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1. 发明申请

WO1996003380A1 AROMATIC AMINO ETHERS AS PAIN RELIEVING AGENTS 审中-公开
标题翻译： AROMATIC AMINO ETHERS AS PAIN RELIEVENT AGENTS
公开(公告)号：WO1996003380A1
公开(公告)日：1996-02-08
申请号：PCT/GB1995001728
申请日：1995-07-21
申请人： ZENECA LIMITED , BREAULT, Gloria, Anne , OLDFIELD, John , TUCKER, Howard , WARNER, Peter
发明人： ZENECA LIMITED
IPC分类号： C07D213/79
CPC分类号： C07D213/40 , C07C45/41 , C07C45/68 , C07C45/71 , C07C229/30 , C07C229/42 , C07C229/60 , C07C237/30 , C07C237/32 , C07C255/58 , C07C255/59 , C07D213/38 , C07D213/80 , C07D213/82 , C07D237/24 , C07D239/42 , C07D241/18 , C07D257/04 , C07D263/48 , C07D277/56 , C07D285/13 , C07D285/135 , C07D307/14 , C07D333/32 , C07D333/38 , C07D401/04 , C07D405/12 , C07D409/12 , C07D409/14 , C07D413/12 , C07D417/12 , C07C47/575 , C07C47/565
摘要： The present invention relates to compounds of formula (I), wherein A is an optionally substituted phenyl, naphthyl, pyridyl, pyrazinyl, pyridazinyl, pyrimidyl, thienyl, thiazolyl, oxazolyl, thiadiazolyl having at least two adjacent ring carbon atoms or a bicyclic ring system, provided that the -CH(R )N(R )B-R and -OCH(R -)-D linking groups are positioned in a 1,2 relationship to one another on ring carbon atoms and the ring atom positioned ortho to the -OCHR - linking group (and therefore in the 3-position relative to the -CHR NR - linking group) is not substituted; B is an optionally substituted ring system; D is an optionally substituted ring system; R is a variety of group as defined in the description; R is hydrogen, C1-6alkyl, C2-6alkenyl, C2-6alkynyl, phenylC1-3alkyl or 5- or 6-membered heteroarylC1-3alkyl; R is hydrogen or C1-4alkyl; R is hydrogen or C1-4alkyl; and N-oxides of NR where chemically possible; and S-oxides of sulphur containing rings were chemically possible; and pharmaceutically acceptable salts and in vivo hydrolysable esters and amides thereof. Process for their preparation, intermediates in their preparation, their use as therapeutic agents and pharmaceutical compositions containing them.
摘要翻译：本发明涉及式（I）化合物，其中A是任选取代的苯基，萘基，吡啶基，吡嗪基，哒嗪基，嘧啶基，噻吩基，噻唑基，恶唑基，具有至少两个相邻环碳原子的噻二唑基或双环体系条件是-CH（R 3）N（R 2）BR 1和-OCH（R 4 - ） - D连接基彼此在环上相互关联。碳原子和位于-OCHR 4 - 连接基团（因此相对于-CHR 3 NR 2 - 连接基团的3位）邻位的环原子不被取代; B是任选取代的环系; D是任选取代的环系; R 1是描述中定义的各种组; R 2是氢，C 1-6烷基，C 2-6烯基，C 2-6炔基，苯基C 1-3烷基或5-或6-元杂芳基C 1-3烷基; R 3是氢或C 1-4烷基; R 4是氢或C 1-4烷基; 和NR 2的N-氧化物，其中化学上可能; 含硫环的S-氧化物在化学上是可能的; 和其药学上可接受的盐和体内可水解的酯和酰胺。其制备方法，其制备中的中间体，它们作为治疗剂的用途和含有它们的药物组合物。

