KR100781864B1 - 트리아졸로(4,5-d)피리미딘 화합물의 신규 결정형 및비결정형 - Google Patents
트리아졸로(4,5-d)피리미딘 화합물의 신규 결정형 및비결정형 Download PDFInfo
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Abstract
Description
Claims (32)
- 하기 X-선 분말 회절 패턴들에 의해 특징지워지는, 결정형인 하기 화학식 I의 화합물.<화학식 I>5.3°(±0.1°), 20.1°(±0.1°), 20.7°(±0.1°), 21.0°(±0.1°) 및 21.3°(±0.1°) 2θ에서 고강도의 특정 피이크를 함유하는 X-선 분말 회절 패턴;5.5°(±0.1°), 13.5°(±0.1°), 18.3°(±0.1°), 22.7°(±0.1°) 및 24.3°(±0.1°) 2θ에서 고강도의 특정 피이크를 함유하는 X-선 분말 회절 패턴;14.0°(±0.1°), 17.4°(±0.1°), 18.4°(±0.1°), 21.4°(±0.1°) 및 24.1°(±0.1°) 2θ에서 고강도의 특정 피이크를 함유하는 X-선 분말 회절 패턴; 및4.9°(±0.1°), 9.2°(±0.1°), 11.6°(±0.1°), 15.6°(±0.1°) 및 16.4°(±0.1°) 2θ에서 고강도의 특정 피이크를 함유하는 X-선 분말 회절 패턴.
- 제1항에 있어서, 화합물 분자 당 0.4 미만의 물 분자를 가지는 무수 형태로 존재하는 화학식 I의 화합물.
- 제1항에 있어서, 5.3°(±0.1°), 20.1°(±0.1°), 20.7°(±0.1°), 21.0°(±0.1°) 및 21.3°(±0.1°) 2θ에서 고강도의 특정 피이크를 함유하는 X-선 분말 회절 패턴에 의해 특징지워지는 화학식 I의 화합물.
- 제1항 또는 3항에 있어서, 5.3°(±0.1°), 8.0°(±0.1°), 9.6°(±0.1°), 13.9°(±0.1°), 15.3°(±0.1°), 20.1°(±0.1°), 20.7°(±0.1°), 21.0°(±0.1°), 21.3°(±0.1°), 26.2°(±0.1°) 및 27.5°(±0.1°) 2θ에서 특정 피이크를 함유하는 X-선 분말 회절 패턴에 의해 특징지워지는 화학식 I의 화합물.
- 제1항 또는 제3항에 있어서, 146 - 152 ℃ 범위 내의 용융 개시점을 갖는 시차 주사 열량측정 곡선에 의해 특징지워지는 화학식 I의 화합물.
- 제1항에 있어서, 5.5°(±0.1°), 13.5°(±0.1°), 18.3°(±0.1°), 22.7°(±0.1°) 및 24.3°(±0.1°) 2θ에서 고강도의 특정 피이크를 함유하는 X-선 분말 회절 패턴에 의해 특징지워지는 화학식 I의 화합물.
- 제1항 또는 6항에 있어서, 5.5°(±0.1°), 6.8°(±0.1°), 10.6°(±0.1°), 13.5°(±0.1°), 14.9°(±0.1°), 18.3°(±0.1°), 19.2°(±0.1°), 22.7°(±0.1°), 24.3°(±0.1°) 및 27.1°(±0.1°) 2θ에서 특정 피이크를 함유하는 X-선 분말 회절 패턴에 의해 특징지워지는 화학식 I의 화합물.
- 제1항 또는 제6항에 있어서, 136 - 139 ℃ 범위 내의 용융 개시점을 갖는 시차 주사 열량측정 곡선에 의해 특징지워지는 화학식 I의 화합물.
- 제1항에 있어서, 14.0°(±0.1°), 17.4°(±0.1°), 18.4°(±0.1°), 21.4°(±0.1°) 및 24.1°(±0.1°) 2θ에서 고강도의 특정 피이크를 함유하는 X-선 분말 회절 패턴에 의해 특징지워지는 화학식 I의 화합물.
- 제1항 또는 9항에 있어서, 5.6°(±0.1°), 12.5°(±0.1°), 14.0°(±0.1°), 17.4°(±0.1°), 18.4°(±0.1°), 21.4°(±0.1°), 22.2°(±0.1°), 22.9°(±0.1°), 24.1°(±0.1°) 및 24.5°(±0.1°) 2θ에서 특정 피이크를 함유하는 X-선 분말 회절 패턴에 의해 특징지워지는 화학식 I의 화합물.
- 제1항 또는 제9항에 있어서, 127 - 132 ℃ 범위 내의 용융 개시점을 갖는 시차 주사 열량측정 곡선에 의해 특징지워지는 화학식 I의 화합물.
- 제1항에 있어서, 4.9°(±0.1°), 9.2°(±0.1°), 11.6°(±0.1°), 15.6°(±0.1°) 및 16.4°(±0.1°) 2θ에서 고강도의 특정 피이크를 함유하는 X-선 분말 회절 패턴에 의해 특징지워지는 화학식 I의 화합물.
