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1. 发明申请

WO2006067587A2 CHEMICAL COMPOUNDS 审中-公开
标题翻译：化学化合物
公开(公告)号：WO2006067587A2
公开(公告)日：2006-06-29
申请号：PCT/IB2005/003825
申请日：2005-12-12
申请人： PFIZER LIMITED , JONES, Lyn, Howard , MIDDLETON, Donald, Stuart , MOWBRAY, Charles, Eric , NEWMAN, Sandra, Dora , WILLIAMS, David, Howard
发明人： JONES, Lyn, Howard , MIDDLETON, Donald, Stuart , MOWBRAY, Charles, Eric , NEWMAN, Sandra, Dora , WILLIAMS, David, Howard
IPC分类号： C07C311/29 , C07D215/36 , C07D213/75 , C07D217/22 , C07D217/18 , C07D265/30 , C07D211/16
CPC分类号： C07D215/36 , C07C311/46 , C07D207/12 , C07D207/16 , C07D211/26 , C07D211/42 , C07D213/71 , C07D213/75 , C07D213/89 , C07D215/08 , C07D215/40 , C07D215/48 , C07D231/12 , C07D231/40 , C07D237/20 , C07D239/42 , C07D241/08 , C07D241/20 , C07D261/08 , C07D271/07 , C07D295/185 , C07D413/04 , C07D471/04
摘要： This invention relates to biaryl ether derivatives of formula (I), wherein R 1 , R 3 , R 4 , X, W, Y and m are defined in the description, and to compositions containing them and the uses of such derivatives. The compounds of the present invention bind to the enzyme reverse transcriptase and are modulators, especially inhibitors thereof.
摘要翻译：本发明涉及式（I）的联芳醚衍生物，其中R 1，R 3，R 4，X，W，Y和 m在描述中定义，并且含有它们的组合物和这种衍生物的用途。本发明的化合物与酶逆转录酶结合，是调节剂，特别是其抑制剂。

2. 发明申请

WO2005016344A1 PIPERAZINE DERIVATIVES FOR THE TREATMENT OF HIV INFECTIONS 审中-公开
标题翻译：用于治疗艾滋病毒感染的哌嗪衍生物
公开(公告)号：WO2005016344A1
公开(公告)日：2005-02-24
申请号：PCT/IB2004/002562
申请日：2004-08-04
申请人： PFIZER LIMITED , PFIZER INC. , MIDDLETON, Donald, Stuart , MOWBRAY, Charles, Eric , STEPHENSON, Peter, Thomas , WILLIAMS, David, Howard
发明人： MIDDLETON, Donald, Stuart , MOWBRAY, Charles, Eric , STEPHENSON, Peter, Thomas , WILLIAMS, David, Howard
IPC分类号： A61K31/496
CPC分类号： C07D263/56 , C04B35/632 , C07D213/64 , C07D213/81 , C07D215/20 , C07D215/227 , C07D215/26 , C07D215/38 , C07D215/48 , C07D217/02 , C07D217/22 , C07D217/24 , C07D217/26 , C07D231/12 , C07D231/56 , C07D233/64 , C07D235/08 , C07D239/74 , C07D249/08 , C07D271/06 , C07D295/192 , C07D401/04 , C07D401/12
摘要： This invention relates to a compound of formula (I) or pharmaceutically acceptable salts, solvates or derivatives thereof, wherein R 1 to R 5 are defined in the description, and to processes for the preparation thereof, intermediates used in their preparation, compositions containing them and the uses of such derivatives. The compounds of the present invention inhibit the interaction of gp 120 with CD4 and are therefore of use in the treatment of HIV, a retroviral infection genetically related to HIV, or AIDS.
摘要翻译：本发明涉及式（I）化合物或其药学上可接受的盐，溶剂合物或衍生物，其中R 1至R 5在说明书中定义，及其制备方法，其制备中使用的中间体，含有它们的组合物和这些衍生物的用途。本发明的化合物抑制gp120与CD4的相互作用，因此可用于治疗与HIV或AIDS有遗传学关系的逆转录病毒感染的HIV。

