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KR960704544A - 비인슐린 의존성 당뇨병(niddm)의 개시를 예방 또는 지체시키기 위한 티아졸리딘디온의 용도[use of thiazolidinediones to prevent or delay onset of niddm] - Google Patents

비인슐린 의존성 당뇨병(niddm)의 개시를 예방 또는 지체시키기 위한 티아졸리딘디온의 용도[use of thiazolidinediones to prevent or delay onset of niddm]

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Publication number
KR960704544A
KR960704544A KR1019960701336A KR19960701336A KR960704544A KR 960704544 A KR960704544 A KR 960704544A KR 1019960701336 A KR1019960701336 A KR 1019960701336A KR 19960701336 A KR19960701336 A KR 19960701336A KR 960704544 A KR960704544 A KR 960704544A
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올레프스키 제롤드
안토누치 타미
록우드 딘
노리스 레베카
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가와우라 요시부미
상꾜가부시끼가이샤
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First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=22401599&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=KR960704544(A) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by 가와우라 요시부미, 상꾜가부시끼가이샤 filed Critical 가와우라 요시부미
Priority claimed from PCT/US1994/010389 external-priority patent/WO1995007694A1/en
Publication of KR960704544A publication Critical patent/KR960704544A/ko

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Abstract

비인슐린 의존성 당뇨병(NIDDM : noninuslin-dependent diabetes mellitus) 및 그에 따르는 합병증을 예방 또는 지체시키기 위해 티아졸리디논 유도체 및 관련 항과다혈증제를 사용하여 손상된 글루코스 내성을 앓고있는 환자를 치료하기 위한 신규의 치료방법이 개시되어 있다.

Description

비인슐린 의존성 당뇨병(NIDDM)의 개시를 예방 또는 지체시키기 위한 티아졸리딘디온의 용도[USE OF THIAZOLIDINEDIONES TO PREVENT OR DELAY ONSET OF NIDDM]
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음

Claims (23)

