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    1, 2, 4 -TRIAZOLE DERIVATIVES AS VASOPRESSIN ANTAGONISTS
    1.
    发明申请
    1, 2, 4 -TRIAZOLE DERIVATIVES AS VASOPRESSIN ANTAGONISTS 审中-公开
    1,2,4-异噻唑衍生物作为VASOPRESSIN ANTAGONISTS

    公开(公告)号：WO2006123242A1

    公开(公告)日：2006-11-23

    申请号：PCT/IB2006/001442

    申请日：2006-05-08

    Applicant: PFIZER LIMITED ,  BRYANS, Justin, Stephen ,  JOHNSON, Patrick, Stephen ,  ROBERTS, Lee, Richard ,  RYCKMANS, Thomas

    Inventor： BRYANS, Justin, Stephen ,  JOHNSON, Patrick, Stephen ,  ROBERTS, Lee, Richard ,  RYCKMANS, Thomas

    IPC: C07D403/04 ,  C07D471/04 ,  C07D491/10 ,  C07D471/10 ,  C07D403/14 ,  C07D401/04 ,  C07D487/04 ,  C07D498/04 ,  A61K31/4196 ,  A61P15/00 ,  A61P9/00

    CPC classification number: C07D471/04 ,  C07D401/04 ,  C07D403/04 ,  C07D403/14 ,  C07D471/10 ,  C07D487/04 ,  C07D491/10 ,  C07D498/04

    Abstract: Compounds of formula (I), or a pharmaceutically acceptable salt, solvate, ester or amide thereof, wherein R 1 represents [CH 2 ] n -R 2 ; R 2 represents H, C 1-6 alkyloxy or Het; n represents a number selected from 0 to 6; Het represents an unsaturated heterocycle of 5 or 6 atoms containing one or more heteroatoms selected from O, N, and S; R 3 represents halo; Ring A represents a 4 to 7 membered, saturated, partially saturated, or unsaturated heterocycle containing one or more heteroatoms selected from O, N, and S; Ring B represents a saturated, partially saturated, or unsaturated heterocycle of from 3 to 8 atoms containing one or more heteroatoms selected from O, N, and S, or Ring B represents a saturated or unsaturated carbocyclic ring of from 3 to 8 atoms; Ring B is optionally fused to an aryl ring and is optionally substituted with one or more groups independently selected from R 4 ; Ring A and Ring B share at least one atom; R 4 represents oxo, [CH 2 ] m -R 5 , or CH-R 6 R 7 ; R 5 represents H, OH, C 1-6 alkyloxy, COOH, or CONR 8 R 9 ; m represents a number selected from 0 or 1 ; and R 6 , R 7 , R 8 and R 9 independently represent H or C 1-6 alkyl; are useful for treating a disorder for which a V1a antagonist is indicated, in particular, dysmenorrhoea.

    Abstract translation: 式（I）化合物或其药学上可接受的盐，溶剂合物，酯或酰胺，其中R 1表示[CH 2 N] -R 2 ; R 2表示H，C 1-6烷氧基或Het; n表示选自0〜6的数; Het表示含有一个或多个选自O，N和S的杂原子的5或6个原子的不饱和杂环; R 3表示卤素; 环A表示含有一个或多个选自O，N和S的杂原子的4至7元饱和的，部分饱和的或不饱和的杂环; 环B表示含有一个或多个选自O，N和S的杂原子的3至8个原子的饱和，部分饱和或不饱和杂环，或环B表示3至8个原子的饱和或不饱和碳环; 环B任选地与芳环稠合并且任选地被一个或多个独立地选自R 4的基团取代; 环A和环B共享至少一个原子; R 4表示氧代，[CH 2 CH 2] m -R 5或CH-R 6 - [R 7 ; R 5表示H，OH，C 1-6烷氧基，COOH或CONR 8 R 9; m表示选自0或1的数字; 且R 6，R 7，R 8和R 9独立地表示H或C 1〜 6烷基; 可用于治疗指示V1a拮抗剂的疾病，特别是痛经。

    TRIAZOLE DERIVATIVES WHICH INHIBIT VASOPRESSIN ANTAGONISTIC ACTIVITY
    2.
    发明申请
    TRIAZOLE DERIVATIVES WHICH INHIBIT VASOPRESSIN ANTAGONISTIC ACTIVITY 审中-公开
    抑制VASOPRESSIN拮抗活性的三唑衍生物

