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1. 发明申请

WO1997003084A1 NEW INHIBITORS OF PLATELET AGGREGATION 审中-公开
标题翻译：新的抑制剂聚集
公开(公告)号：WO1997003084A1
公开(公告)日：1997-01-30
申请号：PCT/SE1996000911
申请日：1996-07-04
申请人： ASTRA PHARMACEUTICALS LTD. , ASTRA AKTIEBOLAG , COX, David , INGALL, Anthony , WILLIS, Paul
发明人： ASTRA PHARMACEUTICALS LTD. , ASTRA AKTIEBOLAG
IPC分类号： C07H19/16
CPC分类号： C07D487/04 , C07H19/06
摘要： Compounds of formula (I), wherein B is O or CH2; X is selected from NR R , SR , and C1-C7 alkyl; Y is selected from SR NR R , and C1-C7 alkyl; R and R are each and independently selected from H, or C1-C7 alkyl optionally substituted upon or within the alkyl chain by one or more of O, S, N or halogen; R and R are both H, or R and R together form a bond; A is COOH, C(O)NH(CH2)pCOOH, C(O)N[(CH2)qCOOH]2; C(O)NHCH(COOH)(CH2)rCOOH, or 5-tetrazolyl, wherein p, q and r are each and independently 1, 2, or 3; as well as pharmaceutically acceptable salts and prodrugs thereof, pharmaceutical compositions comprising the novel compounds and use of the compounds in therapy. Also within the scope of the invention are novel intermediates to the novel compounds. The novel compounds are in particular useful in the prevention of platelet aggregation.
摘要翻译：式（I）化合物，其中B为O或CH 2; X选自NR 1 R 2，SR 1和C 1 -C 7烷基; Y选自SR 1 NR 1 R 2和C 1 -C 7烷基; R 1和R 2各自独立地选自H或在烷基链上或在烷基链上被O，S，N或卤素中的一个或多个取代的C 1 -C 7烷基; R 3和R 4都是H，R 3或R 3和R 4一起形成键; A是COOH，C（O）NH（CH 2）p COOH，C（O）N [（CH 2）q COOH] 2; C（O）NHCH（COOH）（CH 2）r COOH，或5-四唑基，其中p，q和r各自独立地为1,2或3; 以及其药学上可接受的盐和前药，包含新化合物的药物组合物和化合物在治疗中的用途。在本发明范围内也是新化合物的新中间体。新型化合物特别可用于预防血小板聚集。

2. 发明申请

WO1998028300A1 TRIAZOLO[4,5-D]PYRIMIDINYL DERIVATIVES AND THEIR USE AS MEDICAMENTS 审中-公开
标题翻译：三唑并[4,5-D]吡啶衍生物及其作为药物使用
公开(公告)号：WO1998028300A1
公开(公告)日：1998-07-02
申请号：PCT/SE1997002091
申请日：1997-12-12
申请人： ASTRA PHARMACEUTICALS LTD. , ASTRA AKTIEBOLAG , BONNERT, Roger , INGALL, Anthony , SPRINGTHORPE, Brian , WILLIS, Paul
发明人： ASTRA PHARMACEUTICALS LTD. , ASTRA AKTIEBOLAG
IPC分类号： C07D487/04
CPC分类号： C07D487/04
摘要： The invention relates to triazolo[4,5-d]pyrimidin-3-yl derivatives of formula (I), which are useful in the treatment of platelet aggregation disorders.
摘要翻译：本发明涉及式（I）的三唑并[4,5-d]嘧啶-3-基衍生物，其可用于治疗血小板聚集障碍。

3. 发明申请

WO1998028301A1 PYRROLO[3,4-D]PYRIMIDINONE DERIVATIVES AND THEIR USE AS MEDICAMENTS 审中-公开
标题翻译： PYRROLO [3,4-D]嘧啶酮衍生物及其作为药物使用
公开(公告)号：WO1998028301A1
公开(公告)日：1998-07-02
申请号：PCT/SE1997002157
申请日：1997-12-18
申请人： ASTRA PHARMACEUTICALS LTD. , ASTRA AKTIEBOLAG , COOPER, Martin , CHESHIRE, David , DONALD, David , FURBER, Mark , PERRY, Matthew , HARRISON, Richard , TOMKINSON, Nicholas
发明人： ASTRA PHARMACEUTICALS LTD. , ASTRA AKTIEBOLAG
IPC分类号： C07D487/04
CPC分类号： C07D487/04
摘要： The invention provides certain novel 5-substituted pyrrolo[3,4-d]pyrimidine-2,4-diones according to general formula (I), processes for their preparation, pharmaceutical compositions containing them, a process for preparing the pharmaceutical compositions, and methods of treatment involving their use.
摘要翻译：本发明提供了一些根据通式（I）的5-取代吡咯并[3,4-d]嘧啶-2,4-二酮，其制备方法，含有它们的药物组合物，制备该药物组合物的方法和涉及其使用的治疗方法。

