专利快速检索-快速检索全球专利，免费商用专利数据库-IPRDB

1. 发明申请

WO2008117169A1 PYRIMIDO [4, 5-D] AZEPINE DERIVATIVES AS 5-HT2C AGONISTS 审中-公开
标题翻译： PYRIMIDO [4，5-D] AZEPINE衍生物作为5-HT2C激动剂
公开(公告)号：WO2008117169A1
公开(公告)日：2008-10-02
申请号：PCT/IB2008/000731
申请日：2008-03-14
申请人： PFIZER LIMITED , ANDREWS, Mark, David , BLAGG, Julian , BRENNAN, Paul, Edward , FISH, Paul, Vincent , ROBERTS, Lee, Richard , STORER, Robert, Ian , WHITLOCK, Gavin, Alistair
发明人： ANDREWS, Mark, David , BLAGG, Julian , BRENNAN, Paul, Edward , FISH, Paul, Vincent , ROBERTS, Lee, Richard , STORER, Robert, Ian , WHITLOCK, Gavin, Alistair
IPC分类号： C07D487/04 , A61K31/55 , A61P15/00 , A61P25/00
CPC分类号： C07D487/04
摘要： The present invention relates to compounds of formula (I): wherein R 1 , R 2 , R 3a , R 3b , R 3c , R 3d and R 100 are as defined in the specification. These compounds act as 5-HT 2C agonists.
摘要翻译：本发明涉及式（I）的化合物：其中R 1，R 2，R 3a，R SUP， > 3b，R 3c，R 3d和R 100如说明书中所定义。这些化合物起5-HT 2C激动剂的作用。

2. 发明申请

WO2007135530A2 PHARMACEUTICALLY & VETERINARILY SUITABLE SALT 审中-公开
标题翻译：药用和维生素适用的盐
公开(公告)号：WO2007135530A2
公开(公告)日：2007-11-29
申请号：PCT/IB2007/001296
申请日：2007-05-10
申请人： PFIZER LIMITED , FISH, Paul, Vincent , WAKENHUT, Florian
发明人： FISH, Paul, Vincent , WAKENHUT, Florian
CPC分类号： C07D207/14
摘要： An improved pharmaceutical and veterinarily acceptable salt of 2,3-dichloro- Ν -cyclopentyl- Ν -[(3S)- pyrrolidin-3-yl]benzamide and compositions thereof, is described.
摘要翻译：描述了2,3-二氯-α-环戊基-α-[（3S） - 吡咯烷-3-基]苯甲酰胺及其组合物的改进的药物和兽医学上可接受的盐。

