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1. 发明申请

WO2004056780A3 TETRAHYDROQUINOLINE DERIVATIVES 审中-公开
标题翻译：四氢喹啉衍生物
公开(公告)号：WO2004056780A3
公开(公告)日：2004-08-05
申请号：PCT/EP0351025
申请日：2003-12-16
申请人： AKZO NOBEL NV , TIMMERS CORNELIS MARIUS , KARSTENS WILLEM FREDERIK JOHAN
发明人： TIMMERS CORNELIS MARIUS , KARSTENS WILLEM FREDERIK JOHAN
IPC分类号： A61K31/47 , A61P5/08 , C07D215/38 , C07D401/12 , C07D405/12 , C07D409/12 , C07D409/14 , C07D413/12
CPC分类号： C07D215/38 , C07D215/44 , C07D401/12 , C07D405/12 , C07D409/12 , C07D409/14 , C07D413/12
摘要： The present invention relates to tetrahydroquinoline derivatives having general formula (I) or a pharmaceutically acceptable salt thereof, wherein R and R are H or Me; R is H, hydroxy, (1-4C)alkoxy, (di)(1-4C)alkylamino(2-4C)alkoxy or (2-6)heterocycloakl(2-4C)alkoxy; R is H, OH, (1-4C)alkoxy or R ; R is H, OH, (1-4C)alkoxy or R ,with the proviso that if R is H, R is not H, OH or (1-4C)alkoxy and that if R is H, R is not H, OH or (1-4C)alkoxy; R is (2-5C)heteroaryl, (6C)aryl, (3-8C)cycloalkyl, (2 6C)heterocycloalkyl or (1-6C)alkyl; R is amino, (di)(1-4C) alkylamino, (6C)arylcarbonylamino, (6C)arylcarbonyloxy, (2-5C) heteroarylcarbonylamino, (2-5C)heteroarylcarbonyloxy, R -(2-4C)alkylamino, R -(2-4C)alkoxy, R -methylamino or R -methoxy; R is hydroxy, amino, (1-4C)alkoxy, (di)(1-4C)alkylamino, (2-6C)heterocycloalkyl, (2-6C) heterocycloalkylcarbonylamino, (di)(1-4C)alkylaminocarbonylamino, (1-4C) alkoxycarbonylamino and R is aminocarbonyl, (di)(1-4C)alkylaminocarbonyl, (2-5C)heteroaryl or (6C)aryl. The present invention also relates to pharmaceutical compositions comprising said derivatives and the use of these derivatives to regulate fertility.
摘要翻译：本发明涉及具有通式（I）的四氢喹啉衍生物或其药学上可接受的盐，其中R 1和R 2是H或Me; R 3是H，羟基，（1-4C）烷氧基，（二）（1-4C）烷基氨基（2-4C）烷氧基或（2-6）杂环烷基（2-4C）烷氧基; R 4是H，OH，（1-4C）烷氧基或R 7; R 5是H，OH，（1-4C）烷氧基或R 7，条件是如果R 4是H，则R 5不是H，OH或（1-4C）烷氧基和如果R 5是H，则R 4不是H，OH或（1-4C）烷氧基; R 6是（2-5C）杂芳基，（6C）芳基，（3-8C）环烷基，（26C）杂环烷基或（1-6C）烷基; （6C）芳基羰基氨基，（6C）芳基羰基氧基，（2-5C）杂芳基羰基氨基，（2-5C）杂芳基羰基氧基，R 8 - （2-4C ）烷基氨基，R 8 - （2-4C）烷氧基，R 9 - 甲基氨基或R 9 - 甲氧基; （1-4C）烷基氨基，（2-6C）杂环烷基，（2-6C）杂环烷基羰基氨基，（二）（1-4C）烷基氨基羰基氨基，（1-4C）烷氧基羰基氨基和R 9是氨基羰基，（二）（1-4C）烷基氨基羰基，（2-5C）杂芳基或（6C）芳基。本发明还涉及包含所述衍生物的药物组合物以及这些衍生物用于调节生育力的用途。