  1. 환자에게 치료학적 유효량의 하기식 Ⅰ의 화합물 및 약학적으로 허용가능한 그의 염을 투여함을 특징으로 하는 비인슐린 의존성 당뇨병(diabetes mellitus)의 개시를 예방 또는 지체시키기 위한 손상된 글루코스 내성의 치료방법 :
    (식 중, R1및 R2은 동일 또는 상이하며 각각 수소 원자 또는 C1-C5알킬기이며, R3은 수소 원자, C1-C6지방족 아실기, 지방족 고리 아실기, 방향족 아실기, 헤테로고리 아실기, 아르지방족 아실기, (C1-C6알콕시)카르보닐기, 또는 아르알킬옥시카르보닐기이며; R4및 R5는 동일 또는 상이하며 각각 수소 원자, C1-C5알킬기 또는 C1-C5알콕시기, 또는 R4은 R5와 함께 C1-C4알킬렌디옥시기이며; n은 1, 2 또는 3이며; W은 -CH2-, >CO, 또는 CO-OR6기(식 중, R6은 R3에 정의한 원자들 또는 기들 중 하나를 나타내며 R3과 동일 또는 상이하다)이며; Y 및 Z는 동일 또는 상이하며 각각 산소 원자 또는 아미노(=NH)기이다).
  2. 약학적으로 허용가능한 부형제, 희석제, 또는 담체와 혼합하여 제1항에 따른 혼합물의 치료학적 유효량을 투여함을 특징으로 하는 비인슐린 의존성 당뇨병의 개시를 예방 또는 지체시키기 위한 손상된 글루코스 내성의 치료방법.
  3. 제2항에 있어서, 상기 질환을 앓고 있는 환자에게 Y 및 Z가 산소인 일반식 Ⅰ의 화합물의 치료학적 유효량을 투여함을 특징으로 하는 치료방법.
  4. 제2항에 있어서, 상기 질환을 앓고 있는 환자에게 W가 -CH2-인 일반식 Ⅰ의 화합물의 치료학적 유효량을 투여함을 특징으로 하는 치료방법.
  5. 제2항에 있어서, 상기 질환을 앓고 있는 환자에게 n이 1인 일반식 Ⅰ의 화합물의 치료학적 유효량을 투여함을 특징으로 하는 치료방법.
  6. 제2항에 있어서, 상기 질환을 앓고 있는 환자에게 R1, R2, R4, 및 R5는 저급 알킬이며, R3은 H인 일반식 Ⅰ의 화합물의 치료학적 유효량을 투여함을 특징으로 하는 치료방법.
  7. 제2항에 있어서, 상기 질환을 앓고 있는 환자에게 Z 및 Y는 산소이며, n은 1이며, W는 -CH2-인 일반식 Ⅰ의 화합물의 치료학적 유효량을 투여함을 특징으로 하는 치료방법.
  8. 제2항에 있어서, 상기 질환을 앓고 있는 환자에게 화합물이 (+)-5〔〔4-〔(3,4-디히드로-6-히드록시-2,5,7,8-테트라메틸-2H-1-벤조피란-2-일)메톡시〕페닐〕메틸〕-2,4-티아졸리딘디온인, 일반식 Ⅰ의 화합물의 치료학적 유효량을 투여함을 특징으로 하는 치료방법.
  9. 환자에게 치료학적 유효량의 하기식 Ⅱ의 화합물 또는 약학적으로 허용가능한 그의 염을 투여함을 특징으로 하는 비인슐린 의존성 당뇨병의 개시를 예방 또는 지체시키기 위한 손상된 글루코스 내성의 치료방법 :
    〔식 중, R11은 치환 또는 비치환 알킬, 알콕시, 시클로알킬, 페닐알킬, 페닐, 방향족 아실기, 질소, 산소, 및 황으로 구성된 군으로부터 선택한 1 또는 2개의 헤테로원자를 포함하는 5- 또는 6-원 헤테로고리기 또는 하기 식
    (식 중, R13및 R14은 동일 또는 상이하며 각각 저급 알킬이거나 또는 R13과 R14는 함께 직접으로 또는 질소, 산소, 및 황으로부터 선택한 헤테로 원자에 의해 방해되는 식으로 결합되어 5- 또는 6-원 고리를 형성한다)의 기이며; R12은 단일 결합 또는 저급 알킬렌기이며; L1및 L2는 동일 또는 상이하며 각각 수소 원자, 저급 알킬이거나 또는 L1과 L2은 함께 결합하여 알킬렌기를 형성한다〕.
  10. 약학적으로 허용가능한 부형제, 희석제, 또는 담체와 혼합하여 제9항에 따른 화합물의 치료학적 유효량을 투여함을 특징으로 하는 비인슐린 의존성 당뇨병의 개시를 예방 또는 지체시키기 위한 손상된 글루코스 내성의 치료방법.
  11. 제10항에 있어서, 화합물이 피오글리타존인 일반식 Ⅱ의 화합물의 치료학적 유효량을 투여함을 특징으로 하는 치료방법.
  12. 제10항에 있어서, 화합물이 시글리타존인 일반식 Ⅱ의 화합물의 치료학적 유효량을 투여함을 특징으로 하는 치료방법.
  13. 환자에게 치료학적 유효량의 하기식 Ⅲ의 화합물 및 약학적으로 허용가능한 그의 염을 투여함을 특징으로 하는 비인슐린 의존성 당뇨병의 개시를 예방 또는 지체시키기 위한 손상된 글루코스 내성의 치료방법 :
    (식 중, R15및 R16은 독립적으로 수소, 탄소수 1 내지 6의 저급 알킬, 탄소수 1 내지 6의 알콕시, 할로겐, 에티닐, 니트릴, 메틸티오, 트리플루오로메틸, 비닐, 니트로, 또는 할로겐 치환 벤질옥시이며; n은 0 내지 4이다).
  14. 환자에게 치료학적 유효량의 하기식 Ⅳ의 화합물, 약학적으로 허용가능한 그의 양이온성 염 및 약학적으로 허용가능한 그의 산부가염(화합물이 염기성 질소를 함유하는 경우)을 투여함을 특징으로 하는 비인슐린 의존성 당뇨병의 개시를 예방 또는 지체시키기 위한 손상된 글루코스 내성의 치료방법 :