3. 发明申请

WO2006064336A2 NOVEL COMPOUNDS 审中-公开
标题翻译：新型化合物
公开(公告)号：WO2006064336A2
公开(公告)日：2006-06-22
申请号：PCT/IB2005003751
申请日：2005-12-02
申请人： PFIZER LTD , FISH PAUL VINCENT , RYCKMANS THOMAS , STOBIE ALAN , WAKENHUT FLORIAN
发明人： FISH PAUL VINCENT , RYCKMANS THOMAS , STOBIE ALAN , WAKENHUT FLORIAN
IPC分类号： C07D207/34 , A61K31/40 , A61P13/00 , A61P25/24 , A61P29/00
CPC分类号： C07D207/14
摘要： A compound of Formula (I) and pharmaceutically and/or veterinarily acceptable derivatives thereof, wherein: R 1 is H, C 1-6 alkyl, - C(A)D, C 3-8 cycloalkyl, aryl, het, aryl-C 1-4 alkyl or het-C 1 - 4 alkyl, wherein the cycloalkyl, aryl or het groups are optionally substituted by at least one substituent independently selected from C 1-8 allkyl, C 1-8 alkoxy, OH, halo, CF 3 , OCHF 2 , OCF3, SCF 3 , hydroxy-C 1-6 alkyl, C l-4 alkoxy-C 1-6 alkyl and C 1-4 alkyl-S-C 1-4 alkyl; A is S or O; D is H, C 1-6 alkyl, aryl, het, aryl-C 1-4 alkyl or het-C 1-4 alkyl; R 2 represents aryl 1 or het 1 , each of which is substituted by at least one substituent independently selected from B, provided that when R 2 is substituted by halo then it is also substituted with at least one other substituent independently selected from B other than halo; B represents aryl 2 , het 2 , Oaryl 2 , Ohet 2 , Saryl 2 , Shet 2 , SC 1-6 alkyl, halogen, CHF 2 , OCHF 2 , CF 2 CF 3 , CH 2 CF 3 , CF2CH 3 , aryl 2 -C 1-4 alkyl, C 3-6 cycloalkyl, C 3-6 cycloalkyl-C 1-4 alkyl, C 3-6 cycloalkylC 1-4 alkoxy, C 3-6 cycloalkyl-O-C 1-4 alkyl, C 3-6 cycloalkyl-C 1-4 alkoxy-C 1-4 alkyl, OC 3-6 cycloalkyl, SC 3-6 cycloalkyl; wherein the aryl 2 and het 2 groups are optionally substituted by at least one group selected from C 1-6 alkyl, C 3-6 cycloalkyl, C 1-6 alkoxy, OC 3-6 cycloalkyl, halo, CN, OH, CF 3 , CHF 2 , OCF 3 , OCHF 2 , hydroxyC 1 $alkyl, C 1-4 alkoxy-C 1-4 alkyl, SC 1-6 alkyl and SCF 3 ; n is 1 or 2, provided that when n is 1, m is 0 or 1 and when n is 2, m is 0, wherein if m is 0, then * represents a chiral centre; R 3 is H, C 1-6 alkyl, C 3-8 cycloalkyl, C 3-8 cycloalkylC 1-6 alkyl, aryl 3 , het 3 , aryl 3 -C 1-4 alkyl