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1. 发明公开

EP3049424A1 ORGANOMETALLIC COMPOUNDS FOR USE AS ANTHELMINTICS 审中-公开
标题翻译：有机金属化合物用作驱虫药
公开(公告)号：EP3049424A1
公开(公告)日：2016-08-03
申请号：EP14776674.5
申请日：2014-09-26
申请人： Universität Zürich , The University of Melbourne
发明人： GASSER, Gilles , GASSER, Robin B. , HESS, Jeannine , JABBAR, Abdul , PATRA, Malay
IPC分类号： C07F13/00 , A01N37/00 , A01N43/00 , C07F17/00 , C07F17/02
CPC分类号： C07F17/02 , A01N31/04 , A01N33/08 , A01N35/04 , A01N35/10 , A01N37/14 , A01N37/40 , A01N37/44 , A01N47/02 , A01N47/48 , A01N55/02 , A01N59/16 , C07F13/00 , C07F15/06 , C07F17/00
摘要： The Invention comprises a compound characterized by a general formula (1), RL—OM-RR (1) wherein OM is an organometallic compound independently selected from the group of an unsubstituted or substituted metal sandwich compound, an unsubstituted or substituted half metal sandwich compound or a metal carbonyl compound, and wherein at least one of RL and RR is selected from and their use for in a method of treatment of disease, in particular their use against helminths.

2. 发明公开

EP3049425A1 BIS-ORGANOMETALLIC 2-AMINO-3-HYDROXY-2-METHYLPROPANENITRILE DERIVATIVES FOR USE AS ANTHELMINTICS 审中-公开
标题翻译：双 - 异喹啉-2-氨基-3-羟基-2-甲基丙烯酰胺酸锌维生素ALS ANTHELMINTIKA
公开(公告)号：EP3049425A1
公开(公告)日：2016-08-03
申请号：EP14781122.8
申请日：2014-09-26
申请人： Universität Zürich , The University of Melbourne
发明人： GASSER, Gilles , GASSER, Robin B. , HESS, Jeannine , JABBAR, Abdul , PATRA, Malay
IPC分类号： C07F17/02 , A01N37/34
CPC分类号： C07F17/02 , A01N55/02
摘要： The invention comprises a compound characterized by a general formula (1), wherein X is a group described by a general formula -K
p -F
l -K
q -, wherein - F
l is -C(=O)-,-C(=S)-,with l being 0 or 1, - K
p is a C
p –alkyl with p being 0, 1, 2, 3 or 4, - K
q is a C
q -alkyl with q being 0, 1, 2, 3 or 4, and wherein Z is a group described by a general formula –K
r -F
i –K
t -, wherein - F
i is -O-, -S-, -O-C(=O)-, -O-C(=S)-, -S-C(=O)- or NH-(C=O)-with i being 0 or 1, - K
r is a C
r -alkyl with r being 0, 1, 2, 3 or 4, - K
t is a C
t -alkyl with t being 0, 1, 2, 3 or 4, wherein each OM is an organometallic compound independently selected from each other from the group of an unsubstituted or substituted metal sandwich compound, an unsubstituted or substituted half metal sandwich compound or a metal carbonyl compound and their use.
摘要翻译：本发明包括由通式（1）表征的化合物。其中X为通式所示的基团，其中l为0或1，为烷基，p为或为具有q为或-4的烷基，Z为由通式表示的基团，其中与 l为0或1，Kr为α-烷基，r为0,1,2,3或4，Kt为α-烷基，t为0,1,2,3或4，其中每个OM独立地为有机金属化合物从未取代或取代的金属夹心化合物，未取代或取代的半金属夹心化合物或羰基金属化合物的组中选择，以及它们的用途。

