公开(公告)号：WO2016184429A1

公开(公告)日：2016-11-24

申请号：PCT/CN2016/082853

申请日：2016-05-20

Applicant: 常州强力先端电子材料有限公司 ,  常州强力电子新材料股份有限公司

Inventor： 钱晓春

IPC: C07D231/06 ,  G03F7/028 ,  G03F7/004 ,  C08F4/00 ,  C08F226/00

CPC classification number: C07D231/06 ,  C08F4/00 ,  C08F226/00 ,  G03F7/004 ,  G03F7/028

Abstract: 一种吡唑啉类增感剂，其制备方法和应用。该吡唑啉类增感剂具有式（I）或式（II）所示的结构，吸收波段在350-440nm之间，适合在光固化体系特别是含有双咪唑类光引发剂的体系中使用，式（I）、式（II）依次为.

公开(公告)号：WO2016091845A1

公开(公告)日：2016-06-16

申请号：PCT/EP2015/078912

申请日：2015-12-08

Applicant: BAYER PHARMA AKTIENGESELLSCHAFT

Inventor： MOWAT, Jeffrey Stuart ,  STELLFELD, Timo ,  STRESEMANN, Carlo ,  HILLIG, Roman ,  KÖHR, Silke ,  STÖCKIGT, Detlef ,  WEISKE, Jörg ,  BRUMBY, Thomas ,  BARACK, Naomi ,  CHRIST, Clara ,  TER LAAK, Antonius ,  BADOCK, Volker ,  CRAMPTON, Rosemary Helen ,  STEFANUTI, Ian

IPC: C07D403/12 ,  C07D231/06 ,  C07D401/12 ,  C07D413/12 ,  A61K31/506 ,  A61P35/00

CPC classification number: C07D231/06 ,  C07D401/12 ,  C07D403/12 ,  C07D413/12

Abstract: The present invention relates to protein-lysine N-methyltransferase SMYD2 (SET and MYND domain-containing protein 2) inhibitors, in particular SMYD2-inhibitory substituted cyanoguanidine-pyrazolines of general formula (I) wherein R 1 , R 2 , R 3 , R 4 , R 5 , X and r have the meaning as described and defined herein, as well as to pharmaceutical compositions comprising compounds according to the invention and to their prophylactic and therapeutic use for hyperproliferative disorders, in particular for cancer, respectively tumour disorders. The present invention furthermore relates to the use of SMYD2 inhibitors for benign hyperplasias, atherosclerotic disorders, sepsis, autoimmune disorders, vascular disorders, viral infections, neurodegenerative disorders, inflammatory disorders, atherosclerotic disorders and the control of male fertility.

Abstract translation: 本发明涉及蛋白质赖氨酸N-甲基转移酶SMYD2（SET和MYND结构域蛋白2）抑制剂，特别是通式（I）的SMYD2抑制性取代的氰基胍 - 吡唑啉，其中R1，R2，R3，R4，R5， X和r具有如本文所述和定义的含义，以及包含根据本发明的化合物的药物组合物及其对过度增殖性疾病，特别是癌症，分别为肿瘤病症的预防和治疗用途。 本发明还涉及SMYD2抑制剂用于良性增生，动脉粥样硬化病症，败血症，自身免疫性疾病，血管病症，病毒感染，神经退行性疾病，炎症性疾病，动脉粥样硬化性疾病和控制男性生殖力的用途。

公开(公告)号：WO2015143535A1

公开(公告)日：2015-10-01

申请号：PCT/CA2015/000171

申请日：2015-03-24

Applicant: VIROCARB INC.

Inventor： LINGWOOD, Clifford ,  HUESCA, Mario ,  DAYAM, Raveendra ,  SINGH, Shamshare

IPC: A61K31/53 ,  A61K31/381 ,  A61K31/4439 ,  A61K31/497 ,  A61K31/505 ,  A61K31/506 ,  A61K31/513 ,  A61P31/18 ,  C07D239/46 ,  C07D253/075 ,  C07D333/24 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C12Q1/70 ,  C40B30/02

CPC classification number: C07D239/46 ,  A61K31/381 ,  A61K31/4439 ,  A61K31/505 ,  A61K31/513 ,  A61K31/53 ,  A61K31/5377 ,  A61K31/635 ,  A61P31/18 ,  C07D231/06 ,  C07D239/47 ,  C07D239/60 ,  C07D253/07 ,  C07D253/075 ,  C07D333/24 ,  C07D333/48 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D405/12 ,  C07D417/14 ,  C12Q1/70 ,  C40B30/02 ,  G01N33/6893 ,  G01N2333/162 ,  G01N2500/02

Abstract: Small molecule inhibitors GP120-mediated HIV infections, methods for identifying the same, and methods and uses employing of these compounds in treatment, inhibition or prevention of HIV infection are provided. The compounds have a structure according to Formula (I), and comprise a pharmacophore functionally corresponding with pharmacophore (I) of Figure 2.