4. 发明申请

WO1998009969A1 NOVEL ARYL-PYRIDAZINES 审中-公开
标题翻译：新亚美尼亚
公开(公告)号：WO1998009969A1
公开(公告)日：1998-03-12
申请号：PCT/SE1997001359
申请日：1997-08-19
申请人： ASTRA PHARMACEUTICALS LTD. , ASTRA AKTIEBOLAG , BANTICK, John , HIRST, Simon , PERRY, Matthew , PHILLIPS, Eifion
发明人： ASTRA PHARMACEUTICALS LTD. , ASTRA AKTIEBOLAG
IPC分类号： C07D491/052
CPC分类号： C07D495/04 , C07D231/54 , C07D237/26 , C07D237/36 , C07D471/04 , C07D491/04 , C07D491/14 , C07D495/14
摘要： Use of a compound of formula (I) wherein, A, A , A and A are all CH or CR or one of A, A , A or A is nitrogen and the others are all CH or CR ; Ar and Ar are independently phenyl, pyridyl, benzothiazolyl, quinolyl or quinoxalinyl all of which are optionally substituted by one or more substituents, X, Y, Z, R , R , R , R are as described in the specification or a pharmaceutically acceptable derivative thereof in the manufacture of a medicament for the treatment of an allergic or an inflammatory condition.
摘要翻译：其中A，A 1，A 2和A 3的式（I）化合物均为CH或CR 4或A，A 1，A 2或 A 3为氮，其余为CH或CR 4; Ar 1和Ar 2独立地是苯基，吡啶基，苯并噻唑基，喹啉基或喹喔啉基，它们全部被一个或多个取代基X，Y，Z，R 1，R 2， 3>，R 4如说明书或其药学上可接受的衍生物所述，用于制备用于治疗过敏或炎性疾病的药物。

5. 发明申请

WO1998001449A1 NOVEL COMPOUNDS 审中-公开
标题翻译：新型化合物
公开(公告)号：WO1998001449A1
公开(公告)日：1998-01-15
申请号：PCT/SE1997001219
申请日：1997-07-04
申请人： ASTRA PHARMACEUTICALS LTD. , ASTRA AKTIEBOLAG , BANTICK, John , PERRY, Matthew , THORNE, Philip
发明人： ASTRA PHARMACEUTICALS LTD. , ASTRA AKTIEBOLAG
IPC分类号： C07D487/04
CPC分类号： C07D491/04 , C07D239/70 , C07D471/04 , C07D487/04
摘要： The invention relates to pharmaceutically useful pyrimidine compounds of formula (I), methods for their preparation, their use as medicaments, and pharmaceutical formulations including them.
摘要翻译：本发明涉及药学上有用的式（I）嘧啶化合物，其制备方法，它们作为药物的用途，以及包括它们的药物制剂。

6. 发明申请

WO1998028009A1 PHARMACEUTICAL COMPOSITIONS FOR FREEZE DRYING 审中-公开
标题翻译：用于冻干的药物组合物
公开(公告)号：WO1998028009A1
公开(公告)日：1998-07-02
申请号：PCT/SE1997002068
申请日：1997-12-11
申请人： ASTRA PHARMACEUTICALS LTD. , ASTRA AKTIEBOLAG , BLAND, Chris , STEELE, Gerald
发明人： ASTRA PHARMACEUTICALS LTD. , ASTRA AKTIEBOLAG
IPC分类号： A61K47/26
CPC分类号： A61K31/7076 , A61K9/0019 , A61K9/19 , A61K31/704 , A61K47/02 , A61K47/26 , Y10S514/951
摘要： A pharmaceutical composition comprising a nucleotide analogue, mannitol and a modifying additve which is sodium chloride or a polyol which is suitable for freeze drying.
摘要翻译：一种药物组合物，其包含核苷酸类似物，甘露糖醇和改性添加剂，其是适合于冷冻干燥的氯化钠或多元醇。