    公开(公告)号：WO2005079808A1

    公开(公告)日：2005-09-01

    申请号：PCT/IB2005/000079

    申请日：2005-01-11

    Applicant: PFIZER LIMITED ,  PFIZER INC. ,  BRYANS, Justin, Stephen ,  JOHNSON, Patrick, Stephen ,  RYCKMANS, Thomas ,  STOBIE, Alan

    Inventor： BRYANS, Justin, Stephen ,  JOHNSON, Patrick, Stephen ,  RYCKMANS, Thomas ,  STOBIE, Alan

    IPC: A61K31/5517

    CPC classification number: C07D401/14

    Abstract: Compounds of formula (I), or pharmaceutically acceptable derivatives thereof, wherein: Het represents 2-pyridinyl or 2-pyrimidinyl;R 1 represents H, C 1-3 alkyl or a nitrogen-containing heterocyclic ring having 5 or 6 ring atoms; R 2 represents H, benzyl or C 1-3 alkyl; and R 3 represents H, methyl , methoxy or chloro ; are useful for treating anxiety, cardiovascular disease (including angina, atherosclerosis, hypertension, heart failure, edema, hypernatremia), dysmenorrhoea (primary and secondary), endometriosis, emesis (including motion sickness), intrauterine growth retardation, inflammation (including rheumatoid arthritis), mittlesmerchz, preclampsia, premature ejaculation, premature (preterm) labor and Raynaud's disease.

    Abstract translation: 式（I）化合物或其药学上可接受的衍生物，其中：Het表示2-吡啶基或2-嘧啶基; R 1表示H，C 1-3烷基或含有5或6个环原子的含氮杂环; R 2表示H，苄基或C 1-3烷基; R 3表示H，甲基，甲氧基或氯; 可用于治疗焦虑，心血管疾病（包括心绞痛，动脉粥样硬化，高血压，心力衰竭，水肿，高钠血症），痛经（原发性和继发性），子宫内膜异位症，呕吐（包括晕车），宫内生长迟缓，炎症（包括类风湿性关节炎） ，mittlesmerchz，先兆子痫，早泄，早产（早产）劳动和雷诺氏病。

    NOVEL COMPOUNDS
    3.
    发明申请
    NOVEL COMPOUNDS 审中-公开
    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

    Applicant: PFIZER LTD ,  FISH PAUL VINCENT ,  RYCKMANS THOMAS ,  STOBIE ALAN ,  WAKENHUT FLORIAN

    Inventor： FISH PAUL VINCENT ,  RYCKMANS THOMAS ,  STOBIE ALAN ,  WAKENHUT FLORIAN

    IPC: C07D207/34 ,  A61K31/40 ,  A61P13/00 ,  A61P25/24 ,  A61P29/00

    CPC classification number: C07D207/14

    Abstract: 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.

    Abstract translation: 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。

    N-PYRROLIDIN-3YL-AMIDE DERIVATIVES AS SEROTONIN AND NORADRENALIN RE-UPTAKE INHIBITORS
    4.
    发明申请
    N-PYRROLIDIN-3YL-AMIDE DERIVATIVES AS SEROTONIN AND NORADRENALIN RE-UPTAKE INHIBITORS 审中-公开
    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

    Applicant: PFIZER LIMITED ,  FISH, Paul, Vincent ,  RYCKMANS, Thomas ,  STOBIE, Alan ,  WAKENHUT, Florian

    Inventor： FISH, Paul, Vincent ,  RYCKMANS, Thomas ,  STOBIE, Alan ,  WAKENHUT, Florian

    IPC: C07D207/14 ,  A61K31/40

    CPC classification number: C07D207/14

    Abstract: 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.

    Abstract translation: 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。

    N-PYRROLIDIN-3-YL-AMIDE DERIVATIVES AS SEROTONIN AND NORADRENALIN RE-UPTAKE INHIBITORS
    6.
    发明申请
    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

    Applicant: PFIZER LIMITED ,  FISH, Paul, Vincent ,  RYCKMANS, Thomas ,  STOBIE, Alan ,  WAKENHUT, Florian

    Inventor： FISH, Paul, Vincent ,  RYCKMANS, Thomas ,  STOBIE, Alan ,  WAKENHUT, Florian

    IPC: C07D207/34 ,  A61K31/40 ,  A61P13/00 ,  A61P25/24 ,  A61P29/00

    Abstract: 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.

