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1. 发明公开

EP2805951A3 Inhibitors of diacylglycerol o-acyltransferase 1 (DGAT-1) and uses thereof 有权转让
标题翻译：二酰基甘油O-酰基转移酶1抑制剂（DGAT-1）和其用途
公开(公告)号：EP2805951A3
公开(公告)日：2015-04-29
申请号：EP14172611.7
申请日：2010-03-19
申请人： Metabasis Therapeutics, Inc.
发明人： Reddy, K. Raja , Stebbins, Jeff , Boyer, Serge, H. , Erion, Mark, D. , Hecker, Scott, J. , Raffaele, Nicholas, Brian , Bookser, Brett, C. , Reddy, Mali, Venkat
IPC分类号： C07D473/16 , C07D473/34 , C07D473/40 , C07F9/30 , C07F9/32 , C07F9/653 , C07F9/6561 , C07F9/6574 , A61K31/52 , A61K31/662 , A61K31/665 , A61K31/675 , A61P3/10 , A61P3/04 , A61K45/06
CPC分类号： A61K31/675 , A61K31/52 , A61K31/542 , A61K31/662 , A61K31/665 , A61K31/683 , A61K31/688 , A61K45/06 , A61P3/04 , A61P3/10 , C07D473/16 , C07D473/34 , C07D473/40 , C07F9/303 , C07F9/3229 , C07F9/40 , C07F9/48 , C07F9/65312 , C07F9/6552 , C07F9/6561 , C07F9/65616 , C07F9/65742 , A61K2300/00
摘要： The invention pertains to use of DGAT-1 inhibitors to treat and/or prevent overweight, obesity and various diseases and disorders associated therewith. Other conditions also can be ameliorated or avoided, such as high postprandial triglycerides or diet-related hypertriglyceridemia, cardiovascular risk associated with excessive triglycerides, and insulin resistance/glucose intolerance in overweight patients, those with diabetes or other glucose metabolic disorders such as Syndrome X and/or polycystic ovary disease. Compounds and compositions suitable for use in the disclosed methods are also provided.

2. 发明授权

EP0016383B1 Oxadiazolylmethylthiolphosphate, Verfahren zu ihrer Herstellung und ihre Verwendung zur Bekämpfung von Schädlingen 失效
标题翻译：氧化二甲基苯乙醇磷酸盐，其生产方法及其在组合中的应用
公开(公告)号：EP0016383B1
公开(公告)日：1982-05-26
申请号：EP80101165.1
申请日：1980-03-07
申请人： BASF Aktiengesellschaft
发明人： Theobald, Hans, Dr. , Adolphi, Heinrich, Dr. , Kiehs, Karl, Dr.
IPC分类号： C07F9/65 , A01N57/16
CPC分类号： C07F9/65312 , A01N57/08

3. 发明授权

EP2858650B1 NEPRILYSIN INHIBITORS 有权
公开(公告)号：EP2858650B1
公开(公告)日：2018-11-14
申请号：EP13733129.4
申请日：2013-06-06
申请人： Theravance Biopharma R&D IP, LLC
发明人： HUGHES, Adam , FLEURY, Melissa
IPC分类号： A61K45/06 , C07F9/653 , C07D405/12 , C07D413/12 , C07D249/12 , C07D257/04 , C07D249/04 , C07D231/14 , C07D261/18 , C07D277/56
CPC分类号： C07F9/653 , A61K31/41 , A61K31/415 , A61K31/4192 , A61K31/4196 , A61K31/42 , A61K31/426 , A61K31/5377 , A61K31/675 , A61K45/06 , C07D231/14 , C07D249/04 , C07D249/12 , C07D257/04 , C07D261/18 , C07D277/56 , C07D319/06 , C07D405/12 , C07D413/12 , C07F9/65312
摘要： In one aspect, the invention relates to compounds having the formula X: where Ra, Rb, R2, R7, and X are as defined in the specification, or a pharmaceutically acceptable salt thereof. The compounds described herein are prodrugs of compounds having neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising these compounds; methods of using these compounds; and processes and intermediates for preparing these compounds.