Abstract translation: 提供了小分子抑制剂GP120介导的HIV感染，鉴定其的方法，以及使用这些化合物治疗，抑制或预防HIV感染的方法和用途。 所述化合物具有式（I）的结构，并且包含在功能上对应于图2的药效团（I）的药效团。

公开(公告)号：WO2014114250A1

公开(公告)日：2014-07-31

申请号：PCT/CN2014/071207

申请日：2014-01-23

Applicant: SYNGENTA PARTICIPATIONS AG ,  LU, Long

Inventor： LU, Long ,  CASSAYRE, Jérome Yves ,  BERTHON, Guillaume ,  EL QACEMI, Myriem ,  WU, Yaming

IPC: C07D401/04 ,  C07D401/14 ,  C07D403/04 ,  C07D403/10 ,  C07D403/14 ,  A01N43/56 ,  A01P7/04 ,  A01P7/02 ,  A01P5/00 ,  A01P9/00 ,  C07D231/06

CPC classification number: C07D413/12 ,  A01N43/16 ,  A01N43/56 ,  A01N43/58 ,  A01N43/60 ,  A01N43/78 ,  A01N43/80 ,  A01N43/90 ,  A01N53/00 ,  C07D231/06 ,  C07D409/12

Abstract: The present invention relates to compounds of formula (I) wherein P is selected from P1 and P2, or P and R 5 together are P3 or P is a heterocycle H, selected from H1 to H9 wherein Y 1 , Y 2 and Y 3 are independently of each other C-H, C-R 5 , or nitrogen; and G 1 , G 2 , G 3 ,Z, R 1 , R 2 , R 3 , R 4 , R 5 , R 6a , R 6b , R 7 , R 8 , R 9 , R 10 , R 11 , p, n and k are as defined in the claims. The invention also relates to methods of controlling insects, acarines, nematodes or molluscs which comprises applying to a pest, to a locus of a pest, or to a plant susceptible to attack by a pest an insecticidally, acaricidally, nematicidally or molluscicidally effective amount of a compound of formula (I).

Abstract translation: 本发明涉及式（I）化合物，其中P选自P1和P2，或P和R5一起为P3或P为选自H1至H9的杂环H，其中Y1，Y2和Y3彼此独立地 CH，C-R5或氮; 和G1，G2，G3，Z，R1，R2，R3，R4，R5，R6a，R6b，R7，R8，R9，R10，R11，p，n和k如权利要求中所定义。 本发明还涉及防治昆虫，螨虫，线虫或软体动物的方法，其包括向有害生物的害虫部位或易受害虫攻击的植物施用杀虫，杀螨，杀线虫或软体动物有效量的 式（I）的化合物。

公开(公告)号：WO2014018695A1

公开(公告)日：2014-01-30

申请号：PCT/US2013/051919

申请日：2013-07-25

Applicant: JENRIN DISCOVERY, INC.

Inventor： MCELROY, John ,  CHORVAT, Robert

IPC: A61K31/415 ,  A61K31/351 ,  A61K31/435 ,  C07D231/06

CPC classification number: A61K31/415 ,  A61K45/06 ,  C07D231/06 ,  A61K2300/00

Abstract: The present invention provides novel, diastereomeric pyrazolines that are useful as cannabinoid receptor blockers and pharmaceutical compositions thereof and methods of using the same for treating obesity, diabetes, inflammatory disorders, cardiometabolic disorders, hepatic disorders, and/or cancers.