2. 发明申请

WO1997000863A1 AROMATIC COMPOUNDS AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM 审中-公开
标题翻译：芳香化合物和含有它们的药物组合物
公开(公告)号：WO1997000863A1
公开(公告)日：1997-01-09
申请号：PCT/GB1996001442
申请日：1996-06-17
申请人： ZENECA LIMITED , BREAULT, Gloria, Anne
发明人： ZENECA LIMITED
IPC分类号： C07D213/80
CPC分类号： C07D213/80 , C07D237/24 , C07D403/04 , C07D413/12 , C07D417/12
摘要： The invention relates to compounds of formula (I), wherein A is an optionally substituted ring system, provided that the -CH(R )N(R )B-R and -OR groups are positioned in a 1,2 relationship to one another on ring carbon atoms and the ring atom positioned ortho to the OR linking group (and therefore in the 3-position relative to the -CHR NR linking group) is not substituted; B is an optionally substituted ring system: R is positioned on ring B in a 1,3 or 1,4 relationship with the -CH(R )N(R )- linking group and is as defined in the specification. R is hydrogen, C1-6alkyl, optionally substituted by hydroxy, cyano or trifluoromethyl, C2-6alkenyl (provided the double bond is not in the 1-position), C2-6alkynyl (provided the triple bond is not in the 1-position), phenylC1-3alkyl or pyridylC1-3alkyl; R is hydrogen, methyl or ethyl; R is optionally substituted: C1-6alkyl, C3-7cycloalkylC1-3alkyl or C3-7cycloalkyl; and N-oxides of -NR where chemically possible; and S-oxides of sulphur containing rings where chemically possible; and pharmaceutically acceptable salts and in vivo hydrolysable esters and amides thereof. Processes for their preparation, their use as therapeutic agents and pharmaceutical compositions containing them.
摘要翻译：本发明涉及式（I）化合物，其中A是任选取代的环系，条件是-CH（R 3）N（R 2）BR 1和-OR 4基团是在环碳原子上位于1,2个关系中，并且环原子位于OR 4连接基团的邻位（因此相对于-CHR 3 NR 2 - 2-连接的3-位）组）未被替代; B是任选取代的环系：R 1与-CH（R 3）N（R 2） - 连接基以1,3或1,4的关系位于环B上，并且为在规范中定义。 R 2是氢，任选被羟基，氰基或三氟甲基取代的C 1-6烷基，C 2-6烯基（提供双键不在1-位），C 2-6炔基（条件是三键不在1 - 位），苯基C 1-3烷基或吡啶基C 1-3烷基; R 3是氢，甲基或乙基; R 4任选被取代：C 1-6烷基，C 3-7环烷基C 1-3烷基或C 3-7环烷基; 和NR 2的N-氧化物，其中化学上可能; 和化学可能的含硫环的S-氧化物; 和其药学上可接受的盐和体内可水解的酯和酰胺。其制备方法，用作治疗剂和含有它们的药物组合物。

3. 发明申请

WO0220512A9 IMIDAZOLO-5-YL-2-ANILINO-PYRIMIDINES AS AGENTS FOR THE INHIBITION OF THE CELL PROLIFERATION 审中-公开
标题翻译：咪达唑仑5-YL-2-ANILINO-PYRIMININES作为抑制细胞增殖的试剂
公开(公告)号：WO0220512A9
公开(公告)日：2004-05-06
申请号：PCT/GB0103864
申请日：2001-08-30
申请人： ASTRAZENECA AB , ASTRAZENECA UK LTD , BREAULT GLORIA ANNE , NEWCOMBE NICHOLAS JOHN , THOMAS ANDREW PETER
发明人： BREAULT GLORIA ANNE , NEWCOMBE NICHOLAS JOHN , THOMAS ANDREW PETER
IPC分类号： C07D401/14 , A61K31/506 , A61K31/5377 , A61P9/10 , A61P17/06 , A61P19/02 , A61P19/08 , A61P27/02 , A61P29/00 , A61P35/00 , A61P35/02 , A61P37/02 , A61P43/00 , C07D403/04 , C07D403/14 , C07D405/14 , C07D413/14 , C07D417/14
CPC分类号： C07D403/04 , C07D403/14 , C07D405/14 , C07D413/14 , C07D417/14
摘要： Compounds of the formula (I): wherein R , R , R , R , R , R , p, q, and n are as defined within and a pharmaceutically acceptable salts and in vivo hydrolysable esters are described. Also described are processes for their preparation and their use as medicaments, particularly medicaments for producing a cell cycle inhibitory (anti-cell-proliferation) effect in a warm-blooded animal, such as man.
摘要翻译：式（I）化合物：其中R 1，R 2，R 3，R 4，R 5，R 6，p，q和n如上所定义，描述了药学上可接受的盐和体内可水解的酯。还描述了它们的制备方法及其作为药物的用途，特别是用于在温血动物如人中产生细胞周期抑制（抗细胞增殖）作用的药物。

