KR101118779B1 - 면역억제제 화합물 및 조성물 - Google Patents
면역억제제 화합물 및 조성물 Download PDFInfo
- Publication number
- KR101118779B1 KR101118779B1 KR1020057022058A KR20057022058A KR101118779B1 KR 101118779 B1 KR101118779 B1 KR 101118779B1 KR 1020057022058 A KR1020057022058 A KR 1020057022058A KR 20057022058 A KR20057022058 A KR 20057022058A KR 101118779 B1 KR101118779 B1 KR 101118779B1
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- South Korea
- Prior art keywords
- ethyl
- propionic acid
- benzylamino
- trifluoromethyl
- benzyloxyimino
- Prior art date
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- 0 **C(*)(**ON=C(*)*)C1C(*)C1 Chemical compound **C(*)(**ON=C(*)*)C1C(*)C1 0.000 description 3
- GBGPVUAOTCNZPT-UHFFFAOYSA-N Cc1cc(cccc2)c2[o]1 Chemical compound Cc1cc(cccc2)c2[o]1 GBGPVUAOTCNZPT-UHFFFAOYSA-N 0.000 description 1
- BLZKSRBAQDZAIX-UHFFFAOYSA-N Cc1cc(cccc2)c2[s]1 Chemical compound Cc1cc(cccc2)c2[s]1 BLZKSRBAQDZAIX-UHFFFAOYSA-N 0.000 description 1
- DXYYSGDWQCSKKO-UHFFFAOYSA-N Cc1nc(cccc2)c2[s]1 Chemical compound Cc1nc(cccc2)c2[s]1 DXYYSGDWQCSKKO-UHFFFAOYSA-N 0.000 description 1
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- C07D205/02—Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom not condensed with other rings
- C07D205/04—Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
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- A61K31/397—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having four-membered rings, e.g. azetidine
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- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/445—Non condensed piperidines, e.g. piperocaine
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Abstract
Description
Claims (12)
- 화학식 Ⅰa 및 Ⅰb로부터 선택되는 화합물; 또는 그의 약제학적으로 허용되는 염, 수화물, 용매화물, 이성체 또는 프로드럭:<화학식 Ia><화학식 Ib>상기 식에서:A는 -C(O)OR5, -OP(O)(OR5)2, -P(O)(OR5)2, -S(O)20R5, -P(O)(R5)OR5 및 1H-테트라졸-5-일로부터 선택되고; 여기에서 각각의 R5는 독립적으로 수소 및 C1-6알킬로부터 선택되며;W는 결합, C1-3알킬렌, C2-3알케닐렌으로부터 선택되고;Y는 C6-10아릴 및 C2-9헤테로아릴로부터 선택되며; 여기에서 Y의 어느 아릴 또는 헤테로아릴은 할로, 하이드록시, 니트로, C1-6알킬, C1-6알콕시, 할로-치환된 C1-6알킬 및 할로-치환된 C1-6알콕시로부터 선택되는 1 내지 3개의 라디칼로 치환될 수 있고;Z는로부터 선택되며;여기에서 Z의 좌측 및 우측 별표는 각각 화학식 Ⅰa 또는 Ⅰb의 -C(R3)(R4)-와 A 사이의 결합 점을 나타내고; R6는 수소 및 C1-6알킬로부터 선택되며; J1 및 J2는 독립적으로 메틸렌 또는 S, O 및 NR5로부터 선택되는 헤테로원자이고; 여기에서 R5는 수소 및 C1-6알킬로부터 선택되며; Z의 어느 알킬렌은 추가로 할로, 하이드록시, C1-6알킬로부터 선택되는 1 내지 3개의 라디칼에 의해 치환될 수 있거나; R6는 Y의 탄소 원자와 결합하여 5-7 원 환을 형성할 수 있고;R1은 C6-10아릴 및 C2-9헤테로아릴로부터 선택되며; 여기에서 R1의 어느 아릴 또는 헤테로아릴은 C6-10아릴C0-4알킬, C2-9헤테로아릴C0-4알킬, C3-8사이클로알킬C0-4알킬, C3-8헤테로사이클로알킬C0-4알킬 또는 C1-6알킬로부터 선택되는 라디칼에 의해 치환될 수 있고; 여기에서 R1의 어느 아릴, 헤테로아릴, 사이클로알킬 또는 헤테로사이클로알킬 그룹은 할로, C1-6알킬, C1-6알콕시, 할로-치환된-C1-6알킬 및 할로-치환된-C1-6알콕시로부터 선택되는 1 내지 5개의 라디칼에 의해 치환될 수 있으며; R1의 어느 알킬 그룹은 -S-, -S(O)-, -S(0)2-, -NR5- 및 -O-로부터 선택되는 원자 또는 그룹에 의해 대체된 메틸렌을 가질 수 있고; 여기에서 R5는 수소 또는 C1-6알킬로부터 선택되며;R2는 수소, C1-6알킬, C2-6알케닐, C2-6알키닐 및 할로 치환된 C1-6알킬로부터 선택되고;R3 및 R4는 독립적으로 수소, C1-6알킬, 할로, 하이드록시, C1-6알콕시, 할로-치환된 C1-6알킬 및 할로-치환된 C1-6알콕시로부터 선택된다.