7. 发明申请

WO1997038977A1 AMINOISOQUINOLINES AND AMINOTHIENOPYRIDINE DERIVATIVES AND THEIR USE AS ANTI-INFLAMMATORY AGENTS 审中-公开
标题翻译：氨基喹啉和氨基苯并吡啶衍生物及其作为抗炎剂的用途
公开(公告)号：WO1997038977A1
公开(公告)日：1997-10-23
申请号：PCT/SE1997000589
申请日：1997-04-09
申请人： ASTRA PHARMACEUTICALS LTD. , ASTRA AKTIEBOLAG , HAMLEY, Peter , MACDONALD, James , MATZ, James , TINKER, Alan
发明人： ASTRA PHARMACEUTICALS LTD. , ASTRA AKTIEBOLAG
IPC分类号： C07D217/22
CPC分类号： C07D401/04 , C07D217/22 , C07D405/04 , C07D409/04 , C07D417/04 , C07D495/04 , C07F7/081 , C07F7/0814
摘要： Compounds of formula (I) wherein R represents (i) phenyl, benzothiazolyl or a six-membered heterocyclic aromatic ring containing 1 to 3 nitrogen atoms, which phenyl, benzo ring of the benzothiazolyl or heterocyclic aromatic ring is optionally substituted by alkyl C1 to 6, alkoxy C1 to 6, halogen, hydroxy, thioalkyl C1 to 6, benzyloxy, or a group -Q(CH2)pNR R ; or (ii) alkyl C1 to 8, cycloalkyl C3 to 8, alkynyl C2 to 8, piperidyl, phenylalkyl C7 to 14, which alkyl, cylcoalkyl, alkynyl, or piperidyl is optionally substituted by a group -(CH2)pNR R , the phenylalkyl being optionally substituted by a group -(CH2)pNR R , alkyl C1 to 6, alkoxy C1 to 6, halogen or nitro; or (iii) a five-membered heterocyclic aromatic ring containing 1 to 3 heteroatoms selected from O, N or S, optionally substituted by alkyl C1 to 6, phenylalkyl C7 to 14 or halogen; or (iv) hydrogen or phenylalkynyl C7 to 14; Q represents O, NR or a bond; R represents hydrogen, alkyl C1 to 6, alkoxy C1 to 6, trimethylsilyl or halogen; R represents hydrogen, alkyl C1 to 6 or phenyl optionally substituted by alkyl C1 to 6, alkoxy C1 to 6, halogen or hydroxy; R represents hydrogen or halogen; R , R and R independently represent hydrogen or alkyl C1 to 6, or -NR R together represents piperidyl, pyrrolidinyl or morpholinyl; p represents an integer 1 to 5; and A represents a thieno or benzo ring; provided that when A represents a benzo ring and Q represents O, p does not represent 1; or pharmaceutically acceptable salts, enantiomers or tautomers thereof; have been found to be useful as pharmaceuticals, especially for the treatment of inflammatory disease.
摘要翻译：其中R表示（i）苯基，苯并噻唑基或含有1至3个氮原子的6元杂环芳环的式（I）化合物，其苯基，苯并噻唑基或杂环芳环的苯并环任选被烷基C1至6 ，烷氧基C1至6，卤素，羟基，硫代烷基C1至6，苄氧基或基团-Q（CH2）pNR4R5; 或（ii）C1至8烷基，C3至8环烷基，C2至8的炔基，哌啶基，C7至14的苯基烷基，该烷基，环烷基，炔基或哌啶基任选被基团 - （CH 2）p NRR R 苯基烷基任选被 - （CH 2）p NR 4 R 5，烷基C1至6，烷氧基C1至6，卤素或硝基取代; 或（iii）含有1至3个选自O，N或S的杂原子的五元杂环芳环，任选被C 1-6烷基，苯基烷基C 7至14或卤素取代; 或（iv）氢或苯基炔基C7至14; Q表示O，NR 6或键; R 1表示氢，烷基C1至6，烷氧基C1至6，三甲基甲硅烷基或卤素; R 2表示氢，烷基C1至6或任选被C 1-6烷基取代的苯基，烷氧基C1至6，卤素或羟基; R 3表示氢或卤素; R 4，R 5和R 6独立地表示氢或C 1-6的烷基，或-NR 4 R 5一起代表哌啶基，吡咯烷基或吗啉基; p表示1〜5的整数， A表示噻吩并或苯并环; 条件是当A表示苯并环且Q表示O时，p不表示1; 或其药学上可接受的盐，对映体或互变异构体; 已被发现可用作药物，特别是用于治疗炎性疾病。