    (식 중, 점선은 단일 결합 또는 무결합을 나타내며; V는 -CH=CH-, -N=CH-, -CH=N- 또는 S이며; D는 CH2, CHOH, CO, C=NOR17또는 CH=CH이며; X는 S, O, NR18, -CH=N 또는 -N=CH이며; Y는 CH 또는 N이며; Z는 수소, (C1-C7)알킬, (C3-C7)시클로알킬, 페닐, 나프틸, 피리딜, 푸릴, 티에닐, 또는 (C1-C3)알킬, 트리플루오로메틸, (C1-C3)알콕시, 플루오로, 클로로, 또는 브로모로 동일 또는 상이하게 모노-치환 또는 디-치환된 페닐이며; Z1은 수소, 또는 (C1-C3)알킬이며, R17및 R18은 각각 독립적으로 수소 또는 메틸이며; n은 1, 2 또는 3이다).
  15. 환자에게 치료학적 유효량의 하기식 Ⅴ의 화합물, 약학적으로 허용가능한 그의 양이온성 염 및 약학적으로 허용가능한 그의 산부가염(A 또는 B가 N인 경우)을 투여함을 특징으로 하는 비인슐린 의존성 당뇨병의 개시를 예방 또는 지체시키기 위한 손상된 글루코스 내성의 치료방법 :
    (식 중, 점선은 단일 결합 또는 무결합을 나타내며; A 및 B는 각각 독립적으로 CH 또는 N이며(단, A 또는 B가 N일 경우, 다른 하나는 CH이다), X1은 S, SO, SO2, CH|2, CHOH, 또는 CO이며; n은 0 또는 1이며; Y1은 CHR20또는 R21이며(단, n이 1일 경우 Y1은 NR21, X1는 SO2또는 CO이다); Z2은 CHR22, CH2CH2, CH=CH, ,OCH2, SCH2, SOCH2또는 SO2CH2이며, R19, R20, R21및 R22은 각각 독립적으로 수소 또는 메틸이며; X2및 X3는 각각 독립적으로 수소, 메틸, 트리플루오로메틸, 페닐, 벤질, 히드록시, 메톡시, 페녹시, 벤질옥시, 브로모, 클로로 또는 플루오로이다).
  16. 환자에게 치료학적 유효량의 하기식 Ⅵ의 화합물 또는 약학적으로 허용가능한 그의 염을 투여함을 특징으로 하는 비인슐린 의존성 당뇨병의 개시를 예방 또는 지체시키기 위한 손상된 글루코스 내성의 치료방법 :
    (식 중, R23은 탄소수 1 내지 6의 알킬, 탄소수 3 내지 7의 시클로알킬, 페닐 또는 치환체가 독립적으로 탄소수 1 내지 6의 알킬, 탄소수 1 내지 3의 알콕시, 할로겐 또는 트리플루오로메틸인 모노- 또는 디-치환 페닐이다).
  17. 환자에게 치료학적 유효량의 하기식 Ⅶ의 화합물 또는 그의 토오토머형 및/또는 약학적으로 허용가능한 그의 염 및/또는 약학적으로 허용가능한 그의 용매화물을 투여함을 특징으로 하는 비인슐린 의존성 당뇨병의 개시를 예방 또는 지체시키기 위한 손상된 글루코스 내성의 치료방법 :
    (식 중, A2는 알킬기, 치환 또는 비치환 아릴기, 또는 아릴렌 또는 아릴 부분이 치환 또는 비치환될 수 있는 아르알킬기이며; A3은 3 이하의 임의의 치환체를 갖는 벤젠 고리이며; R24는 수소 원자, 알킬기, 아실기, 알킬 또는 아릴 부분이 치환 또는 비치환될 수 있는 아르알킬기, 또는 치환 또는 비치환 아릴기이며; 또는 A2는 R24과 함께 치환 또는 비치환 C2-3폴리메틸렌기이며, 폴리메틸렌기의 임의의 치환체는 알킬 또는 아릴로부터 선택하거나 결합하고 있는 메틸렌 탄소 원자와 함께 인접하는 치환체는 치환 또는 비치환 페닐렌기를 형성하며; R25및 R26은 각각 수소이거나, R25와 R26은 함께 단일 결합을 나타내며; X4는 O 또는 S이며; n은 2 내지 6의 정수이다).
  18. 환자에게 치료학적 유효량의 하기식 Ⅷ의 화합물 또는 그의 토오토머형 및/또는 약학적으로 허용가능한 그의 염 및/또는 약학적으로 허용가능한 그의 용매화물을 투여함을 특징으로 하는 비인슐린 의존성 당뇨병의 개시를 예방 또는 지체시키기 위한 손상된 글루코스 내성의 치료방법 :
    (식 중, R27및 R28는 각각 독립적으로 알킬기, 치환 또는 비치환 아릴기, 또는 아릴 또는 알킬 부분이 치환 또는 비치환된 아르알킬기이며; 또는 R27은 R28과 함께 연결기이며, 연결기는 임의로 치환되는 메틸렌기 및 추가적으로 임의로 치환된 메틸렌기 또는 O 또는 S 원자중의 하나로 구성되며, 상기 메틸렌기의 임의적인 치환체는 알킬, 아릴, 또는 아르알킬로부터 선택되며, 또는 결합하고 있는 탄소 원자와 함께 인접 메틸렌기의 치환체는 치환 또는 비치환 페닐렌기를 형성하며; R29및 R30은 각각 수소, 또는 R29및 R30은 함께 단일 결합이며; A4는 총 3 이하의 임의의 치환체를 갖는 벤젠 고리이며; X5는 O 또는 S이며; n은 2 내지 6의 정수이다).
  19. 환자에게 치료학적 유효량의 하기식 Ⅸ의 화합물 또는 그의 토오토머형 및/또는 약학적으로 허용가능한 그의 염 및/또는 약학적으로 허용가능한 그의 용매화물을 투여함을 특징으로 하는 비인슐린 의존성 당뇨병의 개시를 예방 또는 지체시키기 위한 손상된 글루코스 내성의 치료방법 :
    〔식 중, A5는 치환 또는 비치환 방향족 헤테로시클일기이며; A6은 총 5 이하의 치환체를 갖는 벤젠 고리이며; X6은 O, S, 또는 NR32(식 중, R32은 수소 원자, 알킬기, 아실기, 아릴 부분이 치환 또는 비치환될 수 있는 아르알킬기, 또는 치환 또는 비치환 아릴기이다)이며; Y2는 O 또는 S이며; R31은 알킬, 아르알킬, 또는 아릴기이며; n은 2 내지 6의 정수이다〕.