3. 发明申请

WO2005121094A1 PIPERAZINE AND PIPERIDINE DERIVATIVES AS ANTI-HIV-AGENTS 审中-公开
标题翻译：哌嗪和哌啶衍生物作为抗病毒剂
公开(公告)号：WO2005121094A1
公开(公告)日：2005-12-22
申请号：PCT/IB2005/001677
申请日：2005-05-30
申请人： PFIZER LIMITED , PFIZER INC. , FENWICK, David, Roy , MIDDLETON, Donald, Stuart , STEPHENSON, Peter, Thomas , TRAN, Thien-Duc , WILLIAMS, David, Howard
发明人： FENWICK, David, Roy , MIDDLETON, Donald, Stuart , STEPHENSON, Peter, Thomas , TRAN, Thien-Duc , WILLIAMS, David, Howard
IPC分类号： C07D217/22
CPC分类号： C07D217/22 , C07D213/74 , C07D217/24 , C07D239/94 , C07D401/12 , C07D413/12 , C07D471/04 , C07D491/04
摘要： This invention relates to a compound of formula (I) or pharmaceutically acceptable salts, solvates or derivatives thereof, wherein R 1 to R 5 are defined in the description, and to processes for the preparation thereof, intermediates used in their preparation, compositions containing them and the uses of such derivatives. The compounds of the present invention inhibit the interaction of gp120 with CD4 and are 10 therefore of use in the treatment of HIV, a retroviral infection genetically related to HIV, or AIDS.
摘要翻译：本发明涉及式（I）化合物或其药学上可接受的盐，溶剂合物或衍生物，其中R 1至R 5在说明书中定义，及其制备方法，其制备中使用的中间体，含有它们的组合物和这些衍生物的用途。本发明的化合物抑制gp120与CD4的相互作用，并且因此用于治疗HIV，与HIV或AIDS有遗传学关系的逆转录病毒感染。

4. 发明申请

WO2002083643A1 PHENYL HETEROCYCLYL ETHER DERIVATIVES AS SEROTONIN RE-UPTAKE INHIBITORS 审中-公开
标题翻译：苯基异喹啉酮衍生物作为丝氨酸还原抑制剂
公开(公告)号：WO2002083643A1
公开(公告)日：2002-10-24
申请号：PCT/IB2002/001032
申请日：2002-03-27
申请人： PFIZER LIMITED , PFIZER INC. , ADAM, Mavis, Diane , ANDREWS, Mark, David , GYMER, Geoffrey, Edward , HEPWORTH, David , HOWARD, Harry, Ralph, Jr. , MIDDLETON, Donald, Stuart , STOBIE, Alan
发明人： ADAM, Mavis, Diane , ANDREWS, Mark, David , GYMER, Geoffrey, Edward , HEPWORTH, David , HOWARD, Harry, Ralph, Jr. , MIDDLETON, Donald, Stuart , STOBIE, Alan
IPC分类号： C07D213/65
CPC分类号： C07D213/65 , C07D213/80 , C07D213/82 , C07D241/18 , C07D401/06
摘要： The invention relates to compounds of the formula (I) which exhibit activity as selective serotonin re-uptake inhibitors.
摘要翻译：本发明涉及作为选择性5-羟色胺再摄取抑制剂的活性的式（I）化合物。

5. 发明申请

WO2004016593A1 DIARYL COMPOUNDS AS MONOAMINE REUPTAKE INHIBITORS 审中-公开
标题翻译： DIARYL化合物作为单胺类抑制剂
公开(公告)号：WO2004016593A1
公开(公告)日：2004-02-26
申请号：PCT/IB2003/003510
申请日：2003-08-04
申请人： PFIZER LIMITED , PFIZER INC. , ANDREWS, Mark, David , HEPWORTH, David , MIDDLETON, Donald, Stuart
发明人： ANDREWS, Mark, David , HEPWORTH, David , MIDDLETON, Donald, Stuart
IPC分类号： C07D213/38
CPC分类号： C07D213/70 , C07D213/38
摘要： The invention relates to compounds of formula (I) which inhibit monoamine re-uptake. Compounds of the present invention activity as selective serotonin re-uptake inhibitors (SSRIs) and have utility therefore in a variety of therapeutic areas. Notably the compounds of the present invention are useful in the treatment or prevention of a variety of disorders, including those in which the regulation of monoamine transporter function is implicated, such as depression, attention deficit hyperactivity disorder, obsessive-compulsive disorder, post-traumatic stress disorder, substance abuse disorders and sexual dysfunction including premature ejaculation.
摘要翻译：本发明涉及抑制单胺再摄取的式（I）化合物。作为选择性5-羟色胺再摄取抑制剂（SSRI）的本发明化合物活性，因此可用于多种治疗领域。值得注意的是，本发明的化合物可用于治疗或预防各种疾病，包括涉及调节单胺转运蛋白功能的疾病，例如抑郁症，注意缺陷多动障碍，强迫症，创伤后应激障碍，药物滥用障碍和性功能障碍，包括早泄。