3. 发明公开

EP3048889A1 ORGANOMETALLIC N-2-CYANO-1-HYDROXYPROPAN-2-YL FOR USE AS ANTHELMINTICS 审中-公开
标题翻译：有机物分子N-2-氰基-1-羟基丙酸酯2-YL ZUR VERWENDUNG ALS ANTHELMINTIKUM
公开(公告)号：EP3048889A1
公开(公告)日：2016-08-03
申请号：EP14777572.0
申请日：2014-09-26
申请人： Universität Zürich , The University of Melbourne
发明人： GASSER, Gilles , GASSER, Robin B. , HESS, Jeannine , JABBAR, Abdul , PATRA, Malay
IPC分类号： A01N55/02 , C07F15/00 , C07F15/02 , A61K31/28 , A61K31/295
CPC分类号： C07F17/02 , A01N55/00 , C07F17/00
摘要： The invention relates to a compound characterized by a general formula (1), wherein OM is an organometallic compound independently selected from the group of an unsubstituted or substituted metal sandwich compound, an unsubstituted or substituted half metal sandwich compound or a metal carbonyl compound, wherein Z is a group described by a general formula –K
r -F
i –K
t -, wherein -F
i is -O-, -S-, -O-C(=O)-, -O-C(=S)-, -S-C(=O)- or NH-(C=O)- with i being 0 or 1, -K
r is a C
r -alkyl with r being 0, 1, 2, 3 or 4, -K
t is a C
t -alkyl with t being 0, 1, 2, 3 or 4, and wherein each R
X1 independently from any other R
X1 is -C(=O)OR
X2 , -C(=O)NR
X2
2 , -C(=O)SR
X2 , -C(=S)OR
X2 , -C(NH)NR
X2
2 , CN
4 H
2 , -NR
X2
2 ,-C(=O)R
X2 , -C(=S)R
X2 , -OR
X2 , -SR
X2 , -CF
3 ,-OCF
3 , -SCF
3 , -SOCF
3 , -SO
2 CF
3 ,-CN, -NO
2 , -F, -Cl, -Br or -I, and wherein - n of R
X1
n is 0, 1, 2, 3, 4 or 5, and with each R
X2 independently from any other R
X2 being hydrogen or an unsubstituted or substituted C
1 -C
4 alkyl and their use in a method for treatment of infections by helminths.
摘要翻译：本发明涉及以通式表示的化合物，其中OM是独立地选自未取代或取代的金属夹心化合物，未取代或取代的半金属夹心化合物或金属羰基化合物的有机金属化合物，其中Z是基团，其通式如下：其中i是或为具有r的烷基，或者是具有t的烷基，或者其中每个RX 1独立地为任何其它基团，或者其中各个独立地为另一个是氢或未取代或取代的烷基，以及它们在用于治疗蠕虫感染的方法中的用途。

4. 发明公开

EP3016962A1 ORGANOMETALLIC 2-CYANO-2-AMINOBENZOATE-PROPYL DERIVATES AND THEIR USE AS ANTHELMINTICS 有权
标题翻译： ORGANOMETALLISCHE 2-CYANO-2-AMINOBENZOAT-PROPLL-DERIVATE UND DEREN VERWENDUNG ALS ANTHELMINTIKA
公开(公告)号：EP3016962A1
公开(公告)日：2016-05-11
申请号：EP14742159.8
申请日：2014-07-01
申请人： Universität Zürich , The University of Melbourne
发明人： HESS, Jeannine , PATRA, Malay , GASSER, Gilles , JABBAR, Abdul , GASSER, Robin B.
IPC分类号： C07F17/02 , A01N37/34 , C07F13/00 , C07F15/06
CPC分类号： C07F15/02 , A01N55/02 , C07F13/00 , C07F15/0046 , C07F15/06 , C07F17/02
摘要： The invention relates to compounds characterized by a general formula (1), wherein X is a group described by a general formula -K p -F l - K q -, wherein - F l is -C(=O)-,-C(=S)-, with I being 0 or 1, - K p is a C p -alkyl with p being 0, 1, 2, 3 or 4, - Kq is a C q -alkyl with q being 0, 1, 2, 3 or 4, and wherein n of R 1 n is 0, 1, 2, 3, 4 or 5, and each R 1 independently from any other R 1 is -C(=O)OR 2 , -C(=O)NR 2 2 , -C(=O)SR 2 , -C(=S)OR 2 , -C(NH)NR 2 2 , CN 4 H 2 , -NR 2 2 , -C(=O)R 2 , -C(=S)R 2 , -OR 2 , -SR 2 , -CF 3 , -OCF 3 , -SCF 3 , -SOCF 3 , -SO 2 CF 3 , -CN, -NO 2 , -F, -Cl, -Br or -I, with each R 2 independently from any other R 2 being a hydrogen or C 1 -C 4 alkyl, and wherein OM is an organometallic compound independently selected from the group of an unsubstituted or substituted metal sandwich compound, an unsubstituted or substituted half metal sandwich compound or a metal carbonyl compound and their use in a method for treatment of infections by helminths.
摘要翻译：本发明涉及以通式（1）为特征的化合物，其中X为通式-K p -F 1 -K q - 所述基团，其中-F 1为-C（= O） - ， - C （= S） - ，其中I为0或1，-K p为C为P的烷基，p为0,1,2,3或4， - Kq为C q - 烷基，q为0,1或2， 2，3或4，并且其中R 1 n的n为0,1,2,3,4或5，并且每个R 1独立地为任何其它R 1为-C（= O）OR 2，-C（= O）NR 2 2，-C（= O）SR 2，-C（= S）OR 2，-C（NH）NR 2 2，CN 4 H 2，-NR 2 2，-C（= O）R 2，-C（= S）R 2，-OR 2，-SR 2，-CF 3，-OCF 3，-SCF 3，-SOCF 3，-SO 2 CF 3，-CN，-NO 2，-F ，-Cl，-Br或-I，其中每个R 2独立地为任何其它R 2为氢或C 1 -C 4烷基，并且其中OM为独立地选自未取代或取代的金属三明治组的有机金属化合物化合物，未取代或取代的半金属夹心化合物或金属羰基化合物，以及它们在蠕虫感染治疗方法中的用途。