or het 3 -C 1 4alkyl, wherein the C 3-8 cycloalkyl, aryl 3 or het 3 groups are optionally substituted by at least one substituent independently selected from C 1-6 alkyl, C 1-6 alkoxy, CN, OH, halo, CF 3 , OCF 3 , SCF 3 , hydroxy-C 1-6 alkyl, C 1-4 alkoxy - C 1-6 alkyl and C 1-4 alkyl-S-C 1-4 alkyl; at each occurrence aryl, aryl 1 , aryl 2 and aryl 3 independently represent phenyl, naphthyl, anthracyl or phenanthryl; het 1 represents an aromatic 5- or 6- membered heterocycle which contains at least one N, O or S heteroatom, optionally fused to an aryl group; at each occurrence het, het 2 , and het 3 independently represents an aromatic or non-aromatic 4-, 5- or 6- membered heterocycle which contains at least one N, O or S heteroatom, optionally fused to a 5- or 6- membered carbocyclic group or a second 4-, 5- or 6membered heterocycle which contains at least one N, 0 or S heteroatom.
摘要翻译：式（I）化合物及其药学和/或兽医学上可接受的衍生物，其中：R 1是H，C 1-6烷基，-C（A）D ，C 3-8环烷基，芳基，杂环基，芳基-C 1-4烷基或叔丁基C 1 -C 4 - 烷基，其中环烷基，芳基或苯基基团任选地被至少一个独立地选自C 1-8烷基，C 1-8 - 烷氧基， OH，卤素，CF 3，OCHF 2，OCF 3，SCF 3，羟基-C 1-6烷基 C 1-4烷氧基-C 1-6烷基和C 1-4烷基-C 1-4亚烷基 >烷基; A是S或O; D是H，C 1-6烷基，芳基，杂环基，芳基-C 1-4烷基或叔丁基C 1-4烷基 ; R 2表示芳基，或每个被至少一个独立地选自B的取代基取代，其中R 1， SUP> 2被卤素取代，则其还被至少一个独立地选自除卤素以外的B的其它取代基取代; B表示芳基2，H 2，O 2，O 2，O 2，S 2 O 2， CH 2，CHF 2，OCHF 2，CF，SUB，C 1-6烷基，卤素，CHF 2，OCHF 2， CF 2 CH 3，CH 2 CH 3，CH 2 CH 3，芳基2， C 1-4烷基，C 3-6环烷基，C 3-6环烷基-C 1〜 4个C 1 -C 4烷基，C 3-6环烷基C 1-4烷氧基，C 3-6环烷基-OC 1- 4个C 1 -C 4烷基，C 3-6环烷基-C 1-4烷氧基-C 1-4烷基， 3-6个环烷基，SC 3〜6个环烷基; 其中芳基2和H 2 O 2基团任选被至少一个选自C 1-6烷基，C 3 -6个环烷基，C 1-6烷氧基，OC 3-6环烷基，卤素，CN，OH，CF 3， CHF 2，OCF 3，OCHF 2，羟基C 1 -C 1-4烷基，C 1-4烷基，烷氧基-C 1-4烷基，SC 1-6烷基和SCF 3 N; n为1或2，条件是当n为1时，m为0或1，当n为2时，m为0，其中如果m为0，则*表示手性中心; R 3是H，C 1-6烷基，C 3-8环烷基，C 3-8环烷基C C 1-6烷基，芳基3，叔丁基，正丁基，正丁基，其中C 3〜8个环烷基，芳基3个或3个以上烷基，或者它们可以被至少一个独立地选自C 1-6烷基，C 1-6烷氧基，CN， OH，卤素，CF 3，OCF 3，SCF 3，羟基-C 1-6烷基，C 1-4个烷氧基-C 1-6烷基和C 1-4烷基-SC 1-4烷基 ; 芳基独立地代表苯基，萘基，蒽基或菲基;芳基，芳基，杂环基，芳基，代表芳族5-或6-元杂环，其含有至少一个任选地与芳基稠合的N，O或S杂原子; 在每次发生时，het＆lt; 2＆gt;和＆lt; 3＆gt; 3＆lt; 3＆gt; 3独立地表示芳族或非芳族的4-，5-或6-元杂环，其含有至少一个N， O或S杂原子，任选地稠合到含有至少一个N，O或S杂原子的5-或6-元碳环基团或第二个4-，5-或6-元杂环。