4. 发明申请

WO1997000864A1 AROMATIC COMPOUNDS AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM 审中-公开
标题翻译：芳香化合物和含有它们的药物组合物
公开(公告)号：WO1997000864A1
公开(公告)日：1997-01-09
申请号：PCT/GB1996001443
申请日：1996-06-17
申请人： ZENECA LIMITED , BREAULT, Gloria, Anne
发明人： ZENECA LIMITED
IPC分类号： C07D237/24
CPC分类号： C07D213/80 , C07D213/82 , C07D237/18 , C07D237/24 , C07D401/04 , C07D403/04 , C07D413/04 , C07D413/12 , C07D417/12
摘要： The invention relates to compounds of formula (I), wherein A is an optionally substituted, ring system provided that the -CH(R )N(R )B-R and -OD groups are positioned in a 1,2 relationship to one another on ring carbon atoms and the ring atom positioned ortho to the -OD linking group (and therefore in the 3-position relative to the -CHR NR linking group) is not substituted; B is an optionally substituted ring system; R is positioned on ring B in a 1,3 or 1,4 relationship with the -CH(R )N(R )- linking group and is as defined in the description; R is hydrogen, C1-6alkyl, optionally substituted by hydroxy, cyano or trifluoromethyl, C2-6alkenyl (provided the double bond is not in the 1-position), (C2-6alkynyl (provided the triple bond is not in the 1-position), phenylC1-3alkyl or pyridylC1-3alkyl; R is hydrogen, methyl or ethyl; D is hydrogen, an optionally substituted 5-7 membered carbocyclic ring containing one double bond, C1-3alkyl substituted by an optionally substituted 5-7 membered carbocyclic ring containing one double bond or D is of the formula -(CH2)nCH(R )C(R )=C(R )R and N-oxides of -NR where chemically possible; and S-oxides of sulphur containing rings where chemically possible; and pharmaceutically acceptable salts and in vivo hydrolysable esters and amides thereof; excluding 4-[5-carboxy-2-hydroxybenzylamino]benzoic acid, 4-[2,5-dihydroxybenzylamino]benzoic acid, 5-[2-hydroxybenzylamino]-2-hydroxybenzoic acid, 3-[2,5-dihydroxybenzylamino]benzoic acid, 4-[2,5-dihydroxybenzylamino]benzenecarboxamide, 3-[2-hydroxybenzylamino]benzoic acid, 4-[2,5-dihydroxybenzylamino]-2-hydroxybenzoic acid, 4-[hydroxybenzylamino]-2-hydroxybenzoic acid and 4[2-hydroxybenzylamino]benzoic acid. Processes for their preparation, intermediates in their preparation, their use as therapeutic agents and pharmaceutical compositions containing them.
摘要翻译：本发明涉及式（I）化合物，其中A是任选取代的环系，条件是-CH（R 3）N（R 2）BR 1和-OD基团位于在环碳原子上彼此相关，并且位于-OD连接基团（因此相对于-CHR 3 NR 2连接基团的3位）的环原子未被取代 ; B是任选取代的环系; R 1与-CH（R 3）N（R 2） - 连接基以1,3或1,4个关系位于环B上，并且如说明书中所定义; R 2是氢，任选被羟基，氰基或三氟甲基取代的C 1-6烷基，C 2-6烯基（提供双键不在1-位），（C 2-6炔基（条件是三键不在 1-位），苯基C 1-3烷基或吡啶基C 1-3烷基; R 3是氢，甲基或乙基; D是氢，任选取代的含有一个双键的5-7元碳环，被任选取代的C 1-3烷基含有一个双键的5-7元碳环或D具有式 - （CH 2）n CH（R 4）C（R 5）= C（R 6）R 7和N-氧化物其中化学上可能的是-NR 2，和其中化学可能的含硫环的S-氧化物;及其药学上可接受的盐和体内可水解的酯和酰胺;不包括4- [5-羧基-2-羟基苄基氨基]苯甲酸， 4- [2,5-二羟基苄基氨基]苯甲酸，5- [2-羟基苄基氨基] -2-羟基苯甲酸，3- [2,5-二羟基苄基氨基]苯甲酸，4- [2,5-二羟基苄基氨基]苯甲醛 de，3- [2-羟基苄基氨基]苯甲酸，4- [2,5-二羟基苄基氨基] -2-羟基苯甲酸，4- [羟基苄基氨基] -2-羟基苯甲酸和4 [2-羟基苄基氨基]苯甲酸。其制备方法，制备中的中间体，作为治疗剂的用途和含有它们的药物组合物。