6. 发明申请

WO2005009966A1 NICOTINAMIDE DERIVATIVES USEFUL AS PDE4 INHIBITORS 审中-公开
标题翻译： NICOTINAMIDE衍生物作为PDE4抑制剂有用
公开(公告)号：WO2005009966A1
公开(公告)日：2005-02-03
申请号：PCT/IB2004/002379
申请日：2004-07-13
申请人： PFIZER LIMITED , PFIZER INC. , BAILEY, Simon , BARBER, Christopher, Gordon , GLOSSOP, Paul, Alan , MIDDLETON, Donald, Stuart
发明人： BAILEY, Simon , BARBER, Christopher, Gordon , GLOSSOP, Paul, Alan , MIDDLETON, Donald, Stuart
IPC分类号： C07D213/82
CPC分类号： C04B35/632 , C07D213/82 , C07D401/12 , C07D405/12
摘要： This invention relates to nicotinamide derivatives of formula (I) and to pharmaceutical compositions containing, and the uses of such derivatives as PDE4 inhibitors wherein R 7 is attached to the 3- or 4-position of the phenyl ring and is S(O) p R 8 , R 8 is (C 1 -C 4 )alkyl optionally substituted by (C 3 -C 6 )cycloalkyl; m is 0 or 1; L is a (C 3 -C 8 )carbocyclic non-aromatic ring; and the remaining variables are as defined in the claims.
摘要翻译：本发明涉及式（I）的烟酰胺衍生物以及含有和其衍生物如PDE4抑制剂的用途的药物组合物，其中R 7连接于苯环的3-或4-位且为S（O）p R 8， R8是任选被（C 3 -C 6）环烷基取代的（C 1 -C 4）烷基; m为0或1; L是（C 3 -C 8）碳环非芳香环; 并且其余变量如权利要求中所定义。

7. 发明申请

WO2003051868A1 LACTAMS AS TACHYKININ ANTAGONISTS 审中-公开
标题翻译： LACTAMS作为TACHYKININ ANTAGONISTS
公开(公告)号：WO2003051868A1
公开(公告)日：2003-06-26
申请号：PCT/IB2002/005234
申请日：2002-12-06
申请人： PFIZER LIMITED , PFIZER INC. , MIDDLETON, Donald, Stuart , STOBIE, Alan
发明人： MIDDLETON, Donald, Stuart , STOBIE, Alan
IPC分类号： C07D401/14
CPC分类号： C07D401/14 , C07D401/04 , C07D405/14 , C07D413/14 , C07D491/10
摘要： Compounds of the formula (I) or a pharmaceutically acceptable salt, prodrug, solvate or polymorph thereof, wherein: R is het a ; R 1 is phenyl optionally substituted by one or more substituents; m is 1-4; Z is selected from: a) N(R 3 )(R 4 X) wherein X is NR 3 R 5 , OR 5 , Oaryl 1 , Ohet b , Ohet c , aryl 1 , het b or het c ; b) N(R 3 )Y wherein Y is aryl 1 , het b or het c ; and c) a 4-7 membered N containing saturated or partially saturated heterocycle said heterocycle attached to the alkylene link via said nitrogen atom, said heterocycle optionally containing an additional 1-3 groups, each independently selected from C=O, NH, S(O) p and O; optionally, said heterocycle is: (i) spirofused with het b , such that both rings share 1 atom; or (ii) optionally independently substituted by 1-3 groups; wherein R 3 and R 6 are both independently selected from H and C 1-6 alkyl; wherein R 4 is selected from C 1-6 alkylene; wherein R 5 is selected from C(O)OR 3 , S(O) p R 3 , S(O) p aryl 1 , C(O)R 3 , and C(O)NR 3 R 6 ; het b is a 4-7 membered heterocycle containing 1-3 heteroatoms, each independently selected from N, O and S, said N being optionally substituted with O, said ring optionally containing 1-2 C=O groups, said ring being saturated or partially saturated, said ring being optionally benzofused, said ring being optionally substituted by 1-3 substituents; het a and het c are a 5-7 membered aromatic heterocycle containing 1-3 heteroatoms each independently selected from N, O and S, said ring being optionally benzofused, said ring system as a whole being optionally substituted by 1-3 substituents; aryl 1 is phenyl or naphthyl, each being optionally substituted by 1-3 substituents; p is 0, 1 or 2; and n is 0-4; are useful in treating or preventing a condition for which an NK 2 antagonist is efficacious.
摘要翻译：式（I）化合物或其药学上可接受的盐，前药，溶剂化物或多晶型物，其中：R为 R 1是任选被一个或多个取代基取代的苯基; m为1-4; Z选自：a）N（R 3）（R 4 X）其中X是NR 3 R 5，OR 5，Oaryl 1，Ohet， c>，芳基1，het b或het c; b）N（R 3）Y，其中Y是芳基1，het b或het c; 和c）含有饱和或部分饱和杂环的4-7元N所述杂环通过所述氮原子连接到亚烷基链上，所述杂环任选地含有另外1-3个基团，各自独立地选自C = O，NH，S（ O）p和O; 任选地，所述杂环是：（i）用het b螺旋掺入，使得两个环共享1个原子; 或（ii）任选独立地被1-3个基团取代; 其中R 3和R 6均独立地选自H和C 1-6烷基; 其中R 4选自C 1-6亚烷基; 其中R 5选自C（O）OR 3，S（O）p R 3，S（O）paryl 1，C（O）R 3和C（O）NR <3> [R <6>; het b是含有1-3个杂原子的4-7元杂环，每个杂原子各自独立地选自N，O和S，所述N任选被O取代，所述环任选地含有1-2个C = O基团，所述环是饱和或部分饱和，所述环任选被苯并稠合，所述环任选被1-3个取代基取代; 它们是含有1-3个各自独立地选自N，O和S的杂原子的5-7元芳族杂环，所述环任选地是苯并稠合的，所述环系统整体上任选被1- 3个取代基; 芳基1是苯基或萘基，各自任选被1-3个取代基取代; p为0,1或2; n为0-4; 可用于治疗或预防NK2拮抗剂有效的病症。