4. 发明申请

WO2006064332A1 N-PYRROLIDIN-3YL-AMIDE DERIVATIVES AS SEROTONIN AND NORADRENALIN RE-UPTAKE INHIBITORS 审中-公开
标题翻译： N-吡咯烷-3-基酰胺衍生物作为丝氨酸和诺达霉素再摄取抑制剂
公开(公告)号：WO2006064332A1
公开(公告)日：2006-06-22
申请号：PCT/IB2005/003742
申请日：2005-12-02
申请人： PFIZER LIMITED , FISH, Paul, Vincent , RYCKMANS, Thomas , STOBIE, Alan , WAKENHUT, Florian
发明人： FISH, Paul, Vincent , RYCKMANS, Thomas , STOBIE, Alan , WAKENHUT, Florian
IPC分类号： C07D207/14 , A61K31/40
CPC分类号： C07D207/14
摘要： A compound of Formula (I) and pharmaceutically and/or veterinarily acceptable derivatives thereof, wherein: R 1 is H, C 1-6 alkyl, - C(A)D, C 3-8 cycloalkyl, aryl, het, aryl-C 1-4 alkyl or het-C 1-4 alkyl, wherein the cycloalkyl, aryl or het groups are optionally substituted; A is S or O; D is H, C 1-6 alkyl, aryl, het, aryl-C 1-4 alkyl or het-C 1-4 alkyl; aryl represents phenyl, naphthyl, anthracyl or phenanthryl; het represents an aromatic or non-aromatic 4-, 5-or 6- membered heterocycle which contains at least one N, O or S heteroatom, optionally fused to a 5- or 6- membered carbocyclic group or a second 4-, 5- or 6-membered heterocycle which contains at least one N, O or S heteroatom; R 2 is aryl 1 or het 1 , each optionally substituted; n is 1 or 2, provided that when n is 1, m is 0 or 1 and when n is 2, m is 0, wherein if m is 0, then * represents a chiral centre; R 3 is (CH 2 ) a E, wherein a is 0, 1 or 2 and E is a group selected from: Formula (i) wherein: X is O, S, NR 12 , (CH 2 ) v or a bond; b is 1, 2, 3 or 4; c is 1, 2 or 3; v is 1 or 2; R 10 and 11 are each independently H or C 1-4 alkyl; and R 12 is H, 1-6 alkyl, C(O)C 1-6 alkyl, SO 2 -C 1-6 alkyl; and wherein one or more pairs of hydrogen atoms on adjacent carbon or nitrogen atoms may be replaced by a corresponding number of double bonds, provided the ring system is not aromatic; Formula (ii) a carbocyclic spiro group containing 6 to 12 carbon atoms; Formula (iii) wherein: d is 1, 2, 3 or 4; a is 1, 2 or 3; f is 1 or 2; and R 30 is H or C 14 alkyl; and wherein one or more pairs of hydrogen atoms on adjacent carbon atoms may be replaced by a corresponding number of double bonds, provided the ring system is not aromatic; Formula (iv) wherein: g is 0, 1, 2 or 3; J is NR 40 ; and R 40 is C(O)C 1-6 alkyl, S0 2 -C 1-6 alkyl; Formula (v) wherein: h is 0, 1, 2 or 3; and R 50 is H, C 1-8 alkyl, C 1-8 alkoxy, OH, halo, CF 3 , OCF 3 , SCF 3 , hydroxy-C 1-6 alkyl, C 1-4 alkoxy-C 1-6 alkyl and C 1-4 alkyl-S-C 1-4 alkyl; Formula (vi) -CH(cyclopropane) 2 ; Formula (vii) C 1-6 alkyl, substituted by at least one substituent; and Formula (viii) C 3-8 cycloalkyl-C 1-6 alkyl; wherein the C 1-6 alkyl moiety is substituted at any point other than at the junction with the C 3-8 cycloalkyl moiety, by at least one substituent. The compounds exhibit activity as both serotonin and/or noradrenaline re-uptake inhibitors and therefore have utility in a variety of therapeutic areas, for example urinary incontinence.
摘要翻译：式（I）化合物及其药学和/或兽医学上可接受的衍生物，其中：R 1是H，C 1-6烷基，-C（A）D C 3-8环烷基，芳基，杂环基，芳基-C 1-4烷基或叔-C 1-4烷基，其中环烷基，芳基或苯基基团任选被取代; A是S或O; D是H，C 1-6烷基，芳基，杂芳基-C 1-4烷基或叔丁基C 1-4烷基 ; 芳基表示苯基，萘基，蒽基或菲基; 其表示芳族或非芳族的4-，5-或6-元杂环，其含有至少一个N，O或S杂原子，任选地与5-或6-元碳环基团或第二个4-，或含有至少一个N，O或S杂原子的6元杂环; R 2是每个任选被取代的芳基1或1或1; n为1或2，条件是当n为1时，m为0或1，当n为2时，m为0，其中如果m为0，则*表示手性中心; R 3是（CH 2）n，其中a是0,1或2，E是选自下式的基团：式（i ）其中：X为O，S，NR 12，（CH 2）2 H或键; b为1,2,3或4; c为1,2或3; v为1或2; R 10和H 11各自独立地为H或C 1-4烷基; 和R 12是H，C 1-6烷基，C（O）C 1-6烷基，SO 2 > -C _{1-6 烷基; 并且其中相邻碳原子或氮原子上的一对或多对氢原子可被相应数目的双键代替，条件是所述环系不是芳族的; 式（ⅱ）含有6至12个碳原子的碳环螺环; 式（ⅲ）其中：d为1,2,3或4; a是1,2或3; f为1或2; 并且R 30是H或C 14烷基; 并且其中相邻碳原子上的一对或多对氢原子可被相应数目的双键代替，条件是所述环系不是芳族的; 式（ⅳ）其中：g为0,1,2或3; J是NR 40; 且R 40是C（O）C 1-6烷基，S 0-2 -C 1-6烷基 ; 式（v）其中：h为0,1,2或3; R 50是H，C 1-8烷基，C 1-8烷氧基，OH，卤素，CF 3， 3，OCF 3，SCF 3，羟基-C 1-6烷基，C 1-4烷氧基 C 1-6烷基和C 1-4烷基-C 1-4烷基; 式（vi）-CH（环丙烷）2 式（vii）被至少一个取代基取代的C 1-6烷基; 和式（viii）C 3-8环烷基-C 1-6烷基; 其中C 1-6烷基部分在除C 3〜C 8环烷基部分的连接以外的任何点被至少一个取代基取代。该化合物表现出作为血清素和/或去甲肾上腺素再摄取抑制剂的活性，因此可用于各种治疗领域，例如尿失禁。}