5. 发明申请

WO1996006822A1 ORTHO-SUBSTITUTED AROMATIC ETHER COMPOUNDS AND THEIR USE IN PHARMACEUTICAL COMPOSITIONS FOR PAIN RELIEF 审中-公开
标题翻译： ORTHO替代芳香醚化合物及其在药物组合物中的用途
公开(公告)号：WO1996006822A1
公开(公告)日：1996-03-07
申请号：PCT/GB1995002030
申请日：1995-08-29
申请人： ZENECA LIMITED , BREAULT, Gloria, Anne , OLDFIELD, John , TUCKER, Howard , WARNER, Peter
发明人： ZENECA LIMITED
IPC分类号： C07C65/21
CPC分类号： C07D213/40 , C07C45/298 , C07C45/41 , C07C45/45 , C07C45/513 , C07C45/565 , C07C45/68 , C07C47/565 , C07C47/575 , C07C49/83 , C07C65/24 , C07C205/22 , C07C205/37 , C07C217/76 , C07C235/42 , C07C235/46 , C07C235/60 , C07C251/48 , C07C255/37 , C07C255/54 , C07C311/21 , C07C317/18 , C07C317/22 , C07C323/20 , C07D213/80 , C07D257/04 , C07D277/56 , C07D417/12
摘要： The present invention relates to compounds of formula (I) wherein: A is an optionally substituted ring system as defined herein; B is an optionally substituted 5- or 6-membered heteroaryl ring system or optionally substituted phenyl; D is an optionally substituted ring system as defined herein; X is of the formula -(CHR )n- or -(CHR )pCR =CR (CHR )q- wherein n is 1 to 3 and p and q are either both 0 or one of p and q is 1 and the other is 0; R is positioned on ring B in a 1,3 or 1,4 relationship with the -OCH(R )- linking group in 6-membered rings and in a 1,3 relationship with the -OCH(R )- linking group in 5-membered rings and is one of a variety or groups as defined herein; R is hydrogen or C1-4alkyl; R is hydrogen or C1-4alkyl; and N-oxides thereof where chemically possible; and S-oxides of sulphur containing rings where chemically possible; a pharmaceutically acceptable salt and in vivo hydrolysable ester and amide thereof. The present invention also relates to processes for their preparation, intermediates in their preparation, their use as therapeutic agents and pharmaceutical compositions containing them.
摘要翻译：本发明涉及式（I）的化合物，其中：A是如本文所定义的任选取代的环系; B是任选取代的5或6元杂芳基环系或任选取代的苯基; D是如本文所定义的任选取代的环系; X具有式 - （CHR 4）n - 或 - （CHR 4）p CR 4 = CR 4（CHR 4）q - ，其中n为1至3，p和q为 p和q中的0或1都是1，另一个是0; R 1与6位环中的-OCH（R 3） - 连接基以1,3或1,4个关系位于环B上，与-OCH（R 3元环） - 五元环中的连接基团，并且是如本文定义的多种或多种之一; R 3是氢或C 1-4烷基; R 4是氢或C 1-4烷基; 化学可能的N-氧化物; 和化学可能的含硫环的S-氧化物; 其药学上可接受的盐和体内可水解的酯和酰胺。本发明还涉及其制备方法，其制备中的中间体，它们作为治疗剂的用途和含有它们的药物组合物。