- 제1항에 있어서, R1은 C6-10아릴C0-4알킬, C2-9헤테로아릴C0-4알킬, C3-8사이클로알킬C0-4알킬, C3-8헤테로사이클로알킬C0-4알킬 또는 C1-6알킬에 의해 치환될 수 있는 페닐, 나프틸 또는 티에닐이고; 여기에서 R1의 어느 아릴, 헤테로아릴, 사이클로알킬 또는 헤테로사이클로알킬 그룹은 할로, C1-6알킬, C1-6알콕시, 할로-치환된-C1-6알킬 및 할로-치환된-C1-6알콕시로부터 선택되는 1 내지 5개의 라디칼에 의해 치환될 수 있으며; R1의 어느 알킬 그룹은 -S-, -S(O)-, -S(0)2-, -NR5- 및 -O-로부터 선택되는 원자 또는 그룹에 의해 대체된 메틸렌을 가질 수 있고; 여기에서 R5는 수소 또는 C1-6알킬인 화합물.
- 제1항에 있어서, Y는로부터 선택되고,여기에서 R7은 수소 또는 C1-6알킬이며; Y의 좌측 및 우측 별표는 a) 각각, 화학식 Ⅰa의 -C(R2)=NOWR1과 -CR3R4- 사이, 또는 -CR3R4-와 -C(R2)=NOWR1 사이의 결합 점, 또는 b) 각각, 화학식 Ⅰb의 -CR3R4-와 W 사이, 또는 W와 -CR3R4- 사이의 결합 점을 나타내고; 여기에서 Y의 어느 아릴 또는 헤테로아릴은 할로, 하이드록시, 니트로, C1-6알킬, C1-6알콕시, 할로-치환된 C1-6알킬 및 할로-치환된 C1-6알콕시로부터 선택되는 1 내지 3개의 라디칼로 치환될 수 있는 화합물.
- 제1항에 있어서, R1은로부터 선택되고,여기에서, 별표는 R1의 W와의 결합 점이고; R8은 C6-10아릴C0-4알킬, C2-9헤테로아릴C0-4알킬, C3-8사이클로알킬C0-4알킬, C3-8헤테로사이클로알킬C0-4알킬 또는 C1-6알킬이며; 여기에서 R8의 어느 아릴, 헤테로아릴, 사이클로알킬 또는 헤테로사이클로알킬 그룹은 할로, C1-6알킬, C1-6알콕시, 할로-치환된-C1-6알킬 및 할로-치환된-C1-6알콕시로부터 선택되는 1 내지 3개의 라디칼에 의해 치환될 수 있고; R8의 어느 알킬 그룹은 -S-, -S(O)-, -S(0)2-, -NR5- 및 -O-로부터 선택되는 원자 또는 그룹에 의해 대체된 메틸렌을 가질 수 있으며; 여기에서 R5는 수소 또는 C1-6알킬이고; R9은 할로, C1-6알킬, C1-6알콕시, 할로-치환된-C1-6알킬 및 할로-치환된-C1-6알콕시로부터 선택되는 화합물.