5. 发明申请

WO2006064336A3 N-PYRROLIDIN-3-YL-AMIDE DERIVATIVES AS SEROTONIN AND NORADRENALIN RE-UPTAKE INHIBITORS 审中-公开
公开(公告)号：WO2006064336A3
公开(公告)日：2006-06-22
申请号：PCT/IB2005/003751
申请日：2005-12-02
申请人： PFIZER LIMITED , FISH, Paul, Vincent , RYCKMANS, Thomas , STOBIE, Alan , WAKENHUT, Florian
发明人： FISH, Paul, Vincent , RYCKMANS, Thomas , STOBIE, Alan , WAKENHUT, Florian
IPC分类号： C07D207/34 , A61K31/40 , A61P13/00 , A61P25/24 , A61P29/00
摘要： A compound of Formula (I) and pharmaceutically and/or veterinarily acceptable derivatives thereof, wherein: R 1 is H, C 1-6 alkyl, - C(A)D, C 3-8 cycloalkyl, aryl, het, aryl-C 1-4 alkyl or het-C 1 - 4 alkyl, wherein the cycloalkyl, aryl or het groups are optionally substituted by at least one substituent independently selected from C 1-8 allkyl, C 1-8 alkoxy, OH, halo, CF 3 , OCHF 2 , OCF3, SCF 3 , hydroxy-C 1-6 alkyl, C l-4 alkoxy-C 1-6 alkyl and C 1-4 alkyl-S-C 1-4 alkyl; A is S or O; D is H, C 1-6 alkyl, aryl, het, aryl-C 1-4 alkyl or het-C 1-4 alkyl; R 2 represents aryl 1 or het 1 , each of which is substituted by at least one substituent independently selected from B, provided that when R 2 is substituted by halo then it is also substituted with at least one other substituent independently selected from B other than halo; B represents aryl 2 , het 2 , Oaryl 2 , Ohet 2 , Saryl 2 , Shet 2 , SC 1-6 alkyl, halogen, CHF 2 , OCHF 2 , CF 2 CF 3 , CH 2 CF 3 , CF2CH 3 , aryl 2 -C 1-4 alkyl, C 3-6 cycloalkyl, C 3-6 cycloalkyl-C 1-4 alkyl, C 3-6 cycloalkylC 1-4 alkoxy, C 3-6 cycloalkyl-O-C 1-4 alkyl, C 3-6 cycloalkyl-C 1-4 alkoxy-C 1-4 alkyl, OC 3-6 cycloalkyl, SC 3-6 cycloalkyl; wherein the aryl 2 and het 2 groups are optionally substituted by at least one group selected from C 1-6 alkyl, C 3-6 cycloalkyl, C 1-6 alkoxy, OC 3-6 cycloalkyl, halo, CN, OH, CF 3 , CHF 2 , OCF 3 , OCHF 2 , hydroxyC 1 $alkyl, C 1-4 alkoxy-C 1-4 alkyl, SC 1-6 alkyl and SCF 3 ; n is 1 or 2, provided that when n is 1, m is 0 or 1 and when n is 2, m is 0, wherein if m is 0, then * represents a chiral centre; R 3 is H, C 1-6 alkyl, C 3-8 cycloalkyl, C 3-8 cycloalkylC 1-6 alkyl, aryl 3 , het 3 , aryl 3 -C 1-4 alkyl or het 3 -C 1 4alkyl, wherein the C 3-8 cycloalkyl, aryl 3 or het 3 groups are optionally substituted by at least one substituent independently selected from C 1-6 alkyl, C 1-6 alkoxy, CN, OH, halo, CF 3 , OCF 3 , SCF 3 , hydroxy-C 1-6 alkyl, C 1-4 alkoxy - C 1-6 alkyl and C 1-4 alkyl-S-C 1-4 alkyl; at each occurrence aryl, aryl 1 , aryl 2 and aryl 3 independently represent phenyl, naphthyl, anthracyl or phenanthryl; het 1 represents an aromatic 5- or 6- membered heterocycle which contains at least one N, O or S heteroatom, optionally fused to an aryl group; at each occurrence het, het 2 , and het 3 independently represents an aromatic or non-aromatic 4-, 5- or 6- membered heterocycle which contains at least one N, O or S heteroatom, optionally fused to a 5- or 6- membered carbocyclic group or a second 4-, 5- or 6membered heterocycle which contains at least one N, 0 or S heteroatom.

