KR950701928A - 비정상적인 칼슘 및 인산염 대사를 치료하기 위한 티오-치환된 환상 포스포네이트 화합물(thio-substituted cyclic phosphonate compounds, for treating abnormal calcium and phosphate metabolism) - Google Patents

비정상적인 칼슘 및 인산염 대사를 치료하기 위한 티오-치환된 환상 포스포네이트 화합물(thio-substituted cyclic phosphonate compounds, for treating abnormal calcium and phosphate metabolism)

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KR950701928A
KR950701928A KR1019940704306A KR19940704306A KR950701928A KR 950701928 A KR950701928 A KR 950701928A KR 1019940704306 A KR1019940704306 A KR 1019940704306A KR 19940704306 A KR19940704306 A KR 19940704306A KR 950701928 A KR950701928 A KR 950701928A
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수잔 메리 카스
프랭크 할록 에베티노
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제이코버스 코넬리스 레이서
프록터 앤드 갬블 파마슈티칼즈 인코포레이티드
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Abstract

본 발명은 비스포스포네이트, 포스포노알킬포스피네이트, 포스포노카복실레이트 및 포스포노설포네이트를 포함하는 티오-치환된 환상 포스포네이트 화합물, 및 이들의 약학적으로 허용가능한 염 및 에스테르에 관한 것이다. 본 발명은 또한 안전하고 효과적인 양의 본 발명 화합물 및 약학적으로 허용가능한 부형제를 함유하는 약학 조성물에 관한 것이다. 마지막으로, 본 발명은 골가공증 및 관절염, 특히 류마티스성 관절염 및 골관절염을 치료 또는 예방하는 것을 포함하는, 인간 또는 다른 포유동물에서 비정상적인 칼슘 및 인산염 대사를 특징으로 하는 병리학적 상태를 치료 또는 예방하기 위한 방법에 관한 것이다. 이 방법은 안전하고 효과적인 양의 본 발명 화합물 또는 조성물을 이렇게 치료해야 할 인간 또는 기타 포유동물에게 투여하는 것을 포함한다. 이들 화합물은 단일환상 또는 이중환상일 수 있으며, 하기 일반 구조(Ⅰ)(단, R1, R2및 R3중 적어도 하나는 SR6또는 R8SR6임)를 갖는다;

Description

비정상적인 칼슘 및 인산염 대사를 치료하기 위한 티오-치환된 환상 포스포네이트 화합물(THIO-SUBSTITUTED CYCLIC PHOSPHONATE COMPOUNDS, FOR TREATING ABNORMAL CALCIUM AND PHOSPHATE METABOLISM)
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음

Claims (15)