    N- [ (3S)- PYRROLIDIN-3-YL]- BENZAMIDE DERIVATIVES AS MONOAMINE RE-UPTAKE INHIBITORS
    9.
    发明申请
    N- [ (3S)- PYRROLIDIN-3-YL]- BENZAMIDE DERIVATIVES AS MONOAMINE RE-UPTAKE INHIBITORS 审中-公开
    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

    Applicant: PFIZER LIMITED ,  PFIZER INC. ,  FISH, Paul, Vincent ,  RYCKMANS, Thomas ,  STOBIE, Alan ,  WAKENHUT, Florian ,  WHITLOCK, Gavin, Alistair

    Inventor： FISH, Paul, Vincent ,  RYCKMANS, Thomas ,  STOBIE, Alan ,  WAKENHUT, Florian ,  WHITLOCK, Gavin, Alistair

    IPC: C07D207/14 ,  A61K31/40

    CPC classification number: C07D405/12 ,  C07D207/14

    Abstract: 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.

    Abstract translation: 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。

    3-HETEROCYCLYL-4-PHENYL-TRIAZOLE DERIVATIVES AS INHIBITORS OF THE VASOPRESSIN V1A RECEPTOR
    10.
    发明申请
    3-HETEROCYCLYL-4-PHENYL-TRIAZOLE DERIVATIVES AS INHIBITORS OF THE VASOPRESSIN V1A RECEPTOR 审中-公开
    作为VASOPRESSIN V1A受体的抑制剂的3-环己基-4-苯基 - 三唑衍生物

    公开(公告)号：WO2005105779A1

    公开(公告)日：2005-11-10

    申请号：PCT/IB2005/001062

    申请日：2005-04-18

    Applicant: PFIZER LIMITED ,  PFIZER INC. ,  BRYANS, Justin, Stephen ,  JOHNSON, Patrick, Stephen ,  RYCKMANS, Thomas ,  STOBIE, Alan

    Inventor： BRYANS, Justin, Stephen ,  JOHNSON, Patrick, Stephen ,  RYCKMANS, Thomas ,  STOBIE, Alan

    IPC: C07D401/04

    CPC classification number: C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/14

    Abstract: Compounds of formula (I): or a pharmaceutically acceptable derivative thereof, wherein R represents C 1-6 alkyl (optionally substituted by C 1-6 alkyloxy or Het) or C 1-6 alkyloxy; R 1 and R 2 independently represent hydrogen, halo or C 1-6 alkyl, ring A represents Het 1 ; X represents O or NR 3 ; R 3 represents hydrogen or C 1-6 alkyl; ring B represents a phenyl group or Het 2 , either of which may be optionally substituted with one or more groups selected from halo, CN, C 1-6 alkyloxy, CF 3 , C 1-6 alkyl, NH 2 and NO 2 ; Het and Het 1 independently represent a 5- or 6-membered saturated, partially unsaturated or aromatic heterocyclic group comprising either (a) 1 to 4 nitrogen atoms, (b) one oxygen or one sulphur atom or (c) 1 oxygen atom or 1 sulphur atoms and 1 or 2 nitrogen atoms are useful for treating anxiety, cardiovascular disease (including angina, atherosclerosis, hypertension, heart failure, edema, hypernatremia), dysmenorrhoea (primary and secondary), endometriosis, emesis (including motion sickness), intrauterine growth retardation, inflammation (including rheumatoid arthritis) mittlesmerchz, preclampsia, premature ejaculation, premature (preterm) labour and Raynaud’s disease.

    Abstract translation: 式（I）化合物或其药学上可接受的衍生物，其中R表示C 1-6烷基（任选被C 1-6烷氧基或Het取代）或C 1-6烷氧基; R 1和R 2独立地表示氢，卤素或C 1-6烷基，环A表示Het 1; X表示O或NR 3; R 3表示氢或C 1-6烷基; 环B表示苯基或Het 2，其任一个可以任选被一个或多个选自卤素，CN，C 1-6烷氧基，CF 3，C 1-6烷基，NH 2和NO 2的基团取代; Het和Het 1独立地表示包含（a）1至4个氮原子，（b）一个氧或一个硫原子或（c）1个氧原子的5或6元饱和，部分不饱和或芳族杂环基 或1个硫原子和1或2个氮原子可用于治疗焦虑，心血管疾病（包括心绞痛，动脉粥样硬化，高血压，心力衰竭，水肿，高钠血症），痛经（原发性和继发性），子宫内膜异位症，呕吐（包括晕车病） 子宫内生长迟缓，炎症（包括类风湿关节炎）手足牢，先兆子痫，早泄，早产（早产）劳动和雷诺氏病。

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