  20. 환자에게 치료학적 유효량의 하기식 Ⅹ의 화합물 또는 그의 토오토머형 및/또는 약학적으로 허용가능한 그의 염 및/또는 약학적으로 허용가능한 그의 용매화물을 투여함을 특징으로 하는 비인슐린 의존성 당뇨병의 개시를 예방 또는 지체시키기 위한 손상된 글루코스 내성의 치료방법 :
    〔식 중, A7는 치환 또는 비치환 아릴기이며; A8은 총 5 이하의 치환체를 갖는 벤젠 고리이며; X8은 O, S, 또는 NR39(식 중, R39은 수소 원자, 알킬기, 아실기, 아릴 부분이 치환 또는 비치환될 수 있는 아르알킬기, 또는 치환 또는 비치환 아릴기이다)이며; Y3는 O 또는 S이며; R37은 수소 원자이며; R38은 수소 또는 알킬, 아르알킬, 또는 아릴기거나 또는 R37과 함께 단일 결합을 나타내며; n은 2 내지 6의 정수이다〕.
  21. 환자에게 치료학적 유효량의 하기식 ⅩⅠ의 화합물 또는 그의 토오토머형 및/또는 약학적으로 허용가능한 그의 염 및/또는 약학적으로 허용가능한 그의 용매화물을 투여함을 특징으로 하는 비인슐린 의존성 당뇨병의 개시를 예방 또는 지체시키기 위한 손상된 글루코스 내성의 치료방법 :
    (식 중, A1는 치환 또는 비치환 방향족 헤테로시클일기이며; R1은 수소 원자, 알킬기, 아실기, 아릴 부분이 치환 또는 비치환될 수 있는 아르알킬기, 또는 치환 또는 비치환 아릴기이며; A2은 총 5 이하의 치환체를 갖는 벤젠고리이며; n은 2 내지 6의 정수이다).
  22. 환자에게 치료학적 유효량의 하기식 ⅩⅡ 또는 ⅩⅢ의 화합물 또는 약학적으로 허용가능한 그의 염을 투여함을 특징으로 하는 비인슐린 의존성 당뇨병의 개시를 예방 또는 지체시키기 위한 손상된 글루코스 내성의 치료방법 :
    (식들 중, 점선은 단일 결합 또는 무결합이며; R은 탄소수 3 내지 7의 시클로알킬, 나프틸, 티에닐, 푸릴, 페닐 또는 치환체가 탄소수 1 내지 3의 알킬, 탄소수 1 내지 3의 알콕시, 트리플루오로메틸, 클로로, 플루오로 또는 비스(트리플루오로메틸)인 치환된 페닐이며; R1은 탄소수 1 내지 3의 알킬이며; X는 O 또는 C=O이며; A는 O 또는 S이며; B는 N 또는 CH이다).
  23. 환자에게 하기로 구성된 군으로부터 선택한 화합물의 치료학적 유효량을 투여함을 특징으로 하는 비인슐린 의존성 당뇨병의 개시를 예방 또는 지체시키기 위한 손상된 글루코스 내성의 치료방법 : (+)-5-〔〔4-〔(3,4-디히드로-6-히드록시-2,5,7,8-테트라메틸-2H-1-벤조피란-2-일)메톡시〕-페닐〕메틸〕-2,4-티아졸리딘디온 : (트로글리타존); 4-(2-나프틸메틸)-1,2,3,5-옥사티아디아졸-2-옥시드; 5-〔4-〔2-〔N-(벤즈옥사졸-2-일)-N-메틸아미노〕에톡시〕-벤질〕-5-메틸티아졸리딘-2,4-디온; 5-〔4-〔2-〔2,4-디옥소-5-페닐티아졸리딘-3-일)에톡시〕-벤질〕티아졸리딘-2,4-디온; 5-〔4-〔2-〔N-메틸-N-(페녹시카르보닐)아미노〕에톡시〕-벤질〕티아졸리딘-2,4-디온 ; 5-〔4-(2-페녹시에톡시)벤질〕티아졸리딘-2,4-디온; 5-〔4-〔2-(4-클로로페닐)에틸술포닐〕벤질〕-티아졸리딘-2,4-디온; 5-〔4-〔3-(5-메틸-2-페닐옥사졸-4-일)프로피오닐〕-벤질〕티아졸리딘-2,4-디온; 5-〔4-〔(1-메틸시클로헥실)〕메톡시〕-벤질〕티아졸리딘-2,4-디온: (시글리타존); 5-〔〔4-(3-히드록시-1-메틸시클로헥실)메톡시〕벤질〕-티아디아졸리딘-2,4-디온; 5-〔4-〔2-(5-메틸-2-페닐옥사졸-4-일)에톡실〕-벤질〕티아디아졸리디온-2,4-디온; 5-〔4-〔2-(5-에틸피리딘-2-일)에톡실〕벤질〕티아디아졸리딘-2,4-디온: (피오글리타존); 5-〔(2-벤질-2,3-디히드로벤조피란)-5-일메틸〕티아디아졸린-2,4-디온: (엔글리타존); 5-〔〔2-(2-나프틸메틸)벤즈옥사졸〕-5-일메틸〕티아디아졸린-2,4-디온; 5-〔4-〔2-(3-페닐우레이도)에톡실〕벤질〕티아디아졸린-2,4-디온; 5-〔4-〔2-〔N-(벤즈옥사졸-2-일)-N-메틸아미노〕에톡시〕-벤질〕티아디아졸린-2,4-디온; 5-〔2-(5-메틸-2-페닐옥사졸-4-일메틸)-벤조푸란-5-일메틸〕-옥사졸리딘-2,4-디온; 5-〔4-〔2-〔N-메틸-N-(2-피리딜)아미노〕에톡시〕-벤질〕티아졸리딘-2,4-디온; 및 5-〔4-〔2-〔N-(벤즈옥사졸-2-일)-N-메틸아미노〕에톡시〕-벤질〕옥사졸리딘-2,4-디온.
    ※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
KR1019960701336A 1993-09-15 1994-09-14 비인슐린 의존성 당뇨병(niddm)의 개시를 예방 또는 지체시키기 위한 티아졸리딘디온의 용도[use of thiazolidinediones to prevent or delay onset of niddm] KR960704544A (ko)