4. 发明公开

EP2858650A1 NEPRILYSIN INHIBITORS 有权
标题翻译：脑啡肽酶抑制剂
公开(公告)号：EP2858650A1
公开(公告)日：2015-04-15
申请号：EP13733129.4
申请日：2013-06-06
申请人： Theravance Biopharma R&D IP, LLC
发明人： HUGHES, Adam , FLEURY, Melissa
IPC分类号： A61K31/497 , C07D319/06 , C07D249/04 , C07D231/14
CPC分类号： C07F9/653 , A61K31/41 , A61K31/415 , A61K31/4192 , A61K31/4196 , A61K31/42 , A61K31/426 , A61K31/5377 , A61K31/675 , A61K45/06 , C07D231/14 , C07D249/04 , C07D249/12 , C07D257/04 , C07D261/18 , C07D277/56 , C07D319/06 , C07D405/12 , C07D413/12 , C07F9/65312
摘要： In one aspect, the invention relates to compounds having the formula X: where Ra, Rb, R2, R7, and X are as defined in the specification, or a pharmaceutically acceptable salt thereof. The compounds described herein are prodrugs of compounds having neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising these compounds; methods of using these compounds; and processes and intermediates for preparing these compounds.

5. 发明公开

EP2594571A1 Kupfer-Komplexe für optoelektronische Anwendungen 审中-公开
标题翻译： Kupfer-Komplexefüroptoelektronische Anwendungen
公开(公告)号：EP2594571A1
公开(公告)日：2013-05-22
申请号：EP11195010.1
申请日：2011-12-21
申请人： Cynora GmbH
发明人： Die Erfindernennung liegt noch nicht vor
IPC分类号： C07F1/08 , H01L51/00
CPC分类号： H01L51/0091 , C07F1/08 , C07F9/5022 , C07F9/5027 , C07F9/5045 , C07F9/65066 , C07F9/65068 , C07F9/65186 , C07F9/65312 , C07F9/6539 , C09K11/06 , C09K2211/1033 , C09K2211/1037 , C09K2211/1044 , C09K2211/1048 , C09K2211/1051 , C09K2211/1059 , C09K2211/188 , H01L51/009 , H01L51/0508 , H01L51/42 , H01L51/5012 , H01L51/5016 , H01L51/56 , Y02E10/549 , Y02P70/521
摘要： Die Erfindung betrifft Kupfer(I)komplexe der Formel