2. 发明申请

WO2004056780A2 TETRAHYDROQUINOLINE DERIVATIVES 审中-公开
标题翻译：四氢喹啉衍生物
公开(公告)号：WO2004056780A2
公开(公告)日：2004-07-08
申请号：PCT/EP2003/051025
申请日：2003-12-16
申请人： AKZO NOBEL N.V. , TIMMERS, Cornelis, Marius , KARSTENS, Willem, Frederik, Johan
发明人： TIMMERS, Cornelis, Marius , KARSTENS, Willem, Frederik, Johan
IPC分类号： C07D215/38
CPC分类号： C07D215/38 , C07D215/44 , C07D401/12 , C07D405/12 , C07D409/12 , C07D409/14 , C07D413/12
摘要： The present invention relates to tetrahydroquinoline derivatives having general formula (I) or a pharmaceutically acceptable salt thereof, wherein R 1 and R 2 are H or Me; R 3 is H, hydroxy, (1-4C)alkoxy, (di)(1-4C)alkylamino(2-4C)alkoxy or (2-6)heterocycloakl(2-4C)alkoxy; R 4 is H, OH, (1-4C)alkoxy or R 7 ; R 5 is H, OH, (1-4C)alkoxy or R 7 ,with the proviso that if R 4 is H, R 5 is not H, OH or (1-4C)alkoxy and that if R 5 is H, R 4 is not H, OH or (1-4C)alkoxy; R 6 is (2-5C)heteroaryl, (6C)aryl, (3-8C)cycloalkyl, (2 6C)heterocycloalkyl or (1-6C)alkyl; R 7 is amino, (di)(1-4C) alkylamino, (6C)arylcarbonylamino, (6C)arylcarbonyloxy, (2-5C) heteroarylcarbonylamino, (2-5C)heteroarylcarbonyloxy, R 8 -(2-4C)alkylamino, R 8 -(2-4C)alkoxy, R 9 -methylamino or R 9 -methoxy; R 8 is hydroxy, amino, (1-4C)alkoxy, (di)(1-4C)alkylamino, (2-6C)heterocycloalkyl, (2-6C) heterocycloalkylcarbonylamino, (di)(1-4C)alkylaminocarbonylamino, (1-4C) alkoxycarbonylamino and R 9 is aminocarbonyl, (di)(1-4C)alkylaminocarbonyl, (2-5C)heteroaryl or (6C)aryl. The present invention also relates to pharmaceutical compositions comprising said derivatives and the use of these derivatives to regulate fertility.
摘要翻译：本发明涉及具有通式（I）的四氢喹啉衍生物或其药学上可接受的盐，其中R 1和R 2为H或Me; R 3是H，羟基，（1-4C）烷氧基，（二）（1-4C）烷基氨基（2-4C）烷氧基或（2-6）杂环基（2-4C）烷氧基; R 4是H，OH，（1-4C）烷氧基或R 7; R 5是H，OH，（1-4C）烷氧基或R 7，条件是如果R 4是H，R 5不是H，OH或（1-4C）烷氧基和如果R 5是H，则R 4不是H，OH或（1-4C）烷氧基; R 6是（2-5C）杂芳基，（6C）芳基，（3-8C）环烷基，（2 6C）杂环烷基或（1-6C）烷基; R 7是氨基，（二）（1-4C）烷基氨基，（6C）芳基羰基氨基，（6C）芳基羰氧基，（2-5C）杂芳基羰基氨基，（2-5C）杂芳基羰基氧基，R 8 - （2-4C ）烷基氨基，R 8 - （2-4C）烷氧基，R 9 - 甲基氨基或R 9 - 甲氧基; R 8是羟基，氨基，（1-4C）烷氧基，（二）（1-4C）烷基氨基，（2-6C）杂环烷基，（2-6C）杂环烷基羰基氨基，（二）（1-4C）烷基氨基羰基氨基，（1-4C）烷氧基羰基氨基，R 9是氨基羰基，（二）（1-4C）烷基氨基羰基，（2-5C）杂芳基或（6C）芳基。本发明还涉及包含所述衍生物的药物组合物和这些衍生物用于调节生育力的用途。