- 제5항에 있어서, Y는 페닐, 피리디닐, 티에닐 및 퓨라닐로부터 선택되고; 여기에서 Y의 어느 페닐, 피리디닐, 티에닐 또는 퓨라닐은 메틸, 에틸, 사이클로프로필, 클로로, 브로모, 플루오로 및 메톡시로부터 선택되는 1 내지 3개의 라디칼로 치환될 수 있거나; Y가 페닐인 경우, R6는 Y의 탄소 원자에 결합되어 3,4-디하이드로-1H-이소퀴놀린-2-일을 형성할 수 있는 화합물.
- 제6항에 있어서, 3-{4-[1-(2-트리플루오로메틸-비페닐-4-일메톡시이미노)-에틸]-벤질아미노}-프로피온산, 3-{4-[1-(4-사이클로헥실-3-트리플루오로메틸-벤질옥시이미노)-에틸]-2-에틸-벤질아미노}-프로피온산, 1-{4-[1-(4-사이클로헥실-3-트리플루오로메틸-벤질옥시이미노)-에틸]-2-에틸-벤질}-아제티딘-3-카르복실산, 3-({2-클로로-6-[1-(4-사이클로헥실-3-트리플루오로메틸-벤질옥시이미노)-에틸]-피리딘-3-일메틸}-아미노)-프로피온산, 3-({6-[1-(4-사이클로헥실-3-트리플루오로메틸-벤질옥시이미노)-에틸]-2-에틸-피리딘-3-일메틸}-아미노)-프로피온산, 3-{4-[1-(비페닐-4-일메톡시이미노)-에틸]-벤질아미노}-프로피온산, 4-{4-[1-(비페닐-4-일메톡시이미노)-에틸]-벤질아미노}-부티르산, 1-{4-[1-(비페닐-4-일메톡시이미노)-에틸]-벤질}-아제티딘-3-카르복실산, 1-{4-[1-(비페닐-4-일메톡시이미노)-에틸]-벤질}-피페리딘-3-카르복실산, {4-[1-(비페닐-4-일메톡시이미노)-에틸]-벤질아미노}-아세트산, 3-{4-[1-(비페닐-4-일메톡시이미노)-에틸]-벤질아미노}-사이클로펜탄카르복실산, 3-{4-[1-(4'-트리플루오로메틸-비페닐-4-일메톡시이미노)-에틸]-벤질아미노}-프로피온산, 3-{4-[1-(5-페닐-퓨란-2-일메톡시이미노)-에틸]-벤질아미노}-프로피온산, 3-{4-[1-(3'-트리플루오로메틸-비페닐-4-일메톡시이미노)-에틸]-벤질아미노}-프로피온산, 3-{4-[1-(3-트리플루오로메틸-비페닐-4-일메톡시이미노)-에틸]-벤질아미노}-프로피온산, 3-{4-[1-(4'-메톡시-비페닐-4-일메톡시이미노)-에틸]-벤질아미노}-프로피온산, 3-{4-[1-(비페닐-3-일메톡시이미노)-에틸]-벤질아미노}-프로피온산, 3-{4-[1-(4-티오펜-2-일-벤질옥시이미노)-에틸]-벤질아미노}-프로피온산, 3-{4-[1-(4-티오펜-2-일-3-트리플루오로메틸-벤질옥시이미노)-에틸]-벤질아미노}-프로피온산, 3-{4-[1-(4'-플루오로-비페닐-4-일메톡시이미노)-에틸]-벤질아미노}-프로피온산, 3-{4-[1-(4'-트리플루오로메톡시-비페닐-4-일메톡시이미노)-에틸]-벤질아미노}-프로피온산, 3-{4-[1-(3'-트리플루오로메톡시-비페닐-4-일메톡시이미노)-에틸]-벤질아미노}-프로피온산, 1-{4-[1-(2-트리플루오로메틸-비페닐-4-일메톡시이미노)-에틸]-벤질}-아제티딘-3-카르복실산, 1-{4-[1-(2-트리플루오로메틸-비페닐-4-일메톡시이미노)-에틸]-벤질}-피롤리딘-3-카르복실산, 