5. 发明授权

EP3016962B1 ORGANOMETALLIC 2-CYANO-2-AMINOBENZOATE-PROPYL DERIVATES AND THEIR USE AS ANTHELMINTICS 有权
标题翻译：有机金属2-氰基-2-氨基苯甲酸酯 - 丙基衍生物及其作为甾体化合物的用途
公开(公告)号：EP3016962B1
公开(公告)日：2018-02-28
申请号：EP14742159.8
申请日：2014-07-01
申请人： Universität Zürich , The University Of Melbourne
发明人： HESS, Jeannine , PATRA, Malay , GASSER, Gilles , JABBAR, Abdul , GASSER, Robin B.
IPC分类号： C07F17/02 , A01N37/34 , C07F13/00 , C07F15/06
CPC分类号： C07F15/02 , A01N55/02 , C07F13/00 , C07F15/0046 , C07F15/06 , C07F17/02
摘要： The invention relates to compounds characterized by a general formula (1), wherein X is a group described by a general formula -K p -F l - K q -, wherein - F l is -C(=O)-,-C(=S)-, with I being 0 or 1, - K p is a C p -alkyl with p being 0, 1, 2, 3 or 4, - Kq is a C q -alkyl with q being 0, 1, 2, 3 or 4, and wherein n of R 1 n is 0, 1, 2, 3, 4 or 5, and each R 1 independently from any other R 1 is -C(=O)OR 2 , -C(=O)NR 2 2 , -C(=O)SR 2 , -C(=S)OR 2 , -C(NH)NR 2 2 , CN 4 H 2 , -NR 2 2 , -C(=O)R 2 , -C(=S)R 2 , -OR 2 , -SR 2 , -CF 3 , -OCF 3 , -SCF 3 , -SOCF 3 , -SO 2 CF 3 , -CN, -NO 2 , -F, -Cl, -Br or -I, with each R 2 independently from any other R 2 being a hydrogen or C 1 -C 4 alkyl, and wherein OM is an organometallic compound independently selected from the group of an unsubstituted or substituted metal sandwich compound, an unsubstituted or substituted half metal sandwich compound or a metal carbonyl compound and their use in a method for treatment of infections by helminths.

6. 发明公开

EP3016514A1 N-(1-CYANO-2-HYDROXY-1-METHYL-ETHYL)-4-(TRIFLUOROMETHYLSULFANYL)BENZAMIDE DERIVATIVES FOR USE AS NEMATOCIDAL DRUGS 审中-公开
标题翻译： N-（1-氰基-2-羟基-1-甲基 - 乙基）-4-（三氟甲基磺酰基）苯甲酰胺衍生物维尔维翁
公开(公告)号：EP3016514A1
公开(公告)日：2016-05-11
申请号：EP14742160.6
申请日：2014-07-01
申请人： Universität Zürich , The University of Melbourne
发明人： ANSELL, Brendan Robert , GASSER, Gilles , GASSER, Robin B. , JABBAR, Abdul , PATRA, Malay , HESS, Jeannine
IPC分类号： A01N37/34 , A61K31/275 , C07C381/00 , A61P33/10
CPC分类号： C07C323/62 , A01N37/34 , A01N41/10 , A61K31/381 , A61K31/40 , A61K31/42 , A61K31/426 , A61K31/4965 , A61K31/505 , C07B2200/07 , C07C255/29 , C07C317/44
摘要： The invention relates to compounds characterized by a general formula (1), wherein T is S, SO or SO
2 , and R is hydrogen or CO-R' wherein R' is unsubstituted or substituted alkyl, alkenyl, alkynyl, aryl, heteroaryl, use in a method for treatment of infections by helminths.
摘要翻译：本发明涉及以通式（1）表示的化合物，其中T为S，SO或SO 2，R为氢或CO-R'，其中R'为未取代或取代的烷基，烯基，炔基，芳基，杂芳基，使用在用于治疗蠕虫感染的方法中。