3. 发明申请

WO2006117370A1 4-PHENYL-5-OXO-l,4,5,6,7,8-HEXAHYDROQUINOLINE DERIVATIVES AS MEDICAMENTS FOR THE TREATMENT OF INFERTILITY 审中-公开
标题翻译： 4-苯基-5-OXO-1,4,5,6,7,8-十六氢喹啉衍生物作为治疗感染的药物
公开(公告)号：WO2006117370A1
公开(公告)日：2006-11-09
申请号：PCT/EP2006/061976
申请日：2006-05-02
申请人： N.V. ORGANON , TIMMERS, Cornelis, Marius , KARSTENS, Willem, Frederik, Johan , GRIMA POVEDA, Pedro, Manuel
发明人： TIMMERS, Cornelis, Marius , KARSTENS, Willem, Frederik, Johan , GRIMA POVEDA, Pedro, Manuel
IPC分类号： A61K31/47 , C07D215/20 , C07D401/12 , C07D405/12 , C07D417/12 , A61K31/4709 , A61P5/24
CPC分类号： C07D401/12 , C07D215/20 , C07D405/12 , C07D417/12
摘要： The invention relates to a 4-phenyl-5-oxo-l,4,5,6,7,8-hexahydroquinoline derivative according to Formula (I), wherein the substituents are defined as in the description, or a pharmaceutically salt thereof. The compounds of this invention are potent FSH receptor activators and may be used for treating fertility disorders in e.g. controlled ovarian hyperstimulation and IVF procedures.
摘要翻译：本发明涉及式（I）的4-苯基-5-氧代-1,4,5,6,7,8-六氢喹啉衍生物，其中取代基如描述中所定义，或其药学上的盐。本发明的化合物是有效的FSH受体激活剂，并且可以用于治疗生殖障碍。控制卵巢过度刺激和IVF手术。

4. 发明申请

WO2012106995A1 RORGAMMAT INHIBITORS 审中-公开
标题翻译：罗格玛抑制剂
公开(公告)号：WO2012106995A1
公开(公告)日：2012-08-16
申请号：PCT/CN2012/071017
申请日：2012-02-10
申请人： MERCK SHARP & DOHME CORP. , N.V. ORGANON , KARSTENS, Willem Frederik Johan , STELT, Mario van der , CALS, Jos , AZEVEDO, Rita Corte Real Goncalves , BARR, Kenneth Jay , ZHANG, Hongjun , BERESIS, Richard Thomas , ZHANG, Dongshan , DUAN, Xiaobang
发明人： KARSTENS, Willem Frederik Johan , STELT, Mario van der , CALS, Jos , AZEVEDO, Rita Corte Real Goncalves , BARR, Kenneth Jay , ZHANG, Hongjun , BERESIS, Richard Thomas , ZHANG, Dongshan , DUAN, Xiaobang
IPC分类号： C07D231/56 , C07D403/10 , C07D403/12 , C07D471/04 , A61K31/416 , A61K31/41 , A61K31/422 , A61K31/437 , A61P43/00 , A61P37/00 , A61P29/00
CPC分类号： A61K31/416 , A61K31/422 , A61K31/4245 , A61K31/437 , A61K31/4439 , A61K31/4709 , A61K45/06 , C07D231/56 , C07D401/06 , C07D401/12 , C07D403/10 , C07D409/14 , C07D413/12 , C07D413/14 , C07D471/04 , Y02A50/409
摘要： The present invention relates to compounds according to Formula (I) or a pharmaceutically acceptable salt or solvate thereof. Such compounds can be used in the treatment of RORgammaT-mediated diseases or condition.
摘要翻译：本发明涉及式（I）化合物或其药学上可接受的盐或溶剂合物。这些化合物可用于治疗RORGAMMT介导的疾病或病症。

5. 发明申请

WO2009098283A1 (DIHYDRO)PYRROLO[2,1-A]ISOQUINOLINES 审中-公开
标题翻译：（二氢）吡咯并[2,1-A]异喹啉
公开(公告)号：WO2009098283A1
公开(公告)日：2009-08-13
申请号：PCT/EP2009/051366
申请日：2009-02-06
申请人： N.V. ORGANON , VAN RIJN, Rachel Deborah , LOOZEN, Hubert, Jan, Jozef , TIMMERS, Cornelis, Marius , VAN DER VEEN, Lars, Anders , KARSTENS, Willem, Frederik, Johan
发明人： VAN RIJN, Rachel Deborah , LOOZEN, Hubert, Jan, Jozef , TIMMERS, Cornelis, Marius , VAN DER VEEN, Lars, Anders , KARSTENS, Willem, Frederik, Johan
IPC分类号： C07D471/04 , C07D471/18 , A61K31/551 , A61P15/08
CPC分类号： C07D471/04 , C07D471/18
摘要： The invention relates to 5,6 - dihydropyrrolo [2,1- a ] isoquinoline and pyrrolo[2,1- a ] isoquinoline derivatives according to general formula (I) or a pharmaceutically acceptable salt thereof. The compounds can be used for the treatment of infertility.
摘要翻译：本发明涉及通式（I）的5,6-二氢吡咯并[2,1-a]异喹啉和吡咯并[2,1-a]异喹啉衍生物或其药学上可接受的盐。该化合物可用于治疗不育症。