Abstract translation: 本发明提供了可用作大麻素受体阻滞剂及其药物组合物的新颖的非对映异构吡唑啉，以及用于治疗肥胖症，糖尿病，炎性疾病，心脏代谢紊乱，肝脏疾病和/或癌症的方法。

公开(公告)号：WO2012104331A2

公开(公告)日：2012-08-09

申请号：PCT/EP2012051638

申请日：2012-02-01

Applicant: SYNGENTA PARTICIPATIONS AG ,  SYNGENTA LTD ,  VOCK CHRISTOPH ,  CASSAYRE JEROME YVES ,  EL QACEMI MYRIEM

Inventor： VOCK CHRISTOPH ,  CASSAYRE JÉRÔME YVES ,  EL QACEMI MYRIEM

IPC: C07D413/12

CPC classification number: A01N43/80 ,  C07D231/06 ,  C07D261/04 ,  C07D413/12 ,  A01N2300/00

Abstract: The present invention provides methods comprising applying to a crop of soybean plants, the locus thereof, or propagation material thereof, a compound a compound of formula III wherein wherein A3, A4, A4' and A5' are independently C-H, or nitrogen and wherein #1 indicates the bond to X and #2 indicates the bond to cycle B; cycle B is selected from B1 to B6 wherein #1 indicates the bond to cycle A, #2 indicates the bond to R7 and #3 indicates the bond to cycle C; cycle C is phenyl; R5 is chloro, bromo, CF3 or methyl; R7 is chlorodifluoromethyl or trifluoromethyl; each R8 is independently bromo, chloro, fluoro or trifluoromethyl; p is 2 or 3; and wherein X is defined in the claims. The methods are preferably for the control of stinkbugs, in particular Euschistus.

Abstract translation: 本发明提供了包括向大豆植物作物，其所在地或其繁殖材料施用化合物的方法，其中式III的化合物其中A3，A4，A4'和A5'独立地为CH或氮，并且其中＃ 1表示与X的键，＃2表示与B的键; 循环B选自B1至B6，其中＃1表示与循环A的键，＃2表示与R7的键，以及＃3表示与循环C的键; 循环C是苯基; R5是氯，溴，CF3或甲基; R7是氯二氟甲基或三氟甲基; 每个R 8独立地是溴，氯，氟或三氟甲基; p是2或3; 并且其中X在权利要求中定义。 该方法优选用于控制臭蝽，特别是欧洲香蝽。

公开(公告)号：WO2012068529A2

公开(公告)日：2012-05-24

申请号：PCT/US2011/061508

申请日：2011-11-18

Applicant: JENRIN DISCOVERY ,  MCELROY, John ,  CHORVAT, Robert

Inventor： MCELROY, John ,  CHORVAT, Robert

IPC: A61K31/415 ,  C07D231/06 ,  C07D417/12 ,  A61K31/427 ,  A61P3/04 ,  A61P3/10 ,  A61P3/06 ,  A61P9/00 ,  A61P29/00 ,  A61P1/16 ,  A61P35/00 ,  A61P9/10 ,  A61P9/12 ,  A61P1/00 ,  C07F9/6503 ,  A61K31/683

CPC classification number: C07D231/06 ,  A61K9/0019 ,  A61K9/2018 ,  A61K9/2059 ,  A61K9/4866 ,  C07D403/10 ,  C07D417/12 ,  C07F9/65032

Abstract: The present invention provides novel pyrazolines that are useful as cannabinoid receptor blockers and pharmaceutical compositions thereof and methods of using the same for treating obesity, diabetes, inflammatory disorders, cardiometabolic disorders, hepatic disorders, and/or cancers.

Abstract translation: 本发明提供了可用作大麻素受体阻滞剂及其药物组合物的新的吡唑啉，以及用于治疗肥胖，糖尿病，炎性疾病，心脏代谢紊乱，肝脏疾病和/或癌症的方法。

公开(公告)号：WO2011073444A3

公开(公告)日：2011-09-01

申请号：PCT/EP2010070220

申请日：2010-12-20

Applicant: BASF SE ,  KOERBER KARSTEN ,  KAISER FLORIAN ,  DEYN WOLFGANG VON ,  GROS STEFFEN ,  DESHMUKH PRASHANT ,  DICKHAUT JOACHIM ,  BANDUR NINA GERTRUD ,  NARINE ARUN ,  BEYER CARSTEN ,  CULBERTSON DEBORAH L ,  ANSPAUGH DOUGLAS D ,  BRAUN FRANZ-JOSEF ,  LE VEZOUET RONAN

Inventor： KOERBER KARSTEN ,  KAISER FLORIAN ,  VON DEYN WOLFGANG ,  GROS STEFFEN ,  DESHMUKH PRASHANT ,  DICKHAUT JOACHIM ,  BANDUR NINA GERTRUD ,  NARINE ARUN ,  BEYER CARSTEN ,  CULBERTSON DEBORAH L ,  ANSPAUGH DOUGLAS D ,  BRAUN FRANZ-JOSEF ,  LE VEZOUET RONAN