- 제1항 또는 12항에 있어서, 4.9°(±0.1°), 6.0°(±0.1°), 9.2°(±0.1°), 11.6°(±0.1°), 12.8°(±0.1°), 15.6°(±0.1°), 16.4°(±0.1°), 17.2°(±0.1°) 및 18.1°(±0.1°) 2θ에서 특정 피이크를 함유하는 X-선 분말 회절 패턴에 의해 특징지워지는 화학식 I의 화합물.
- 제1항 또는 제12항에 있어서, 약 139 ℃에서 용융 개시점을 갖는 시차 주사 열량측정 곡선에 의해 특징지워지는 화학식 I의 화합물.
- 제6항에 청구된 화학식 I의 화합물 및 제9항에 청구된 화학식 I의 화합물의 혼합물.
- 화학식 I의 화합물이 에탄올, 에틸 아세테이트, 이소-프로판올, 이소-옥탄, 아세토니트릴, 물 또는 그의 혼합물로 이루어진 군에서 선택된 용매로부터 결정화되는, 제1항에 청구된 화합물의 제조 방법.
- 삭제
- 제18항에 있어서, 용매가 메탄올 및 물의 혼합물, 에탄올, 에틸 아세테이트, 에탄올 및 물의 혼합물, 이소-프로판올 및 물의 혼합물, 에틸 아세테이트 및 이소-옥탄의 혼합물, 및 아세토니트릴로 이루어진 군에서 선택되는 방법.
- 용매가 메탄올 및 물의 혼합물인 제18항 또는 제20항에 따른, 제3항에 청구된 화합물의 제조 방법.
- 종결정을 이용하는 제3항에 청구된 화합물의 제조 방법.
- 제22항에 있어서, 종결정이 제6항에 청구된 화합물을 용융시킴으로써 제조되는 것인 방법.
- 용매가 에틸 아세테이트인 제18항 또는 제20항에 따른, 제6항에 청구된 화합물의 제조 방법.
- 용매가 에탄올 또는 이소프로필 알코올인 제18항 또는 제20항에 따른, 제9항에 청구된 화합물의 제조 방법.
- 화학식 I의 화합물을 5 내지 65 ℃의 온도에서 이소프로필 알코올(IPA)/물 용매계에서 슬러리화하는 것을 포함하는, 제9항에 청구된 화합물의 제조 방법.
- 용매가 아세토니트릴인 제18항 또는 제20항에 따른 방법을 포함하는, 제12항에 청구된 화합물의 제조 방법.
- 삭제
- 삭제
- 관상 동맥, 대뇌혈관 또는 말초 혈관 질환을 가진 환자에서의 동맥 혈전성 합병증을 예방하기 위한 제1항 내지 제3항 중 어느 한 항에 청구된 화합물을 포함하는 제약 조성물.
- 삭제
- 삭제
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Application Number | Priority Date | Filing Date | Title |
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GBGB0013407.2A GB0013407D0 (en) | 2000-06-02 | 2000-06-02 | Forms of a chemical compound |
GB0013407.2 | 2000-06-02 | ||
PCT/SE2001/001239 WO2001092262A1 (en) | 2000-06-02 | 2001-05-31 | New crystalline and amorphous form of a triazolo(4,5-d)pyrimidine compound |
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TWI229674B (en) | 1998-12-04 | 2005-03-21 | Astra Pharma Prod | Novel triazolo[4,5-d]pyrimidine compounds, pharmaceutical composition containing the same, their process for preparation and uses |
GB0013488D0 (en) * | 2000-06-02 | 2000-07-26 | Astrazeneca Ab | Chemical compound |
GB0013407D0 (en) * | 2000-06-02 | 2000-07-26 | Astrazeneca Ab | Forms of a chemical compound |
JP4298212B2 (ja) * | 2002-03-29 | 2009-07-15 | 大日本印刷株式会社 | 塩酸エピナスチン高融点型結晶の製造法 |
WO2008024044A1 (en) * | 2006-08-21 | 2008-02-28 | Astrazeneca Ab | Compositions, suitable for oral administration, comprising a triazolo [4, 5] pyrimidin derivate |
TWI482772B (zh) * | 2006-08-21 | 2015-05-01 | Astrazeneca Ab | 適合口服且包含三唑并[4,5-d]嘧啶衍生物之組合物 |
CA2668180A1 (en) * | 2006-10-31 | 2008-05-08 | Janssen Pharmaceutica N.V. | Triazolopyrimidine derivatives as adp p2y12 receptor antagonists |
US20080254036A1 (en) * | 2007-04-13 | 2008-10-16 | Millennium Pharmaceuticals, Inc. | Combination anticoagulant therapy with a compound that acts as a factor xa inhibitor |
TWI496776B (zh) * | 2007-11-15 | 2015-08-21 | Astrazeneca Ab | 製備(3aR,4S,6R,6aS)-6-胺基-2,2-二甲基四氫-3aH-環戊并[d][1,3]二氧雜環戊烯-4-醇之純非對映異構性之二苯甲醯-L-酒石酸鹽之方法 |
UA100864C2 (uk) * | 2007-12-03 | 2013-02-11 | Астразенека Аб | Спосіб лікування або запобігання аневризмі черевної аорти |
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