6. 发明申请

WO2009027482A3 TSH RECEPTOR ANTAGONIZING TETRAHYDROQUINOLINE COMPOUNDS 审中-公开
公开(公告)号：WO2009027482A3
公开(公告)日：2009-03-05
申请号：PCT/EP2008/061325
申请日：2008-08-28
申请人： N.V. ORGANON , KARSTENS, Willem, Frederik, Johan , CONTI, Paolo, Giovanni, Martino , TIMMERS, Cornelis, Marius , PLATE, Ralf , VAN KOPPEN, Christianus, Johannes
发明人： KARSTENS, Willem, Frederik, Johan , CONTI, Paolo, Giovanni, Martino , TIMMERS, Cornelis, Marius , PLATE, Ralf , VAN KOPPEN, Christianus, Johannes
IPC分类号： A61K31/47 , A61P5/08 , C07D215/38
摘要： The present invention relates the use of a compound, a pharmaceutical composition, compounds and a kit for treating or preventing disorders in a mammal responsive to TSH receptor mediated pathways, including disorders such as hyperthyroidism, Graves' disease, Graves Ophthalmopathy, Graves' associated pretibial dermopathy, nodular goitre and thyroid cancer comprising administering to said mammal an effective amount of a tetrahydroquinoline compound of Formula (I) or an pharmaceutically acceptable salt thereof.

7. 发明申请

WO2006117368A1 4-PHENYL-5-OXO-1,4,5,6,7,8-HEXAHYDROQUINOLINE DERIVATIVES THE TREATMENT OF INFERTILITY 审中-公开
标题翻译： 4-苯基-5-氧代-1,4,5,6,7,8-六氢喹啉衍生物治疗感染
公开(公告)号：WO2006117368A1
公开(公告)日：2006-11-09
申请号：PCT/EP2006/061972
申请日：2006-05-02
申请人： N.V. ORGANON , GRIMA POVEDA, Pedro, Manuel , KARSTENS, Willem, Frederik, Johan , TIMMERS, Cornelis, Marius
发明人： GRIMA POVEDA, Pedro, Manuel , KARSTENS, Willem, Frederik, Johan , TIMMERS, Cornelis, Marius
IPC分类号： A61K31/47 , C07D215/20 , C07D401/12 , C07D405/12 , C07D409/12 , C07D417/12 , A61K31/4709 , A61P5/24
CPC分类号： C07D401/12 , C07D215/20 , C07D405/12 , C07D409/12 , C07D417/12
摘要： The present invention relates to 4-phenyl-5-oxo-l,4)5,6,7,8-hexahydroquinoline derivatives according to Formula I, Formula I or a pharmaceutically acceptable salt thereof, wherein R 1 is (l-6C)alkyl, (2-6C)alkenyl or (2-6C)aDcynyl; R 2 , R 3 are independently halogen, (l-4C)allcyl, (2-4C)alkenyl, (2-4C)- alkynyl, (1 -4C)aBcoxy, (3-4C)alkenyloxy or (3-4C)alkynyloxy; R 4 is phenyl or (2-5C)- heteroaryl, both substituted with R 7 and optionally substituted on the (hetero)aromatic ring with one or more substituents selected from hydroxy, amino, halogen, nitro, trifluoromethyl, cyano, (l-4C)alkyl, (l-4C)alkoxy , (l-4C)alkylthio and (di)(l-4C)- alkylamino. The invention also relates to pharmaceutical compositions comprising said derivatives, as well as to the use of these 4-phenyl-5-oxo-l, 4,5,6, 7,8-hexahydro- quinoline derivatives in therapy, more specifically for the treatment of infertility
摘要翻译：本发明涉及式I式I的4-苯基-5-氧代-1,2,4,5,6,7,8-六氢喹啉衍生物或其药学上可接受的盐，其中R 1〜是（1-6C）烷基，（2-6C）烯基或（2-6C）芳基; （2-4C）链烯基，（2-4C） - 炔基，（1-4C）环烷基，（1-4C）烷基，（1-4C）（3-4C）烯氧基或（3-4C）炔氧基; R 4是苯基或（2-5C） - 杂芳基，两者均被R 7取代，并且任选地在（杂）芳环上取代有一个或多个选自羟基的取代基，氨基，卤素，硝基，三氟甲基，氰基，（1-4C）烷基，（1-4C）烷氧基，（1-4C）烷硫基和（二）（1-4C）烷基氨基。本发明还涉及包含所述衍生物的药物组合物，以及这些4-苯基-5-氧代-1,2,5,6,7,8-六氢 - 喹啉衍生物在治疗中的用途，更具体地说，治疗不育症