1-{4-[1-(2-트리플루오로메틸-비페닐-4-일메톡시이미노)-에틸]-벤질}-피페리딘-3-카르복실산, 3-{4-[1-(3'-메톡시-비페닐-4-일메톡시이미노)-에틸]-벤질아미노}-프로피온산, 2-하이드록시-3-{4-[1-(2-트리플루오로메틸-비페닐-4-일메톡시이미노)-에틸]-벤질아미노}-프로피온산, 3-{4-[1-(4'-메틸-비페닐-4-일메톡시이미노)-에틸]-벤질아미노}-프로피온산, 3-{4-[1-(4-페닐-티오펜-2-일메톡시이미노)-에틸]-벤질아미노}-프로피온산, 1-{4-[1-(비페닐-4-일메톡시이미노)-에틸]-벤질}-피롤리딘-3-카르복실산, 3-{4-[1-(4-퓨란-3-일-벤질옥시이미노)-에틸]-벤질아미노}-프로피온산, 3-{4-[1-(4-티오펜-3-일-3-트리플루오로메틸-벤질옥시이미노)-에틸]-벤질아미노}-프로피온산, 3-{4-[1-(4-티오펜-3-일-2-트리플루오로메틸-벤질옥시이미노)-에틸]-벤질아미노}-프로피온산, 2-플루오로-3-{4-[1-(2-트리플루오로메틸-비페닐-4-일메톡시이미노)-에틸]-벤질아미노}-프로피온산, 3-{4-[1-(2-트리플루오로메틸-비페닐-4-일메톡시이미노)-에틸]-벤질아미노}-부티르산, 3-{4-[1-(5-페닐-티오펜-2-일메톡시이미노)-에틸]-벤질아미노}-프로피온산, 3-{4-[1-(4-사이클로헥실-벤질옥시이미노)-에틸]-벤질아미노}-프로피온산, 3-{4-[1-(3-플루오로-비페닐-4-일메톡시이미노)-에틸]-벤질아미노}-프로피온산, 3-{4-[1-(4'-플루오로-2-트리플루오로메틸-비페닐-4-일메톡시이미노)-에틸]-벤질아미노}-프로피온산, 3-{4-[1-(4'-메틸-2-트리플루오로메틸-비페닐-4-일메톡시이미노)-에틸]-벤질아미노}-프로피온산, 3-{4-[1-(4-퓨란-2-일-3-트리플루오로메틸-벤질옥시이미노)-에틸]-벤질아미노}-프로피온산, 3-{4-[1-(2'-플루오로-2-트리플루오로메틸-비페닐-4-일메톡시이미노)-에틸]-벤질아미노}-프로피온산, 3-(4-{1-[4-(3,3-디메틸-부틸)-3-트리플루오로메틸-벤질옥시이미노]-에틸)-벤질아미노)-프로피온산, 3-{4-[1-(4-퓨란-3-일-3-트리플루오로메틸-벤질옥시이미노)-에틸]-벤질아미노}-프로피온산, 3-{4-[1-(4-피리딘-3-일-벤질옥시이미노)-에틸]-벤질아미노}-프로피온산, 3-{4-[1-(4-피리딘-4-일-벤질옥시이미노)-에틸]-벤질아미노}-프로피온산, 3-{4-[1-(2-플루오로-비페닐-4-일메톡시이미노)-에틸]-벤질아미노}-프로피온산, 3-({2-메톡시-6-[1-(2-트리플루오로메틸-비페닐-4-일메톡시이미노)-에틸]-피리딘-3-일메틸}-아미노)-프로피온산, 3-{4-[1-(4-사이클로헥실-3-트리플루오로메틸-벤질옥시이미노)-에틸]-2-에틸-벤질아미노}-프로피온산, 3-{4-[1-(4-사이클로헥실-3-트리플루오로메틸-벤질옥시이미노)-에틸]-벤질아미노}-프로피온산, 3-{2-브로모-4-[1-(4-사이클로헥실-3-트리플루오로메틸-벤질옥시이미노)-에틸]-벤질아미노}-프로피온산, 3-{4-[1-(4-사이클로펜틸-3-트리플루오로메틸-벤질옥시이미노)-에틸]-벤질아미노}-프로피온산, 