mit

X* = Cl, Br, I, CN, OCN, SCN, Alkinyl und/oder N 3 (unabhängig voneinander),
N*∩E = ein zweibindiger Ligand mit
E = Phosphanyl/Arsenyl/Antimonyl-Rest der Form R 2 E (mit R = Alkyl, Aryl, Alkoxyl, Phenoxyl, oder Amid);
N* = Imin-Funktion, die Bestandteil einer aromatische Gruppe ist, die ausgewählt ist aus Pyridyl, Pyrimidyl, Pyridazinyl, Triazinyl, Oxazolyl, Thiazolyl, Imidazolyl, Pyrazol, Isoxazol, Isothiazol, 1,2,4-Triazole, 1,2,4-Oxadiazole, 1,2,4-Thiadiazole, Tetrazole, 1,2,3,4-Oxatriazole und/oder 1,2,3,4-Thiatriazole, etc.,
"∩" = mindestens ein Kohlenstoffatom, das ebenfalls Bestandteil der aromatischen Gruppe ist, wobei sich das Kohlenstoffatom sowohl direkt benachbart zum Imin-Stickstoffatom als auch zum Phosphor-, Arsen- oder Antimonatom befindet,
L = entweder ein einzähniger Liganden DR 3 mit
D = Phosphanyl/Arsenyl/Antimonyl-Rest der Form R 3 D (mit R = Alkyl, Aryl, Alkoxyl, Phenoxyl, oder Amid), oder ein zweizähniger Liganden R 2 D-B-DR 2 mit
D = Phosphanyl/Arsenyl/Antimonyl-Rest der Form R 2 D (mit R = Alkyl, Aryl, Alkoxyl, Phenoxyl, oder Amid), der über eine Brücke B mit einem weiteren Rest D verbunden ist, wobei die Brücke B eine Alkylen- oder Arylen-Gruppe oder eine Kombination beider, oder -O-, -NR- oder -SiR 2 - ist,
sowie ihre Verwendung in optoelektronischen Bauelementen, insbesondere in OLEDs.
摘要翻译：铜（I）配合物（I）是新的。式（I）的铜（I）络合物是新的。 X：Cl，Br，I，CN，OCN，SCN，炔基和/或N 3; T1：式（N1T2E）（II）的双齿配体（任选被至少一个基团Z1取代）; E：（R）2E型的磷烷基，胂基或锑基; R：烷基，芳基，烷氧基，苯氧基或酰胺; N1：亚胺，其为芳族基团的组分，优选吡啶基，嘧啶基，哒嗪基，三嗪基，恶唑基，噻唑基，咪唑基，吡唑基，异恶唑基，异噻唑基，1,2,4-三唑基，1,2,4-恶二唑基， 2,4,4-噻二唑基，四唑基，1,2,3,4-氧杂三唑基和/或1,2,3,4-噻二唑基; T2：至少一个C是芳族基团的成分，其中C与亚胺N和P，As或Sb直接相邻; L：D1（R）3或（R）2D2-B1-D2（R）2（任选被至少一个基团Z1取代）; D1：（R）3D1的磷烷基，胂基或锑基; D2：通过桥B1与其他基团D2结合的（R）2D2型的磷烷基，二烷基或脒基; B1：亚烷基和/或亚芳基或-O-，-NR-或-Si（R）2-; 和用于增加载流子迁移和/或增加（I）在有机溶剂中的溶解度的Z1：基团。还包括：（1）准备（I）; （2）在光电子部件中使用（I）作为发射极或吸收体; （3）包含（I）的光电子部件; （4）制造光电子部件，包括使用（I）; 和（5）修改电子部件的发射和/或吸收特性，包括将（I）引入用于在光电子部件中传导电子和空穴的基质材料。 [图片]。

6. 发明授权

EP2688885B1 N-(1,3,4-OXADIAZOL-2-YL)ARYLCARBONSÄUREAMIDE UND IHRE VERWENDUNG ALS HERBIZIDE 有权转让
标题翻译： N-（1,3,4-恶二唑-2-基）芳基和它们作为除草剂
公开(公告)号：EP2688885B1
公开(公告)日：2016-06-01
申请号：EP12710708.4
申请日：2012-03-21
申请人： Bayer Intellectual Property GmbH
发明人： KÖHN, Arnim , AHRENS, Hartmut , BRAUN, Ralf , DÖRNER-RIEPING, Simon , LEHR, Stefan , HEINEMANN, Ines , HÄUSER-HAHN, Isolde , GATZWEILER, Elmar , ROSINGER, Christoper, Hugh
IPC分类号： C07D413/04 , C07D413/12 , C07D413/14 , C07D271/07 , A01N43/824 , C07F9/40 , A01P13/00
CPC分类号： A01N43/82 , C07D271/07 , C07D271/113 , C07D413/04 , C07D413/12 , C07D413/14 , C07F9/65312