8. 发明申请

WO2009027482A2 TSH RECEPTOR ANTAGONIZING TETRAHYDROQUINOLINE COMPOUNDS 审中-公开
标题翻译： TSH受体拮抗四氢喹啉化合物
公开(公告)号：WO2009027482A2
公开(公告)日：2009-03-05
申请号：PCT/EP2008061325
申请日：2008-08-28
申请人： ORGANON NV , KARSTENS WILLEM FREDERIK JOHAN , CONTI PAOLO GIOVANNI MARTINO , TIMMERS CORNELIS MARIUS , PLATE RALF , VAN KOPPEN CHRISTIANUS JOHANNE
发明人： KARSTENS WILLEM FREDERIK JOHAN , CONTI PAOLO GIOVANNI MARTINO , TIMMERS CORNELIS MARIUS , PLATE RALF , VAN KOPPEN CHRISTIANUS JOHANNE
IPC分类号： A61K31/47 , A61P5/08
CPC分类号： C07D215/38 , A61K31/47 , A61K31/4709 , C07D401/10 , C07D401/12 , C07D405/12 , C07D409/12
摘要： The present invention relates the use of a compound, a pharmaceutical composition, compounds and a kit for treating or preventing disorders in a mammal responsive to TSH receptor mediated pathways, including disorders such as hyperthyroidism, Graves' disease, Graves Ophthalmopathy, Graves' associated pretibial dermopathy, nodular goitre and thyroid cancer comprising administering to said mammal an effective amount of a tetrahydroquinoline compound of Formula (I) or an pharmaceutically acceptable salt thereof.
摘要翻译：本发明涉及化合物，药物组合物，化合物和用于治疗或预防针对TSH受体介导的途径的哺乳动物疾病的试剂盒的应用，包括诸如甲状腺机能亢进，格雷夫斯病，格雷夫斯眼病，格雷夫斯相关的前囟素皮肤病，结节性甲状腺肿和甲状腺癌，包括向所述哺乳动物施用有效量的式（I）的四氢喹啉化合物或其药学上可接受的盐。

9. 发明申请

WO2006117371A1 4-PHENYL-5-0X0-l,4,5,6,7,8-HEXAHYDR0QËIN0LINE DERIVATIVES AS MEDICAMENTS FOR THE TREATMENT OF INFERTILITY 审中-公开
标题翻译： 4-苯基-5-0X0-1,4,5,6,7,8-HEXAHYDR0QININLINE衍生物作为治疗感染的药物
公开(公告)号：WO2006117371A1
公开(公告)日：2006-11-09
申请号：PCT/EP2006/061978
申请日：2006-05-02
申请人： N.V. ORGANON , KARSTENS, Willem, Frederik, Johan , TIMMERS, Cornelis, Marius
发明人： KARSTENS, Willem, Frederik, Johan , TIMMERS, Cornelis, Marius
IPC分类号： A61K31/47 , C07D215/20 , C07D401/12 , A61K31/4709 , A61P5/24
CPC分类号： C07D215/20 , C07D401/12 , C07D413/12 , C07D417/12
摘要： The present invention- relates to 2-methyl-4-phenyl-5-oxo-1 ,4,5,6,7,8-hexahydroquinoline derivatives having the general Formula (I) wherein the substituents are defined as in the description, or a pharmaceutically acceptable salt thereof. The invention also relates to pharmaceutical compositions comprising said derivatives, as well as to the use of these 2-methyl-4-phenyl-5-oxo-1 ,4,5,6,7,8-hexahydroquinoline derivatives in therapy, more specifically for the treatment of fertility disorders.
摘要翻译：本发明涉及具有通式（I）的2-甲基-4-苯基-5-氧代-1,4,5,6,7,8-六氢喹啉衍生物，其中取代基如描述中所定义，或其药学上可接受的盐。本发明还涉及包含所述衍生物的药物组合物，以及这些2-甲基-4-苯基-5-氧代-1,4,5,6,7,8-六氢喹啉衍生物在治疗中的用途，更具体地说用于治疗生育障碍。