IPC: C07D231/06 ,  A01N43/80 ,  A01P5/00 ,  A01P7/00 ,  C07D277/10 ,  C07D401/04 ,  C07D403/04 ,  C07D413/04 ,  C07D413/10 ,  C07D413/12 ,  C07D417/04 ,  C07D417/10

CPC classification number: C07D413/04 ,  A01N43/80 ,  C07D231/06 ,  C07D277/10 ,  C07D401/04 ,  C07D403/04 ,  C07D413/10 ,  C07D413/12 ,  C07D417/04 ,  C07D417/10

Abstract: The present invention relates to azoline compounds of formula (I) which are useful for combating or controlling invertebrate pests, in particular arthropod pests and nematodes. The invention also relates to a method for controlling invertebrate pests by using these compounds and to plant propagation material and to an agricultural and a veterinary composition comprising said compounds.

Abstract translation: 本发明涉及用于对抗或控制无脊椎害虫，特别是节肢动物害虫和线虫的式（I）的唑啉化合物。 本发明还涉及通过使用这些化合物和植物繁殖材料以及包含所述化合物的农业和兽用组合物来控制无脊椎害虫的方法。

公开(公告)号：WO2008084057A1

公开(公告)日：2008-07-17

申请号：PCT/EP2008/050181

申请日：2008-01-09

Applicant: SOLVAY PHARMACEUTICALS B.V. ,  LANGE, Josephus, H., M. ,  KRUSE, Cornelis, G.

Inventor： LANGE, Josephus, H., M. ,  KRUSE, Cornelis, G.

IPC: C07D231/06 ,  C07D233/90 ,  C07D403/12 ,  A61K31/4155 ,  A61K31/415 ,  A61K31/4164 ,  A61P25/00

CPC classification number: C07D231/06 ,  C07D231/14 ,  C07D233/90 ,  C07D403/12

Abstract: This invention relates to compounds with a combination of cannabinoid-CB 1 antagonism and serotonin reuptake inhibition to pharmaceutical compositions containing these compounds, to methods for preparing the compounds, methods for preparing novel intermediates useful for their synthesis, and methods for preparing compositions. The invention also relates to the uses of such compounds and compositions, particularly their use in administering them to patients to achieve a therapeutic effect in psychosis, anxiety, depression, attention deficits, cognitive disorders, obesity, drug dependence, Parkinson's disease, Alzheimer's disease, pain disorders, neuropathic pain disorders and sexual disorders. In particular the invention relates to compoundsof the general formula (I): wherein the symbols have the meanings given in the specification.

Abstract translation: 本发明涉及含有这些化合物的药物组合物中的大麻素-CB 1拮抗剂和5-羟色胺再摄取抑制的化合物，制备该化合物的方法，制备用于其合成的新中间体的方法和 制备组合物的方法。 本发明还涉及这些化合物和组合物的用途，特别是它们在给予患者以在精神病，焦虑症，抑郁症，注意力缺陷，认知障碍，肥胖，药物依赖，帕金森病，阿尔茨海默病， 疼痛障碍，神经性疼痛障碍和性功能障碍。 特别地，本发明涉及通式（I）的化合物：其中符号具有说明书中给出的含义。

公开(公告)号：WO2008043544A8

公开(公告)日：2008-06-19

申请号：PCT/EP2007008812

申请日：2007-10-10

Applicant: ESTEVE LABOR DR ,  BUSCHMANN HELMUT H ,  TORRENS-JOVER ANTONIO ,  MAS-PRIO JOSEF ,  YENES-MINGUEZ SUSANA

Inventor： BUSCHMANN HELMUT H ,  TORRENS-JOVER ANTONIO ,  MAS-PRIO JOSEF ,  YENES-MINGUEZ SUSANA

IPC: C07D231/06 ,  A61K31/415 ,  A61P3/04 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12 ,  C07D413/12 ,  C07D417/12 ,  C07D513/04

CPC classification number: C07D231/06 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12 ,  C07D413/12 ,  C07D417/12 ,  C07D513/04

Abstract: The present invention relates to substituted pyrazoline compounds of general formula (I), methods for their preparation, medicaments comprising these compounds as well as their use for the preparation of a medicament for the treatment of humans and animals.

Abstract translation: 本发明涉及通式（I）的取代吡唑啉化合物，其制备方法，包含这些化合物的药物及其制备用于治疗人和动物的药物的用途。