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US12225193A 1993-09-15 1993-09-15
US08/122,251 1993-09-15
US08293899 US5478852C1 (en) 1993-09-15 1994-08-23 Use of thiazolidinedione derivatives and related antihyperglycemic agents in the treatment of impaired glucose tolerance in order to prevent or delay the onset of noninsulin-dependent diabetes mellitus
US08/293,899 1994-08-23
PCT/US1994/010389 WO1995007694A1 (en) 1993-09-15 1994-09-14 Use of thiazolidinediones to prevent or delay onset of niddm

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KR1019960701318A KR960704546A (ko) 1993-09-15 1994-09-09 인슐린 비의존성 당뇨병으로 진행할 위험이 있는 질병의 치료에 있어서 티아졸리딘디온 유도체 및 관련 고혈당 억제제의 용도(Use of Thiazolidinedione Derivatives and Related Antihyperglycemic Agents in the Treatment of Disease States at Risk for Progressing to Noninsulin-Dependent Diabetes Mellitus)
KR1019960701336A KR960704544A (ko) 1993-09-15 1994-09-14 비인슐린 의존성 당뇨병(niddm)의 개시를 예방 또는 지체시키기 위한 티아졸리딘디온의 용도[use of thiazolidinediones to prevent or delay onset of niddm]