  1. 하기 일반 구조를 갖는 것을 특징으로 하는, 칼슘 및 인산염 대사의 질환을 치료 또는 예방하는데 유용한 신규한 환상 티오-치환된 포스포네이트, 및 이들의 약학적으로 허용가능한 염 및 에스테르;
    상기 식에서, (a)X및 Y는 존재하지 않거나, 산소, 황, 또는 질소로부터 독립적으로 선택되고; (b)R은 PO3H2또는 P(0)(OH)R4(여기에서, R4는 비치환 또는 치환된 C1-C8알킬임), 바람직하게는 PO3H2이고; (c)m 및 n은 0내지 5의 정수이고, m+n은 0내지 5이며; (d)p및 q는 0내지 3의 정수이고, p+a는 0내지 3이며; (e)s는 0내지 2의 정수이고, X가 존재하지 않고 m+n이 0인 경우 s는 2이며; (f)각 R1은 존재하지 않거나, -SR6; R8SR6; 수소; 비치환 또는 치환된 C1-C8알킬; 비치환 또는 치환된 아릴; 하이드록시; 아미도; 알콕시; -CO2R3; -O2CR3; -NR3 2; -N(R3)C(0)R3; -OR3; -C(0)N(R3)2; 비치환 또는 치환된 벤질; 니트로; 또는 이들의 조합으로부터 독립적으로 선택되며; (h)R3는 수소; 비치환 또는 치환된 C1-C8알킬; 또는 R8SR6으로부터 독립적으로 선택되고; (i)R6는 H; -C(0)R7; -C(S)R7; C(0)N(R7)2; C(S)N(R7)2, C(0)OR7; 또는 C(S)OR7(여기에서, R7은 수소, 또는 비치환 또는 치환된 C1-C8알킬임)로부터 선택되고; (j)R8은 비치환 또는 치환된 C1-C8알킬이고; 단, R1, R2및 R3중 적어도 하나는 SR6또는 R8SR8이다.
  2. 제1항에 있어서, X가 존재하지 않고, m+n이 0이고, s가 2인 단일환상 포스포네이트 화합물.
  3. 제1항 또는 제2항에 있어서, Y가 둘다 존재하지 않는 단일환상 탄소환상 화합물.
  4. 제1항 내지 제3항중 어느 한 항에 있어서, X가 존재하지 않고, m+n이 1내지 3이며, Y가 둘다 존재하지 않는 다중환상 탄소환상 화합물.
  5. 제1항 내지 제4항중 어느 한 항에 있어서, Y가 0,S 또는 N인 단일환상 헤테로환상 화합물.
  6. 제1항 내지 제5항중 어느 한 항에 있어서, X와 Y중 하나가 0, S또는 N이고 m+n이 1내지 3인 다중환상 헤테로환상 화합물.
  7. 안전하고 효과적인 양의 제1항 내지 제6항중 어느 한 항에 따른 화합물, 및 0내지 2%향미제; 0내지 50%보조용매; 0내지 5%완충 시스템; 0내지 276 계면활성재; 0내지 2%보존제; 0내지 5% 감미제; 0내지 5% 점도조절제; 75% 이하의 충진제; 0.5내지 2%윤활제; 1 내지 5% 활주제; 4 내지 15%붕괴제; 및 1내지 10% 결합제로 이루어진 군으로부터 선택된 약학적으로 허용가능한 부형제를 포함하는 것을 특징으로 하는 비정상적인 칼슘 및 인산염 대사의 질환을 치료하는데 유용한 약학조성물.
  8. 안전하고 효과적인 양의 제1항 내지 제6항중 어느 한 항에 따른 화합물을 치료해야 할 인간 또는 기타 포유동물에게 투여하는 것으로 이루어짐을 특징으로 하는 비정상적인 칼슘 및 인산염 대사에 관련된 질환을 치료 또는 예방하는 약제를 제조하기 위한 제1항 내지 제6항중 어느 한 항에 따른 상기 화합물의 용도.
  9. 안전하고 효과적인 양의 제1항 내지 제6항중 어느 한 항에 따른 화합물을 치료해야 할 인간 또는 기타 포유동물에게 투여하는 것으로 이루어짐을 특징으로 하는 골다공증을 치료 또는 예방하는 약제를 제조하기 위한 제1항 내지 제7항중 어느 한 항에 따른 상기 화합물의 용도.
  10. 안전하고 효과적인 양의 제1항 내지 제6항중 어느 한 항에 따른 화합물을 치료해야 할 인간 또는 기타 포유동물에게 투여하는 것으로 이루어짐을 특징으로 하는 관절염을 치료 또는 예방하는 약재를 제조하기 위한 제1항 내지 제6항중 어느 한 항에 따른 상기 화합물의 용도.
  11. 안전하고 효과적인 양의 제1항에 따른 화합물을 치료해야 할 인간 또는 기타 포유동물에게 투여하는 비정상적인 칼슘 및 인산염 대사에 관련된 질환을 치료 또는 예방하는 방법.
  12. 제11항에 있어서, 상기 인간 또는 기타 포유동물이 골다공증에 걸린 방법.
  13. 제11항에 있어서, 상기 인간 또는 기타 포유동물이 관절염에 걸린 방법.
  14. 제11항에 있어서, 상기 인간 또는 기타 포유동물이 관절염에 걸린 방법.
  15. 제11항에 있어서, 상기 인간 또는 기타 포유동물이 류마티스성 관절염에 걸린 방법.
    ※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
KR1019940704306A 1992-05-29 1993-05-26 비정상적인 칼슘 및 인산염 대사를 치료하기 위한 티오-치환된 환상 포스포네이트 화합물 KR100268696B1 (ko)

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US89088692A 1992-05-29 1992-05-29
US07/890886 1992-05-29
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US08/052,696 1993-04-30
US08/052696 1993-04-30
US08/052,696 US5763611A (en) 1992-05-29 1993-04-30 Thio-substituted cyclic phosphonate compounds, pharmaceutical compositions, and methods for treating abnormal calcium and phosphate metabolism
PCT/US1993/004978 WO1993024497A1 (en) 1992-05-29 1993-05-26 Thio-substituted cyclic phosphonate compounds for treating abnormal calcium and phosphate metabolism

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CZ296594A3 (en) 1995-09-13
NO944500L (no) 1995-01-27
NO305959B1 (no) 1999-08-23
IL105833A (en) 1998-10-30
EP0642520A1 (en) 1995-03-15
CA2136822A1 (en) 1993-12-09
CN1044912C (zh) 1999-09-01
JPH07507316A (ja) 1995-08-10
FI945594A (fi) 1994-11-28
WO1993024497A1 (en) 1993-12-09
CA2136822C (en) 2000-12-05
US5763611A (en) 1998-06-09
MY108868A (en) 1996-11-30
NZ253525A (en) 1996-05-28
KR100268696B1 (ko) 2000-11-01
AU4391893A (en) 1993-12-30
HUT69729A (en) 1995-09-28
AU664761B2 (en) 1995-11-30
SG47593A1 (en) 1998-04-17
CN1086821A (zh) 1994-05-18
HU9403413D0 (en) 1995-02-28
FI945594A0 (fi) 1994-11-28
SK144394A3 (en) 1995-07-11
MX9303252A (es) 1994-05-31
NO944500D0 (no) 1994-11-24
IL105833A0 (en) 1993-09-22

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