6. 发明申请

WO2005105100A1 MORPHOLINE COMPOUNDS 审中-公开
标题翻译：吗啉化合物
公开(公告)号：WO2005105100A1
公开(公告)日：2005-11-10
申请号：PCT/IB2005/001154
申请日：2005-04-20
申请人： PFIZER LIMITED , PFIZER, INC. , FISH, Paul, Vincent , MACKENNY, Malcolm, Christian , STOBIE, Alan , WAKENHUT, Florian , WHITLOCK, Gavin, Alistair
发明人： FISH, Paul, Vincent , MACKENNY, Malcolm, Christian , STOBIE, Alan , WAKENHUT, Florian , WHITLOCK, Gavin, Alistair
IPC分类号： A61K31/535
CPC分类号： C07D413/06 , A61K31/535 , C07D265/30 , C07D413/12
摘要： The present invention provides compounds of Formula I: wherein R 1 , R 2 , R 3 , and n have any of the values defined in the specification, and pharmaceutically acceptable salts thereof, that are useful as agents in the treatment of conditions including urinary disorders, pain, premature ejaculation, ADHD and fibromyalgia. Also provided are pharmaceutical compositions comprising one or more compounds of Formula I.
摘要翻译：本发明提供式I化合物：其中R 1，R 2，R 3和n具有说明书中定义的任何值及其药学上可接受的盐，其可用作治疗包括尿失禁，疼痛，早泄，ADHD和纤维肌痛的病症。还提供了包含一种或多种式I化合物的药物组合物。

7. 发明申请

WO2004110995A1 N-PYRROLIDIN-3-YL-AMIDE DERIVATIVES AS SEROTONIN AND NORADRENALINE RE-UPTAKE INHIBITORS 审中-公开
标题翻译： N-吡咯烷-3-基酰胺衍生物作为丝氨酸蛋白酶和肾上腺素再摄取抑制剂
公开(公告)号：WO2004110995A1
公开(公告)日：2004-12-23
申请号：PCT/IB2004/001943
申请日：2004-06-07
申请人： PFIZER LIMITED , PFIZER INC. , FISH, Paul, Vincent , FRAY, Michael, Jonathan , LOVERING, Deborah, Jane , STOBIE, Alan , WAKENHUT, Florian , WHITLOCK, Gavin, Alistair
发明人： FISH, Paul, Vincent , FRAY, Michael, Jonathan , LOVERING, Deborah, Jane , STOBIE, Alan , WAKENHUT, Florian , WHITLOCK, Gavin, Alistair
IPC分类号： C07D207/14
CPC分类号： C07D207/14
摘要： A compound of Formula (I) and pharmaceutically and/or veterinarily acceptable derivatives thereof, wherein R 1 is H, C 1 _ 6 alkyl, -C(X)Y, C 3 _ 8 cycloalkyl, aryl, het, aryl-C l _ 4 alkyl or het-C l _ 4 alkyl, wherein the cycloalkyl, aryl or het groups are optionally substituted by at least one substituent independently selected from C1_ 8 allkyl, C 1 _ 8 alkoxy, OH, halo, CF 3 , OCF 3 , SCF 3 , hydroxy-C l _ 6 alkyl, C 1 _ 4 alkoxy-C 1 _ 6 alkyl and C1_ 4 alkyl-S-C 1 _ 4 alkyl; R 2 is aryl or heteroaryl, each optionally substituted by at least one substituent independently selected from C 1 _ 8 alkyl, C 1 _ 8 alkoxy, OH, halo, CF 3 , OCF 3 , SCF3, hydroxy-C 1 _ 6 alkyl, C1_4alkoxy-C 1 _ 6 alkyl and C1_ 4 alkyl-S-C 1 _ 4 alkyl; R 3 is C 1 _ 6 alkyl, C 3 _ 8 cycloalkyl, C 3 _ 8 cycloalkyl-C 1 _ 6 alkyl, aryl, het, aryl-C l _ 4 alkyl or het-C 1 _ 4 alkyl, wherein the cycloalkyl, aryl or het groups are optionally substituted by at least one substituent independently selected from C 1 _ 6 alkyl, C 1 _ 6 alkoxy, OH, halo, CF 3 , OCF 3 , SCF 3 , hydroxy-C 1 _ 6 alkyl, C 1 _ 4 alkoxy - C 1 _ 6 alkyl and C 1 _ 4 alkyl-SC 1 _ 4 alkyl; X is S or O; Y is H, C 1 _ 6 alkyl, aryl, het, aryl-C 1 _ 4 alkyl or het-C 1 _ 4 alkyl; and n is 1 or 2, provided that when n is 1, m is 0 or 1 and when n is 2, m is 0, wherein if m is 0, then * represents a chiral center. The compounds of the invention exhibit activity as both serotonin and noradrenaline re-uptake inhibitors and therefore have utility in a variety of therapeutic areas, for example urinary incontinence.
摘要翻译：式（I）化合物及其药学和/或兽医学上可接受的衍生物，其中R 1是H，C 1-6烷基，-C（X）Y，C 3-8环烷基，芳基，杂环基，芳基-C 1-4烷基或叔丁基-C 1-4烷基，其中环烷基，芳基或苯基基团任选被至少一个独立地选自C 1-8烷基，C 1-8烷氧基，OH，卤素，CF 3，OCF 3，SCF 3，羟基-C 1-6烷基，C 1-4烷氧基-C 1-6烷基和C 1-4烷基-S-C 1-4烷基的取代基取代; R 2是芳基或杂芳基，各自任选被至少一个独立地选自C 1-8烷基，C 1-8烷氧基，OH，卤素，CF 3，OCF 3，SCF 3，羟基-C 1-6烷基，C 1-4烷氧基-C 1-6烷基和C 1-4烷基-S-C 1-4烷基的取代基取代; R 3是C 1-6烷基，C 3-8环烷基，C 3-8环烷基-C 1-6烷基，芳基，杂芳基，C 1-4烷基或叔丁基C 1-4烷基，其中环烷基，芳基或苯基基团任选被至少一个独立地选自C 1-6烷基，C 1-6烷氧基，OH，卤素，CF 3，OCF 3，SCF 3，羟基-C 1-6烷基，C 1-4烷氧基-C 1-6烷基和C 1-4烷基-C 1-4烷基; X是S或O; Y是H，C 1-6烷基，芳基，杂环基，芳基-C 1-4烷基或叔丁基C 1-4烷基; n为1或2，条件是当n为1时，m为0或1，当n为2时，m为0，其中如果m为0，则*表示手性中心。本发明的化合物表现出5-羟色胺和去甲肾上腺素再摄取抑制剂的活性，因此可用于各种治疗领域，例如尿失禁。