3-{2-클로로-4-[1-(4-사이클로헥실-3-트리플루오로메틸-벤질옥시이미노)-에틸]-벤질아미노}-프로피온산, 3-({6-[1-(4-사이클로헥실-3-트리플루오로메틸-벤질옥시이미노)-에틸]-피리딘-3-일메틸}-아미노)-프로피온산, 3-({5-[1-(4-사이클로헥실-3-트리플루오로메틸-벤질옥시이미노)-에틸]-티오펜-2-일메틸}-아미노)-프로피온산, 3-({5-[1-(4-사이클로헥실-3-트리플루오로메틸-벤질옥시이미노)-에틸]-피리딘-2-일메틸}-아미노)-프로피온산, 3-({5-[1-(4-사이클로헥실-3-트리플루오로메틸-벤질옥시이미노)-에틸]-퓨란-2-일메틸}-아미노)-프로피온산, 3-({2-[1-(4-사이클로헥실-3-트리플루오로메틸-벤질옥시이미노)-에틸]-피리딘-4-일메틸}-아미노)-프로피온산, 3-{4-[1-(4-사이클로헥실-3-플루오로-벤질옥시이미노)-에틸]-벤질아미노}-프로피온산, 3-{2-클로로-4-[1-(4-사이클로헥실-3-트리플루오로메틸-벤질옥시이미노)-에틸]-벤질아미노}-프로피온산, 1-{6-[1-(4-사이클로헥실-3-트리플루오로메틸-벤질옥시이미노)-에틸]-2-에틸-피리딘-3-일메틸}-아제티딘-3-카르복실산, 3-{2-에틸-4-[1-(4-피페리딘-1-일-3-트리플루오로메틸-벤질옥시이미노)-에틸]-벤질아미노}-프로피온산, 3-{4-[1-(4-사이클로헥실-3-메틸-벤질옥시이미노)-에틸]-2-에틸-벤질아미노}-프로피온산, 3-{4-[1-(3-클로로-4-사이클로헥실-벤질옥시이미노)-에틸]-2-에틸-벤질아미노}-프로피온산, 3-{4-[1-(4-사이클로헥실-3-메톡시-벤질옥시이미노)-에틸]-2-에틸-벤질아미노}-프로피온산, 1-{4-[1-(4-사이클로헥실-3-메톡시-벤질옥시이미노)-에틸]-2-에틸-벤질}-아제티딘-3-카르복실산, 3-{4-[1-(4-사이클로헥실-3-트리플루오로메틸-벤질옥시이미노)-에틸]-2-메틸-벤질아미노}-프로피온산, 1-{4-[1-(4-사이클로헥실-3-트리플루오로메틸-벤질옥시이미노)-에틸]-2-메틸-벤질}-아제티딘-3-카르복실산, 3-{4-[1-(4-사이클로헥실-3-트리플루오로메틸-벤질옥시이미노)-에틸]-2-사이클로프로필-벤질아미노}-프로피온산, 1-{4-[1-(4-사이클로헥실-3-트리플루오로메틸-벤질옥시이미노)-에틸]-2-사이클로프로필-벤질}-아제티딘-3-카르복실산, 3-{2-에틸-4-[1-(2-트리플루오로메틸-비페닐-4-일메톡시이미노)-에틸]-벤질아미노}-프로피온산, 1-{4-[1-(4-사이클로헥실-3-에틸-벤질옥시이미노)-에틸]-2-에틸-벤질}-아제티딘-3-카르복실산, 1-{4-[1-(4-사이클로헥실-3-메틸-벤질옥시이미노)-에틸]-2-에틸-벤질}-아제티딘-3-카르복실산, 1-{2-클로로-4-[1-(4-사이클로헥실-3-에틸-벤질옥시이미노)-에틸]-벤질}-아제티딘-3-카르복실산, 3-{2-클로로-4-[1-(4-사이클로헥실-3-에틸-벤질옥시이미노)-에틸]-벤질아미노}-프로피온산, 3-{4-[1-(4-사이클로헥실-3-트리플루오로메틸-벤질옥시이미노)-에틸]-2-플루오로-벤질아미노}-프로피온산, 