8. 发明申请

WO2002079143A1 N-PHENPROPYLCYCLOPENTYL-SUBSTITUTED GLUTARAMIDE DERIVATIVES AS NEP INHIBITORS FOR FSAD 审中-公开
标题翻译： N-丙烯酰基取代的谷氨酰胺衍生物作为FSAD的NEP抑制剂
公开(公告)号：WO2002079143A1
公开(公告)日：2002-10-10
申请号：PCT/IB2002/000807
申请日：2002-03-18
申请人： PFIZER LIMITED , PFIZER INC. , CHALLENGER, Stephen , COOK, Andrew, Simon , GILLMORE, Adam, Thomas , MIDDLETON, Donald, Stuart , PRYDE, David, Cameron , STOBIE, Alan
发明人： CHALLENGER, Stephen , COOK, Andrew, Simon , GILLMORE, Adam, Thomas , MIDDLETON, Donald, Stuart , PRYDE, David, Cameron , STOBIE, Alan
IPC分类号： C07C235/82
CPC分类号： C07D319/18 , C07C235/82 , C07C255/60 , C07C323/40 , C07C2601/08 , C07C2602/08 , C07D213/40 , C07D215/12 , C07D231/56 , C07D307/81 , C07D311/74 , C07D317/62
摘要： The invention relates to compounds of formula (I) for treating for example sexual dysfunction, wherein R 1 is optionally substituted C 1-6 alkyl, optionally substituted carbocyclyl, optionally substituted heterocyclyl, hydrogen, C 1-6 alkoxy, -NR 2 R 3 or - NR 4 SO 2 R 5 ; X is the linkage -(CH 2 ) n - or -(CH 2 ) q -O- (wherein Y is attached to the oxygen); wherein one or more hydrogen atoms in linkage X may be replaced independently by C 1-4 alkoxy; hydroxy; hydroxy(C 1-3 alkyl); C 3-7 cycloalkyl; carbocyclyl; heterocyclyl; or by C 1-4 alkyl optionally substituted by one or more fluoro or phenyl groups; n is 3, 4, 5, 6, or 7; and q is 2, 3, 4, 5 or 6; and Y is phenyl or pyridyl, each of which may be substituted; or two R 8 groups on adjacent carbon atoms together with the interconnecting carbon atoms may form a fused optionally substituted 5- or 6-membered carbocyclic or heterocyclyic ring.
摘要翻译：本发明涉及用于治疗例如性功能障碍的式（I）化合物，其中R 1是任选取代的C 1-6烷基，任选取代的碳环基，任选取代的杂环基，氢，C 1-6烷氧基，-NR 2 R 3或 NR 4 SO 2 R 5; X是连接 - （CH 2）n - 或 - （CH 2）q -O-（其中Y连接到氧上）; 其中连接X中的一个或多个氢原子可以被C 1-4烷氧基独立地取代; 羟基; 羟基（C 1-3烷基）; 3-7环烷基; 碳环; 杂环; 或被任选被一个或多个氟或苯基取代的C 1-4烷基; n为3,4,5,6或7; q为2,3,4,5或6; Y为苯基或吡啶基，各自可以被取代; 或相邻碳原子上的两个R 8基团与互连碳原子一起可以形成稠合的任选取代的5或6元碳环或杂环基。

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