form a bridging moiety —O—CH2—O— between the phenyl carbon atoms to which they are connected; R4 is OH or methoxy; and R5 and R6 are independently H or methyl; R1, R2, R3, R4, R5 and R6 are such that, (i) when R2 and R3 together form a bridging moiety —O—CH2—O— between the phenyl carbon atoms to which they are connected, R1, R5, R6 are H, and R4 is OH; and (ii) when R4 is OH and R1-R3 are H, at least one of R5, R6 is methyl.

Abstract translation: 其中R 1为H，甲基或乙基的式Ⅰ化合物（包括其盐） R2是H，OH，氟，C1-C4直链或支链烷基，其中烷基是直链或支链的C 1 -C 6烷氧基或C 3 -C 5环烷基部分; R3是H，甲氧基，甲基或乙基; 或者R 2和R 3一起在它们连接的苯基碳原子之间形成桥连部分-O-CH 2 -O-; R4是OH或甲氧基; 且R 5和R 6独立地为H或甲基; R 1，R 2，R 3，R 4，R 5和R 6是：（ⅰ）当R 2和R 3在它们连接的苯基碳原子之间一起形成桥连部分-O-CH 2 -O-时，R 1，R 5，R 6 是H，R4是OH; 和（ii）当R 4为OH且R 1 -R 3为H时，R 5，R 6中的至少一个为甲基。

公开(公告)号：US09173394B2

公开(公告)日：2015-11-03

申请号：US12680072

申请日：2008-09-13

Applicant: Heike Hungenberg ,  Peter Jeschke ,  Robert Velten ,  Wolfgang Thielert

Inventor： Heike Hungenberg ,  Peter Jeschke ,  Robert Velten ,  Wolfgang Thielert

IPC: C07D405/00 ,  C07D213/00 ,  C07D211/72 ,  C07D211/84 ,  C07D213/61 ,  A01N43/40

CPC classification number: A01N43/40 ,  A01N37/42 ,  A01N37/52 ,  A01N43/22 ,  A01N43/36 ,  A01N43/56 ,  A01N43/58 ,  A01N43/64 ,  A01N43/68 ,  A01N43/707 ,  A01N43/90 ,  A01N47/02 ,  A01N47/06 ,  A01N47/30 ,  A01N47/34 ,  A01N47/38 ,  A01N2300/00

Abstract: The present invention relates to novel active substance combinations which contain firstly at least one known compound of the formula (I) in which R1 and A have the meanings given in the description, and secondly at least one further known active substance from the class of the macrolides, the carboxylates or other classes, and which are highly suitable for controlling animal pests such as insects and undesired acarids.

Abstract translation: 本发明涉及包含首先至少一种已知的式（I）化合物的新型活性物质组合，其中R1和A具有说明书中给出的含义，其次至少一种另外已知的活性物质类别 大环内酯类，羧酸酯类或其他类，并且它们非常适用于控制动物害虫如昆虫和不需要的螨。

公开(公告)号：US09139551B2

公开(公告)日：2015-09-22

申请号：US14159588

申请日：2014-01-21

Applicant: Xianxing Jiang ,  Dekui Zhang ,  Cheng Jin

Inventor： Xianxing Jiang ,  Dekui Zhang ,  Cheng Jin

IPC: A61K31/445 ,  A61K31/35 ,  C07D401/00 ,  C07D405/00 ,  C07D409/00 ,  C07D411/00 ,  C07D413/00 ,  C07D417/00 ,  C07D419/00 ,  C07D421/00 ,  C07D311/00 ,  C07D311/62

CPC classification number: C07D311/62

Abstract: A new class of high water-soluble compound based upon the Hovenia plant, or its herbal extract form known as DHM, and the methods for synthesizing same, to produce anti-alcohol intoxication treatment to alleviate the symptoms of hangover and other over-drinking, binge-drinking related ailments. Such compounds, known as TDHM and PDHM, can reduce the alcohol concentration in the blood, lengthen the waking time, and shorten the period of drowsiness induced after drinking alcohol; they also are proved to have high water solubility and thus are suitable for immediate protection and treatment to persons with alcohol intoxication or hangover and over-drinking.

Abstract translation: 一种新型的基于禾本科植物的高水溶性化合物或其称为DHM的草药提取物及其合成方法，用于产生抗酒精中毒治疗以缓解宿醉和过度饮酒的症状， 饮酒有关的疾病。 称为TDHM和PDHM的化合物可以降低血液中的酒精浓度，延长醒来时间，并缩短饮酒后诱发的睡意期; 它们也被证明具有高水溶性，因此适用于立即对酒精中毒或宿醉和过度饮酒的人进行保护和治疗。

公开(公告)号：US09029549B2

公开(公告)日：2015-05-12

申请号：US14039806

申请日：2013-09-27

Applicant: Bayer Intellectual Property GmbH

Inventor： Pierre Cristau ,  Stefan Herrmann ,  Nicola Rahn ,  Arnd Voerste ,  Ulrike Wachendorff-Neumann ,  Tomoki Tsuchiya

IPC: C07D405/00 ,  A01N43/78 ,  C07D417/14 ,  A01N43/56

CPC classification number: A01N43/78 ,  A01N43/56 ,  C07D417/04 ,  C07D417/14

Abstract: The use of thiazole-4-carboxylic esters and thioesters of the formula (I) in which R1, R2, R3, R4, R5, R6, R7, Y1, Y2, Y3, W, X and G have the meanings given in the description, and also of agrochemically active salts thereof, as fungicides.

Abstract translation: 使用式（I）的噻唑-4-羧酸酯和硫酯，其中R 1，R 2，R 3，R 4，R 5，R 6，R 7，Y 1，Y 2，Y 3，W，X和G具有 描述，以及其农业化学活性盐，作为杀真菌剂。

公开(公告)号：US09012461B2

公开(公告)日：2015-04-21

申请号：US13543276

申请日：2012-07-06

Applicant: Ian Peter Holmes ,  Ylva Bergman ,  Gillian Elizabeth Lunniss ,  Marica Nikac ,  Neil Choi ,  Catherine Fae Hemley ,  Scott Raymond Walker ,  Richard Charles Foitzik ,  Danny Ganame ,  Romina Lessene

Inventor： Ian Peter Holmes ,  Ylva Bergman ,  Gillian Elizabeth Lunniss ,  Marica Nikac ,  Neil Choi ,  Catherine Fae Hemley ,  Scott Raymond Walker ,  Richard Charles Foitzik ,  Danny Ganame ,  Romina Lessene

IPC: A01N43/54 ,  C07D239/42 ,  C07D401/04 ,  A61K31/497 ,  A61K31/535 ,  C07D403/00 ,  C07D401/00 ,  C07D405/00 ,  C07D409/00 ,  C07D411/00 ,  C07D413/00 ,  C07D417/00 ,  C07D419/00 ,  C07D401/12 ,  C07D401/14 ,  C07D413/12 ,  C07D403/14

CPC classification number: A61K31/506 ,  A61K39/395 ,  A61K39/3955 ,  C07D239/42 ,  C07D401/12 ,  C07D401/14 ,  C07D403/14 ,  C07D413/12

Abstract: A compound of the formula (I): where R1 or R2 is a cyclc amine group and R5 is an aromatic group with a carbonyl containing substituent for use as a FAK inhibitor.

Abstract translation: 式（I）的化合物：其中R 1或R 2为环状胺基，R 5为具有含羰基取代基的芳族基团，用作FAK抑制剂。