1-{4-[1-(4-사이클로헥실-3-트리플루오로메틸-벤질옥시이미노)-에틸]-2-플루오로-벤질}-아제티딘-3-카르복실산, 3-{6-[1-(4-사이클로헥실-3-트리플루오로메틸-벤질옥시이미노)-에틸]-3,4-디하이드로-1H-이소퀴놀린-2-일}-프로피온산, 3-{6-[1-(4-사이클로헥실-3-에틸-벤질옥시이미노)-에틸]-3,4-디하이드로-1H-이소퀴놀린-2-일}-프로피온산, 3-{4-[1-(2-트리플루오로메틸-비페닐-4-일)-에틸리덴아미노옥시메틸]-벤질아미노}-프로피온산, 3-{4-[1-(4-사이클로헥실-3-트리플루오로메틸-페닐)-에틸리덴아미노옥시메틸]-벤질아미노}-프로피온산, 3-{4-[1-(4-사이클로헥실-3-트리플루오로메틸-페닐)-에틸리덴아미노옥시메틸]-2-에틸-벤질아미노}-프로피온산, 1-{4-[1-(4-사이클로헥실-3-트리플루오로메틸-페닐)-에틸리덴아미노옥시메틸]-2-에틸-벤질}-아제티딘-3-카르복실산 및 1-{4-[1-(4-사이클로헥실-3-에틸-페닐)-에틸리덴아미노옥시메틸]-2-에틸-벤질}-아제티딘-3-카르복실산으로부터 선택되는 화합물.
- 치료 유효량의 제1항의 화합물을 포함하는, 동물에서 세포, 조직 또는 기관 동종- 또는 이종이식편의 급성 또는 만성 거부 또는 지연된 이식편 기능, 이식편 대 숙주 질환, 자가면역 질환, 류마티스성 관절염, 전신성 홍반성낭창, 하시모토 갑상선염, 다발성 경화증, 중증 근무력증, Ⅰ형 및 Ⅱ형 당뇨, 혈관염, 악성빈혈, 스조그렌 증후군, 포도막염, 건선, 그레이브스 안병증, 원형탈모증, 알러지 질환, 알러지성 천식, 아토피성 피부염, 알러지성 비염, 결막염, 알러지성 접촉 피부염, 염증성 질환, 염증성 대장 질환, 크론병, 궤양성 결장염, 내재성 천식, 염증성 폐 손상, 염증성 간 손상, 염증성 사구체 손상, 아데롬성경화증, 골관절염, 자극성 접촉 피부염, 습진성 피부염, 지루성 피부염, 면역-매개 장애의 피부 증상, 염증성 안 질환, 각결막염, 심근염 또는 간염, 허혈 손상, 재관류 손상, 심근경색증, 졸중, 외상성 쇼크, 장 허혈, 신 부전, 출혈성 쇼크, T 세포 림프종, T 세포 백혈병, 감염성 질환, 독성 쇼크, 패혈성 쇼크, 바이러스 감염, 성인 호흡기 장애 증후군, AIDS, 바이러스성 간염, 만성 세균 감염, 및 노인성 치매로 이루어진 군으로부터 선택되는 질환 또는 장애를 치료하거나, 또는 상기 질환 또는 장애의 병리 또는 징후를 저해 또는 경감시키는데 사용하기 위한 제약 조성물.
- 유효량의 제1항의 화합물, 또는 그의 약제학적으로 허용되는 염을 포함하는, 대상에서 림프구에 의해 매개되는 장애나 질환을 예방 또는 치료하거나, 급성 또는 만성 이식편 거부 또는 T-세포 매개된 염증성 또는 자가면역 질환을 예방 또는 치료하거나, 조절해제된 혈관형성을 저해 또는 제어하거나, 신-혈관형성 과정에 의해 매개되거나 조절해제된 혈관형성과 관련된 질환을 예방 또는 치료하기 위한 제약 조성물.
- 삭제
- 삭제
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