7. 发明公开

EP2758059A4 SUBSTITUTED PYRIMIDINES 审中-公开
标题翻译：替代吡嗪
公开(公告)号：EP2758059A4
公开(公告)日：2015-07-22
申请号：EP12834521
申请日：2012-09-19
申请人： MERCK SHARP & DOHME
发明人： DANG QUN , ZHOU CHANGYOU , ZOU WUXIN , HUA YUXIA
IPC分类号： A61K31/50 , A01N43/54 , A61K31/4965
CPC分类号： C07F9/65583 , A61K31/505 , C07D413/14 , C07F9/65037 , C07F9/65217 , C07F9/65312
摘要： The present invention relates to substituted pyrimidines useful as HIF prolyl hydroxylase inhibitors to treat anemia and like conditions.
摘要翻译：本发明涉及可用作HIF脯氨酰羟化酶抑制剂治疗贫血和类似病症的取代嘧啶。

8. 发明公开

EP2805951A2 Inhibitors of diacylglycerol o-acyltransferase 1 (DGAT-1) and uses thereof 有权转让
标题翻译：抑制剂二酰基甘油-O-酰基转移酶1（DGAT-1）和Verwendungen davon
公开(公告)号：EP2805951A2
公开(公告)日：2014-11-26
申请号：EP14172611.7
申请日：2010-03-19
申请人： Metabasis Therapeutics, Inc.
发明人： Reddy, K. Raja , Stebbins, Jeff , Boyer, Serge, H. , Erion, Mark, D. , Hecker, Scott, J. , Raffaele, Nicholas, Brian , Bookser, Brett, C. , Reddy, Mali, Venkat
IPC分类号： C07D473/16 , C07D473/34 , C07D473/40 , C07F9/30 , C07F9/32 , C07F9/653 , C07F9/6561 , C07F9/6574 , A61K31/52 , A61K31/662 , A61K31/665 , A61K31/675 , A61P3/10 , A61P3/04 , A61K45/06
CPC分类号： A61K31/675 , A61K31/52 , A61K31/542 , A61K31/662 , A61K31/665 , A61K31/683 , A61K31/688 , A61K45/06 , A61P3/04 , A61P3/10 , C07D473/16 , C07D473/34 , C07D473/40 , C07F9/303 , C07F9/3229 , C07F9/40 , C07F9/48 , C07F9/65312 , C07F9/6552 , C07F9/6561 , C07F9/65616 , C07F9/65742 , A61K2300/00
摘要： The invention pertains to use of DGAT-1 inhibitors to treat and/or prevent overweight, obesity and various diseases and disorders associated therewith. Other conditions also can be ameliorated or avoided, such as high postprandial triglycerides or diet-related hypertriglyceridemia, cardiovascular risk associated with excessive triglycerides, and insulin resistance/glucose intolerance in overweight patients, those with diabetes or other glucose metabolic disorders such as Syndrome X and/or polycystic ovary disease. Compounds and compositions suitable for use in the disclosed methods are also provided.
摘要翻译：本发明涉及使用DGAT-1抑制剂治疗和/或预防超重，肥胖以及与之相关的各种疾病和病症。其他条件也可以被改善或避免，如高餐后甘油三酸酯或饮食相关的高甘油三酯血症，与过量甘油三酯相关的心血管风险，以及超重患者，糖尿病患者或其他葡萄糖代谢紊乱如X综合症患者和胰岛素抵抗/葡萄糖不耐受 /或多囊卵巢疾病。还提供适用于所公开方法的化合物和组合物。

