公开(公告)号：KR101335055B1

公开(公告)日：2013-12-02

申请号：KR1020077022813

申请日：2006-04-03

Applicant: 아스트라제네카 아베

Inventor： 노르드발,군나르 ,  레이,콜린 ,  라인,토비아스 ,  손,다니엘

IPC: C07D513/04 ,  A61K31/519 ,  A61P11/00 ,  A61P9/10

CPC classification number: C07D513/04

Abstract: 본 발명은 화학식 I의 신규한 5-치환된 7-아미노[1,3]티아졸로[4,5-d]피리미딘 유도체, 및 그의 제약상 허용되는 염을, 그의 제조 방법, 그를 포함하는 제약 조성물 및 치료에 있어서의 그의 용도와 함께 개시한다. 화학식 I의 화합물은 CX
3 CR1 수용체 길항제이며, 따라서 신경변성 장애, 탈수초 질환, 심혈관 및 뇌혈관 아테롬성 동맥경화성 장애, 말초 동맥 질환, 류마티스 관절염, 폐 질환, 예컨대 COPD, 천식 또는 통증을 치료하거나 예방하는데 특히 유용한 치료제이다.


식 중에서,
R
1 , R
2 , R
3 , R
4 및 R
5 는 명세서에서 정의된 바와 같다.
5-치환된 7-아미노[1,3]티아졸로[4,5-d]피리미딘 유도체, 케모킨, CX3CR1 수용체 길항제, 아테롬성 동맥경화증

公开(公告)号：KR1020080059285A

公开(公告)日：2008-06-26

申请号：KR1020087010753

申请日：2006-10-02

Applicant: 아스트라제네카 아베

Inventor： 아르비드손,페르1세 ,  아르젤,에르완 ,  버로우스,제레미 ,  클래손,마르티나 ,  레이,콜린 ,  라인,토비아스 ,  로티씨,디디에르 ,  쇠데르만,페터

IPC: C07D471/04 ,  A61K31/437 ,  A61K31/444 ,  A61P19/08

CPC classification number: C07D471/04

Abstract: The present invention relates to new compounds of formula (I) Wherein X is or Y; as a free base or a pharmaceutically acceptable salt, solvate or solvate of salt thereof, a process for their preparation and new intermediates used therein, pharmaceutical formulations containing said therapeutically active compounds and to the use of said active compounds in therapy.

Abstract translation: 本发明涉及新的式（I）化合物，其中X是或Y; 作为其盐的游离碱或其药学上可接受的盐，溶剂化物或溶剂化物，其制备方法和其中使用的新中间体，含有所述治疗活性化合物的药物制剂和所述活性化合物在治疗中的用途。

公开(公告)号：KR1020080004483A

公开(公告)日：2008-01-09

申请号：KR1020077022813

申请日：2006-04-03

Applicant: 아스트라제네카 아베

Inventor： 노르드발,군나르 ,  레이,콜린 ,  라인,토비아스 ,  손,다니엘

IPC: C07D513/04 ,  A61K31/519 ,  A61P11/00 ,  A61P9/10

CPC classification number: C07D513/04

Abstract: There are disclosed novel 5-substituted 7-amino-[1,3]thiazolo[4,5-d] pyrimidine derivatives of formula (I) wherein R1, R2, R3, R4 and R5 are as defined in the specification, and pharmaceutically acceptable salts thereof, together with processes for their preparation, pharmaceutical compositions comprising them and their use in therapy. The compounds of formula (I) are CX3CR1 receptor antagonists and are thereby particularly useful in the treatment or prophylaxis of neurodegenerative disorders, demyelinating disease, cardio-and cerebrovascular atherosclerotic disorders, peripheral artery disease, rheumatoid arthritis, pulmonary diseases such as COPD, asthma or pain.

Abstract translation: 公开了式（I）的新的5-取代的7-取代的7-氨基 - [1,3]噻唑并[4,5-d]嘧啶衍生物，其中R 1，R 2，R 3，R 4和R 5如说明书中所定义， 其可接受的盐及其制备方法，包含它们的药物组合物及其在治疗中的用途。 式（I）化合物是CX3CR1受体拮抗剂，因此特别可用于治疗或预防神经变性疾病，脱髓鞘疾病，心血管和脑血管动脉粥样硬化疾病，外周动脉疾病，类风湿性关节炎，肺疾病如COPD，哮喘或 疼痛。

公开(公告)号：KR1020080004484A

公开(公告)日：2008-01-09

申请号：KR1020077022814

申请日：2006-04-03

Applicant: 아스트라제네카 아베

Inventor： 노르드발,군나르 ,  레이,콜린 ,  라인,토비아스 ,  손,다니엘

IPC: C07D513/04 ,  A61K31/519

CPC classification number: C07D413/04

Abstract: There are disclosed novel 5,7-disubstituted [1,3]thiazolo[4,5-d] pyrimidin-2(3H)-one derivatives of formula (I) [Chemical formula should be inserted here. Please see paper copy] wherein R1, R 2, R3, R4 and R5 are as defined in the specification, and pharmaceutically acceptable salts thereof, together with processes for their preparation, pharmaceutical compositions comprising them and their use in therapy. The compounds of formula (I) are CX3CR1 receptor antagonists and are thereby particularly useful in the treatment or prophylaxis of neurodegenerative disorders, demyelinating disease, cardio-and cerebrovascular atherosclerotic disorders, peripheral artery disease, rheumatoid arthritis, pulmonary diseases such as COPD, asthma or pain.

Abstract translation: 公开了式（I）的新的5,7-二取代[1,3]噻唑并[4,5-d]嘧啶-2（3H） - 酮衍生物[在此应插入化学式。 请参见论文复制]，其中R1，R2，R3，R4和R5如说明书中所定义，及其药学上可接受的盐及其制备方法，包含它们的药物组合物及其在治疗中的应用。 式（I）化合物是CX3CR1受体拮抗剂，因此特别可用于治疗或预防神经变性疾病，脱髓鞘疾病，心血管和脑血管动脉粥样硬化疾病，外周动脉疾病，类风湿性关节炎，肺疾病如COPD，哮喘或 疼痛。