8. 发明申请

WO2002079200A1 3-HETEROCYCLYLPROPANOHYDROXAMIC ACID AS PROCOLLAGEN C-PROTEINASE INHIBITORS 审中-公开
标题翻译： 3-环烷基丙基羟基酸作为方法C-蛋白酶抑制剂
公开(公告)号：WO2002079200A1
公开(公告)日：2002-10-10
申请号：PCT/IB2002/000699
申请日：2002-03-08
申请人： PFIZER LIMITED , PFIZER INC. , BAILEY, Simon , FISH, Paul, Vincent , JAMES, Kim , WHITLOCK, Gavin, Alistair
发明人： BAILEY, Simon , FISH, Paul, Vincent , JAMES, Kim , WHITLOCK, Gavin, Alistair
IPC分类号： C07D413/04
CPC分类号： C07D271/06 , C07D263/32 , C07D413/04 , C07D413/14
摘要： Compounds of compounds of formula (I) and their salts, solvates and prodrugs, wherein the substituents are as defined herein, are Procollagen C-proteinase inhibitors for the treatment of scars.
摘要翻译：式（I）化合物及其盐，溶剂合物和前药，其中取代基如本文所定义的化合物是用于治疗瘢痕的前胶原C蛋白酶抑制剂。

9. 发明申请

WO2013027168A1 NOVEL HETEROCYCLIC COMPOUNDS AS BROMODOMAIN INHIBITORS 审中-公开
标题翻译：新型杂环化合物作为BROMODOMAIN抑制剂
公开(公告)号：WO2013027168A1
公开(公告)日：2013-02-28
申请号：PCT/IB2012/054211
申请日：2012-08-20
申请人： PFIZER INC. , FISH, Paul Vincent , COOK, Andrew Simon , PHILLIPS, Christopher , BENT, Andrew Frank , MILLS, James Edward John , SCIAMMETTA, Nunzio
发明人： FISH, Paul Vincent , COOK, Andrew Simon , PHILLIPS, Christopher , BENT, Andrew Frank , MILLS, James Edward John , SCIAMMETTA, Nunzio
IPC分类号： C07D215/22 , C07D217/24 , C07D239/78 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/12 , C07D409/12 , C07D411/12 , C07D413/12 , C07D417/12 , A61K31/517 , A61P35/00
CPC分类号： C07D403/12 , C07D215/22 , C07D217/24 , C07D239/78 , C07D401/12 , C07D401/14 , C07D405/12 , C07D409/12 , C07D411/12 , C07D413/12 , C07D417/12
摘要： Disclosed are compounds of Formula (I): (I) which are useful as bromodomain inhibitors. Pharmaceutical compositions containing compounds of Formula (I) and the use of compounds of Formula (I) to treat diseases or disorders that are bromodomain-dependent are also disclosed. Methods for preparing and using these compounds are further described.
摘要翻译：公开了可用作溴域结构域抑制剂的式（I）：（I）的化合物。还公开了含有式（I）化合物和式（I）化合物用于治疗溴结构域依赖性疾病或病症的药物组合物。进一步描述制备和使用这些化合物的方法。