10. 发明申请

WO2004056779A3 TETRAHYDROQUINOLINE DERIVATIVES AND THEIR USE AS FSH RECEPTOR MODULATORS 审中-公开
标题翻译：四氢喹啉衍生物及其作为FSH受体调节剂的用途
公开(公告)号：WO2004056779A3
公开(公告)日：2004-08-12
申请号：PCT/EP0351024
申请日：2003-12-16
申请人： AKZO NOBEL NV , TIMMERS CORNELIS MARIUS , KARSTENS WILLEM FREDERIK JOHAN
发明人： TIMMERS CORNELIS MARIUS , KARSTENS WILLEM FREDERIK JOHAN
IPC分类号： A61K31/47 , A61P5/08 , C07D215/38 , C07D401/12 , C07D409/12
CPC分类号： C07D215/38 , C07D401/12 , C07D405/12 , C07D409/12
摘要： The present invention relates to tetrahydroquinoline derivatives having general formula (I) or a pharmaceutically acceptable salt thereof, wherein R and R are H, Me; R is (2-6C)heterocycloalkyl(1-4C)alkyl, (2-5C)heteroaryl(1-4C)alkyl, (6C)aryl (1-4C)alkyl, (1-4C)(di)alkylaminocarbonylamino(2-4C)alkyl, (2-6C) heterocycloalkylcarbonylamino(2-4C)alkyl, R -(2-4C)alkyl or R -carbonyl(1-4C)alkyl; R is (2-5C)heteroaryl, (6C)aryl, (3-8C)cycloalkyl, (2-6C)heterocycloalkyl or (1-6C) alkyl and R is (di)(1-4C)alkylamino, (1-4C)alkoxy, amino, hydroxy, (6C)arylamino, (di)(3-4C)alkenylamino, (2-5C)heteroaryl(1-4C)alkylamino, (6C)aryl(1-4C) alkylamino, (di)[(1-4C)alkoxy(2-4C)alkyl]amino, (di)[(1-4C)alkylamino(2-4C) alkyl]amino, (di)[amino(2-4C)alkyl]amino or (di)[hydroxy(2-4C)alkyl]amino. The present invention also relates to pharmaceutical compositions comprising said derivatives and the use of these derivatives to regulate fertility.
摘要翻译：本发明涉及具有通式（I）的四氢喹啉衍生物或其药学上可接受的盐，其中R 1和R 2是H，Me; （2-3C）杂环烷基（1-4C）烷基，（2-5C）杂芳基（1-4C）烷基，（6C）芳基（1-4C）烷基，（1-4C）（二）烷基氨基羰基氨基（2-4C）烷基，（2-6C）杂环烷基羰基氨基（2-4C）烷基，R 5 - （2-4C）烷基或R 5 - 羰基（1-4C）（2-5C）杂芳基，（6C）芳基，（3-8C）环烷基，（2-6C）杂环烷基或（1-6C）烷基且R 5是（二）（1-4C ）烷基氨基，（1-4C）烷氧基，氨基，羟基，（6C）芳基氨基，（二）（3-4C）烯基氨基，（2-5C）杂芳基（1-4C）（二）[（1-4C）烷氧基（2-4C）烷基]氨基，（二）[（1-4C）烷基氨基（2-4C）烷基]氨基，（二）[氨基（2-4C））烷基]氨基或（二）[羟基（2-4C）烷基]氨基。本发明还涉及包含所述衍生物的药物组合物以及这些衍生物用于调节生育力的用途。

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