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KR1019960701318A KR960704546A (ko) 1993-09-15 1994-09-09 인슐린 비의존성 당뇨병으로 진행할 위험이 있는 질병의 치료에 있어서 티아졸리딘디온 유도체 및 관련 고혈당 억제제의 용도(Use of Thiazolidinedione Derivatives and Related Antihyperglycemic Agents in the Treatment of Disease States at Risk for Progressing to Noninsulin-Dependent Diabetes Mellitus)

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HU9600674D0 (en) 1996-05-28
EP0719143B1 (en) 2000-12-13
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HK1085134A1 (en) 2006-08-18
DE69435328D1 (de) 2011-01-13
GR3035430T3 (en) 2001-05-31
AU678291B2 (en) 1997-05-22
NO961052D0 (no) 1996-03-14
DK1637138T3 (da) 2011-05-23
DE69435039T2 (de) 2008-08-14
NO961052L (no) 1996-03-14
ATE198045T1 (de) 2000-12-15
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DE69426421D1 (de) 2001-01-18
PT1637138E (pt) 2011-02-22
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WO1995007697A2 (en) 1995-03-23
JPH09502722A (ja) 1997-03-18
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CZ72296A3 (en) 1996-10-16
US5478852A (en) 1995-12-26
US5602133A (en) 1997-02-11
AU7724994A (en) 1995-04-03
WO1995007697A3 (en) 1995-05-11
CZ282296A3 (cs) 1998-01-14
DK0719143T3 (da) 2001-03-05
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PT719140E (pt) 2008-01-17
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CN1131391A (zh) 1996-09-18
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US5457109A (en) 1995-10-10
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EP1637138B1 (en) 2010-12-01
PT719143E (pt) 2001-03-30
US5478852C1 (en) 2001-03-13
EP1637138A2 (en) 2006-03-22
CN1106195C (zh) 2003-04-23
CZ282396A3 (cs) 1998-01-14
RU2281094C2 (ru) 2006-08-10
DE69426421T2 (de) 2001-04-19

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