10. 发明申请

WO2006056884A1 N- [ (3S)- PYRROLIDIN-3-YL]- BENZAMIDE DERIVATIVES AS MONOAMINE RE-UPTAKE INHIBITORS 审中-公开
标题翻译： N- [（3S） - 吡咯烷-3-基] - 苯甲酰胺衍生物作为单胺反应抑制剂
公开(公告)号：WO2006056884A1
公开(公告)日：2006-06-01
申请号：PCT/IB2005/003643
申请日：2005-11-18
申请人： PFIZER LIMITED , PFIZER INC. , FISH, Paul, Vincent , RYCKMANS, Thomas , STOBIE, Alan , WAKENHUT, Florian , WHITLOCK, Gavin, Alistair
发明人： FISH, Paul, Vincent , RYCKMANS, Thomas , STOBIE, Alan , WAKENHUT, Florian , WHITLOCK, Gavin, Alistair
IPC分类号： C07D207/14 , A61K31/40
CPC分类号： C07D405/12 , C07D207/14
摘要： A compound of Formula (I) and pharmaceutically and/or veterinarily acceptable derivatives thereof, wherein: R 1 , R 2 , R 3 and R 20 are each independently H, CI, Br, F, I, CF 3 , OCF 3 , Me or Et; R 4 is het or C 3-7 cycloalkyl optionally substituted by C 1-4 alkyl, C 1-4 alkoxy, alkoxyalkyl containing 2 to 4 carbon atoms or -S-(C 1-4 alkyl); a is 0 or 1; and het is a non-aromatic 4-, 5- or 6- membered heterocycle which contains at least one N, O or S heteroatom, optionally fused to a 5- or 6- membered carbocyclic group or a second 4-, 5- or 6-membered heterocycle which contains at least one N, O or S heteroatom, wherein the het group is optionally substituted by at least one substituent independently selected from C 1-8 alkyl, C 1-8 alkoxy, OH, halo, CF 3 , OCF 3 , SCF 3 , hydroxy-C 1-6 alkyl, C 1-4 alkoxy-C 1-6 alkyl and C 1-4 alkyl-S-C 1-4 alkyl; provided that at least one of R 1 , R 2 and R 3 are other than H. The compounds of the invention exhibit activity as both serotonin and noradrenaline re-uptake inhibitors and therefore have utility in a variety of therapeutic areas, for example urinary incontinence.
摘要翻译：式（I）的化合物及其药学和/或兽医学上可接受的衍生物，其中：R 1，R 2，R 3和R 3 各自独立地为H，Cl，Br，F，I，CF 3，OCF 3，Me或Et; R 4是H或任选被C 1-4烷基取代的C 3-7环烷基，C 1-4 - 烷氧基，含有2至4个碳原子的烷氧基烷基或-S-（C 1-4烷基）; a是0或1; 并且het是非芳族的4-，5-或6-元杂环，其含有至少一个N，O或S杂原子，任选地与5-或6-元碳环基团或第二个4-，5-或其含有至少一个N，O或S杂原子的6元杂环，其中所述基团任选地被至少一个独立地选自C 1-8烷基，C 1- 8个烷氧基，OH，卤素，CF 3，OCF 3，SCF 3，羟基-C 1-6 C 1-4烷基，C 1-4烷氧基-C 1-6烷基和C 1-4烷基-S SC 1 -4 烷基; 条件是R 1，R 2和R 3中的至少一个不是H.本发明的化合物表现出作为血清素的活性和去甲肾上腺素再摄取抑制剂，因此可用于各种治疗领域，例如尿失禁。

你已经成功收藏专利！

检索式保存成功!

IPRDB

热门服务

关于我们

友情链接

联系方式