6. 发明申请

WO2002020512A1 IMIDAZOLO-5-YL-2-ANILINO-PYRIMIDINES AS AGENTS FOR THE INHIBITION OF THE CELL PROLIFERATION 审中-公开
标题翻译：咪达唑仑5-YL-2-ANILINO-PYRIMININES作为抑制细胞增殖的试剂
公开(公告)号：WO2002020512A1
公开(公告)日：2002-03-14
申请号：PCT/GB2001/003864
申请日：2001-08-30
申请人： ASTRAZENECA AB , ASTRAZENECA UK LIMITED , BREAULT, Gloria, Anne , NEWCOMBE, Nicholas, John , THOMAS, Andrew, Peter
发明人： BREAULT, Gloria, Anne , NEWCOMBE, Nicholas, John , THOMAS, Andrew, Peter
IPC分类号： C07D403/04
CPC分类号： C07D403/04 , C07D403/14 , C07D405/14 , C07D413/14 , C07D417/14
摘要： Compounds of the formula (I): wherein R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , p, q, and n are as defined within and a pharmaceutically acceptable salts and in vivo hydrolysable esters are described. Also described are processes for their preparation and their use as medicaments, particularly medicaments for producing a cell cycle inhibitory (anti-cell-proliferation) effect in a warm-blooded animal, such as man.
摘要翻译：式（I）化合物：其中R 1，R 2，R 3，R 4，R 5，R 6，p，q和n如上所定义，描述了药学上可接受的盐和体内可水解的酯。还描述了它们的制备方法及其作为药物的用途，特别是用于在温血动物如人中产生细胞周期抑制（抗细胞增殖）作用的药物。

7. 发明申请

WO1992017480A1 ANTIBIOTIC CARBAPENEM DERIVATIVES 审中-公开
标题翻译：抗生素CARBAPENEM衍生物
公开(公告)号：WO1992017480A1
公开(公告)日：1992-10-15
申请号：PCT/GB1992000587
申请日：1992-04-02
申请人： IMPERIAL CHEMICAL INDUSTRIES PLC , I.C.I. PHARMA , BETTS, Michael, John , BREAULT, Gloria, Anne
发明人： IMPERIAL CHEMICAL INDUSTRIES PLC , I.C.I. PHARMA
IPC分类号： C07D477/00
CPC分类号： C07D477/20 , C07D207/12 , C07D403/12 , C07F9/568
摘要： The present invention provides a compound of formula (I) wherein: R is 1-hydroxyethyl, 1-fluoroethyl or hydroxymethyl; R is hydrogen or C1-4 alkyl; n is zero or an integer 1 to 4; and P is a benzene ring substituted by groups R and R which are ortho with respect to one another wherein R and R are independently hydroxy or in vivo hydrolysable esters thereof; or P is a group of formula (II) or (III), wherein M is oxygen or a group NR wherein R is hydrogen or C1-4 alkyl; ring P being optionally further substituted; or a pharmaceutically acceptable salt or in vivo hydrolysable ester thereof.
摘要翻译：本发明提供式（I）化合物，其中：R 1是1-羟乙基，1-氟乙基或羟甲基; R 2是氢或C 1-4烷基; n为0或整数1〜4; 并且P是被R 3和R 4基团取代的苯环，其相对于彼此是邻位的，其中R 3和R 4独立地是羟基或其体内可水解的酯; 或P是式（II）或（III）的基团，其中M是氧或基团NR 5，其中R 5是氢或C 1-4烷基; 环P任选被进一步取代; 或其药学上可接受的盐或体内可水解的酯。

8. 发明申请

WO1992017479A1 ANTIBIOTIC CARBAPENEM DERIVATIVES 审中-公开
标题翻译：抗生素CARBAPENEM衍生物
公开(公告)号：WO1992017479A1
公开(公告)日：1992-10-15
申请号：PCT/GB1992000586
申请日：1992-04-02
申请人： IMPERIAL CHEMICAL INDUSTRIES PLC , I.C.I. PHARMA , BETTS, Michael, John , BREAULT, Gloria, Anne
发明人： IMPERIAL CHEMICAL INDUSTRIES PLC , I.C.I. PHARMA
IPC分类号： C07D477/00
CPC分类号： C07D477/20 , C07D207/16 , C07D403/12 , C07F9/568
摘要： The present invention provides a compound of formula (I) wherein: R is 1-hydroxyethyl, 1-fluoroethyl or hydroxymethyl; R is hydrogen or C1-4alkyl; R and R are ortho with respect to one another wherein R and R are independently hydroxy or in vivo hydrolysable esters thereof; the benzene ring being optionally further substituted; or a pharmaceutically acceptable salt or in vivo hydrolysable ester thereof.
摘要翻译：本发明提供式（I）化合物，其中：R 1是1-羟乙基，1-氟乙基或羟甲基; R 2是氢或C 1-4烷基; R 3和R 4相对于彼此是邻位的，其中R 3和R 4独立地是羟基或其体内可水解的酯; 苯环任选被进一步取代; 或其药学上可接受的盐或体内可水解的酯。

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