9. 发明公开

EP1981837A2 METHODS AND COMPOSITIONS FOR MODULATING SPHINGOSINE-1-PHOSPHATE (S1P) RECEPTOR ACTIVITY 审中-公开
标题翻译：方法和组合物控制调节鞘氨醇-1-磷酸受体活性
公开(公告)号：EP1981837A2
公开(公告)日：2008-10-22
申请号：EP07763628.0
申请日：2007-01-30
申请人： Praecis Pharmaceuticals Incorporated
发明人： DENG, Hongfeng , EVINDAR, Ghotas , KAVARANA, Malcolm, J. , MORGAN, Barry , SAHA, Ashis, K. , SATZ, Alexander, L.
IPC分类号： C07C235/00 , C07D231/12 , C07D233/54 , C07D239/26 , C07D249/06 , C07D261/08 , C07D263/32 , C07D271/10 , C07D277/28 , C07D285/12 , C07D307/42 , C07D317/58 , C07D317/64 , C07D471/04 , C07F9/00
CPC分类号： C07F9/65062 , C07B2200/07 , C07C237/04 , C07C237/42 , C07C255/60 , C07C271/22 , C07C317/40 , C07C323/41 , C07C2601/14 , C07D207/12 , C07D209/88 , C07D213/30 , C07D231/12 , C07D233/54 , C07D233/64 , C07D239/26 , C07D249/06 , C07D261/08 , C07D263/32 , C07D271/10 , C07D277/28 , C07D285/12 , C07D307/42 , C07D317/58 , C07D317/64 , C07D333/16 , C07D417/10 , C07D471/04 , C07F9/091 , C07F9/65033 , C07F9/65037 , C07F9/65122 , C07F9/65181 , C07F9/65182 , C07F9/653 , C07F9/65312 , C07F9/6539 , C07F9/65395 , C07F9/65517 , C07F9/6561
摘要： The present invention relates to compounds which modulate the activity of the SlPl receptor, the use of these compounds for treating conditions associated with signaling through the SlPl receptor, and pharmaceutical compositions comprising these compounds.

10. 发明公开

EP0156638A2 Substituted oxadiazole-phosphate pesticide 失效
标题翻译：替补二唑磷农药。
公开(公告)号：EP0156638A2
公开(公告)日：1985-10-02
申请号：EP85302034.5
申请日：1985-03-25
申请人： UNIROYAL, INC.
发明人： Plant, Howard L. , Regis, Richard R. , Moore, Richard C.
IPC分类号： C07F9/65 , C07D271/10 , C07D261/06 , A01N57/16
CPC分类号： C07D271/10 , A01N57/16 , C07D413/04 , C07F9/65312
摘要： A compound of the formula
wherein R is allyl, halocyclopropyl, C 3 -C 5 -alkoxycarbonylmethyl, CrCg aralkyl, styryl, phenyl, naphthyl, furanyl, pyridyl, thienyl, phenyl substituted with halogen, C 1 -C 4 alkyl, trihalomethyl, C 1 -C 4 alkoxy, trihalomethoxy, trihalomethylthio, C 1 -C 4 alkylthio, phenyl, phenoxy, cyano or nitro or C 7 -C 9 aralkyl substituted with halogen, C 1 -C 4 alkyl, trihalomethyl, C 1 -C 4 alkoxy, trihalomethoxy, trihalomethylthio, C 1 -C 4 alkylthio, phenyl, phenoxy, cyano or nitro; R is hydrogen, C 1 -C 3 alkyl, C 7 -C 9 aralkyl, phenyl , C 7 -C 9 aralkyl substituted with halogen, C 1 -C 4 alkyl, trihalomethyl, C 1 -C 4 alkoxy, trihalomethoxy, trihalomethylthio, C 1 -C 4 alkylthio, phenyl, phenoxy, cyano or nitro or phenyl substituted with halogen, C,-C, alkyl, trihalomethyl, C 1 -C 4 alkoxy, trihalomethoxy, trihalomethylthio, C,-C 4 alkylthio, phenyl phenoxy, cyano or nitro, however, if R is substituted phenyl or substituted C 7 -C 9 aralkyl. then R' cannot be hydrogen; R 2 is C 1 -C 4 alkyl, however, if R or R' is 4-chlorophenyl, R 2 cannot be isopropyl; and X, Y and Z are the same or different and are oxygen or sulfur, is disclosed. A method is provided for protection against pests by employing a pesticidally effective amount of the compound above. A composition comprising the compound above and an inert carrier therefor, for pesticidal use, is also taught.
The disclosure also recites a compound of the formula
where R and R' have the meanings of the first mentioned compound. The compound, effective as an intermediate in .the synthesis of the above compound, is produced by the reaction of a compound of the formula
where R has the meanings given above with a compound of the formula
where R' has the meanings given above.

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