8. 发明申请

WO1998027052A1 PROCESS FOR THE PREPARATION OF NMDA ANTAGONISTS 审中-公开
标题翻译：制备NMDA拮抗剂的方法
公开(公告)号：WO1998027052A1
公开(公告)日：1998-06-25
申请号：PCT/SE1997002092
申请日：1997-12-12
申请人： ASTRA PHARMACEUTICALS LTD. , ASTRA AKTIEBOLAG , HARRIS, Alan, Richard
发明人： ASTRA PHARMACEUTICALS LTD. , ASTRA AKTIEBOLAG
IPC分类号： C07C231/02
CPC分类号： C07C231/02 , Y02P20/55 , C07C237/06
摘要： This invention relates to an improved process for the production of known amine compounds of formula (I) which are useful as medicaments, wherein: R and R are independently phenyl or 4-fluorophenyl; R is hydrogen, alkyl C1-4 or methoxycarbonyl; R is hydrogen or methyl; which comprises reaction of a compound of formula (II) with a compound of formula (III) in which R , R , R , R , R and R are independently C1-6 alkyl followed by deprotection and optionally thereafter forming a pharmaceutically acceptable salt.
摘要翻译：本发明涉及可用作药物的已知的式（I）胺化合物的改进方法，其中：R 1和R 2独立地是苯基或4-氟苯基; R 3是氢，烷基C 1-4或甲氧基羰基; R 4是氢或甲基; 其包括式（II）化合物与其中R 5，R 6，R 7，R 8，R 9和R 10的式（III）化合物的反应，独立地是C 1-6烷基，然后去保护，然后任选地形成药学上可接受的盐。

9. 发明申请

WO1997045428A1 NOVEL PYRIDAZINE COMPOUNDS 审中-公开
标题翻译：新颖的吡咯烷酮化合物
公开(公告)号：WO1997045428A1
公开(公告)日：1997-12-04
申请号：PCT/SE1997000818
申请日：1997-05-20
申请人： ASTRA PHARMACEUTICALS LTD. , ASTRA AKTIEBOLAG , BANTICK, John , HIRST, Simon , PERRY, Matthew
发明人： ASTRA PHARMACEUTICALS LTD. , ASTRA AKTIEBOLAG
IPC分类号： C07D471/04
CPC分类号： C07D471/04
摘要： The invention relates to fused pyridazine compounds, in particular pyrido[h]cinnoline, pyrido[h]cinnolinone, pyridocyclopenta[1,2-c]pyridazine, pyridocyclopenta[1,2-c]pyridazinone, pyridocyclohepta[1,2-c]pyridazine and pyridocyclohepta[1,2-c]pyridazinone derivatives, their use as medicaments and pharmaceutical compositions comprising them.
摘要翻译：本发明涉及稠合的哒嗪化合物，特别是吡啶并[h]噌啉，吡啶并[h]噌啉酮，吡啶并环戊[1,2-c]哒嗪，吡啶并环戊[1,2-c]哒嗪酮，吡啶并杂庚环[1,2-c] 哒嗪和吡啶并环庚三烯并[1,2-c]哒嗪酮衍生物，它们用作药物和包含它们的药物组合物。

10. 发明申请

WO1997034893A1 PHARMACEUTICALLY USEFUL COMPOUNDS 审中-公开
标题翻译：药物有用的化合物
公开(公告)号：WO1997034893A1
公开(公告)日：1997-09-25
申请号：PCT/SE1997000471
申请日：1997-03-20
申请人： ASTRA PHARMACEUTICALS LTD. , ASTRA AKTIEBOLAG , BANTICK, John , BONNERT, Roger , CAGE, Peter , DONALD, David , FURBER, Mark , HIRST, Simon , PERRY, Matthew , PHILLIPS, Eifion
发明人： ASTRA PHARMACEUTICALS LTD. , ASTRA AKTIEBOLAG
IPC分类号： C07D471/04
CPC分类号： C07D231/56 , C07D401/04 , C07D471/04 , C07D487/04
摘要： The invention relates to 2-arylpyrazolisoquinoline and cinnolinone derivatives, methods for their preparation, their use as medicaments, and pharmaceutical formulations including them.
摘要翻译：本发明涉及2-芳基吡唑并喹啉和噌啉酮衍生物，其制备方法，它们作为药物的用途，以及包括它们的药物制剂。

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