7. 发明公开

EP3301100A1 ORGANOMETALLIC FLUCONAZOLE DERIVATES AND THEIR USE AS ANTIMYCOTICS 审中-公开
标题翻译：有机金属氟胞嘧啶衍生物及其作为抗氧化剂的用途
公开(公告)号：EP3301100A1
公开(公告)日：2018-04-04
申请号：EP16191930.3
申请日：2016-09-30
申请人： Universität Zürich
发明人： MASTROBUONI, Luclano , GASSER, Gilles , RUBBLANI, Riccardo , HESS, Jeannine
IPC分类号： C07F17/02 , A61P33/00 , A61K31/295 , A01N37/00
CPC分类号： C07F17/02 , A01N43/653 , A01N55/02
摘要： The invention relates to compounds characterized by a general formula (1),

wherein OM is an organometallic compound. OM is independently selected from the group of an unsubstituted or substituted metal sandwich compound, an unsubstituted or substituted half metal sandwich compound or a metal carbonyl compound.
摘要翻译：本发明涉及由通式（1）表征的化合物，其中OM是有机金属化合物。 OM独立地选自未取代或取代的金属夹心化合物，未取代或取代的半金属夹心化合物或金属羰基化合物。

8. 发明授权

EP3131585B1 MULTIDENTATE BIFUNCTIONAL CHELATING AGENTS FOR RADIONUCLIDE COMPLEXATION IN DIAGNOSTICS AND THERAPY 有权
公开(公告)号：EP3131585B1
公开(公告)日：2020-07-15
申请号：EP15710778.0
申请日：2015-03-18
申请人： Universität Zürich , Universitätsspital Basel
发明人： PATRA, Malay , GASSER, Gilles , MINDT, Thomas, L. , BAUMAN, Andreas
IPC分类号： A61K47/50 , A61K51/08 , C07K7/00 , C07K7/06 , A61P35/00

9. 发明公开

EP3131585A1 MULTIDENTATE BIFUNCTIONAL CHELATING AGENTS FOR RADIONUCLIDE COMPLEXATION IN DIAGNOSTICS AND THERAPY 有权
标题翻译： MEHRZAHNIGE BIFUNKTIONELLE CHELATOREN ZUR KOMPLEXIERUNG VON RADIONUKLIDEN IN DIAGNOSTIK UND THERAPIE
公开(公告)号：EP3131585A1
公开(公告)日：2017-02-22
申请号：EP15710778.0
申请日：2015-03-18
申请人： Universität Zürich , Universitätsspital Basel
发明人： PATRA, Malay , GASSER, Gilles , MINDT, Thomas, L. , BAUMAN, Andreas
IPC分类号： A61K47/50 , A61K51/08 , C07K7/00 , C07K7/06 , A61P35/00
摘要： The invention relates to octadentate ligands of a general formula R1-D-X-D-X-D-X-D-E-R2, wherein D is C(O)N(OH) or N(OH)C(O), pyrimidinone or pyridinone, each X independently of any other X is a saturated or partially unsaturated, substituted or unsubstituted linker comprising 8-11 atoms selected from any of N, C, O; R1 is alkyl, cycloalkyl, arene, or heteroarene, E is a saturated or partially unsaturated, substituted or unsubstituted chain comprising 1-50 atoms and R2 is a moiety capable of selectively binding to a biomolecule, or a nanoparticle. The invention further relates to complexes of the ligand, particularly radionuclides and their use in radioimmunotherapy and imaging.
摘要翻译：本发明涉及通式为R1-DXDXDXDE-R2的八齿配位体，其中D为C（O）N（OH）或N（OH）C（O），嘧啶酮或吡啶酮，每个X独立地为任何其它X为饱和或部分不饱和的取代或未取代的连接体，其包含选自N，C，O中的任何一种的8-11个原子; R1是烷基，环烷基，芳烃或杂芳烃，E是包含1-50个原子的饱和或部分不饱和的取代或未取代的链，R2是能够选择性结合生物分子或纳米颗粒的部分。本发明还涉及配体的复合物，特别是放射性核素及其在放射免疫治疗和成像中的用途。

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