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1. 发明申请

WO2006123242A1 1, 2, 4 -TRIAZOLE DERIVATIVES AS VASOPRESSIN ANTAGONISTS 审中-公开
标题翻译： 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
申请人： PFIZER LIMITED , BRYANS, Justin, Stephen , JOHNSON, Patrick, Stephen , ROBERTS, Lee, Richard , RYCKMANS, Thomas
发明人： BRYANS, Justin, Stephen , JOHNSON, Patrick, Stephen , ROBERTS, Lee, Richard , RYCKMANS, Thomas
IPC分类号： C07D403/04 , C07D471/04 , C07D491/10 , C07D471/10 , C07D403/14 , C07D401/04 , C07D487/04 , C07D498/04 , A61K31/4196 , A61P15/00 , A61P9/00
CPC分类号： C07D471/04 , C07D401/04 , C07D403/04 , C07D403/14 , C07D471/10 , C07D487/04 , C07D491/10 , C07D498/04
摘要： 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.
摘要翻译：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。}}

2. 发明申请

WO2005063754A1 TRIAZOLE DERIVATIVES AS VASOPRESSIN ANTAGONISTS 审中-公开
标题翻译：三唑衍生物作为VASOPRESSIN拮抗剂
公开(公告)号：WO2005063754A1
公开(公告)日：2005-07-14
申请号：PCT/IB2004/004059
申请日：2004-12-09
申请人： PFIZER LIMITED , PFIZER INC. , BRYANS, Justin, Stephen , JOHNSON, Patrick, Stephen , ROBERTS, Lee, Richard , RYCKMANS, Thomas
发明人： BRYANS, Justin, Stephen , JOHNSON, Patrick, Stephen , ROBERTS, Lee, Richard , RYCKMANS, Thomas
IPC分类号： C07D487/04
CPC分类号： C07D401/14 , C07D401/04 , C07D405/14 , C07D413/14 , C07D471/04
摘要： Compounds of formula (I), or pharmaceutically acceptable derivatives thereof, wherein: V represents a direct link or -O-; Ring A represents an optionally substituted 5- to 7-membered saturated heterocyclic ring, or a phenylene group.
摘要翻译：式（I）化合物或其药学上可接受的衍生物，其中：V表示直链或-O-; 环A表示任选取代的5至7元饱和杂环或亚苯基。

3. 发明申请

WO2006114706A1 TRIAZOLE DERIVATIVES AS VASOPRESSIN ANTAGONISTS 审中-公开
标题翻译：三唑衍生物作为VASOPRESSIN拮抗剂
公开(公告)号：WO2006114706A1
公开(公告)日：2006-11-02
申请号：PCT/IB2006/001071
申请日：2006-04-18
申请人： PFIZER LIMITED , BRYANS, Justin, Stephen , BUNNAGE, Mark, Edward , JOHNSON, Patrick, Stephen , MASON, Helen, Janet , ROBERTS, Lee, Richard , RYCKMANS, Thomas , STOBIE, Alan , UNDERWOOD, Toby, James
发明人： BRYANS, Justin, Stephen , BUNNAGE, Mark, Edward , JOHNSON, Patrick, Stephen , MASON, Helen, Janet , ROBERTS, Lee, Richard , RYCKMANS, Thomas , STOBIE, Alan , UNDERWOOD, Toby, James
IPC分类号： C07D401/14 , C07D498/04 , C07D413/14 , C07D487/04 , C07D471/04 , C07D417/14 , C07D513/04 , A61K31/4196 , A61P25/00
CPC分类号： C07D471/04 , C07D401/14 , C07D413/14 , C07D417/14 , C07D487/04 , C07D513/04
摘要： Compounds of formula (I), or pharmaceutically acceptable derivatives thereof, wherein: R 1 represents a group selected from H, CF 3 , and C 1-6 alkyl (optionally substituted by C 1-6 alkyloxy or triazolyl); R 2 represents halo; Ring A represents a 5- or 6-membered heterocyclic ring containing at least one N atom (the ring being optionally bridged with two or more carbon atoms); R 3 represents a 5- or 6-membered heterocyclic ring containing at least one atom selected from N, O or S, the heterocyclic ring being optionally substituted by one or more groups selected from C 1-6 alkyl, oxo or NH 2 , the heterocyclic ring being further optionally fused to a 5- or 6-membered aryl or heterocyclic ring containing at least one atom selected from N, O or S, the fused aryl or heterocyclic ring being substituted by one or more halo atoms; are useful for treating a disorder for which a V1a antagonist is indicated, in particular, dysmenorrhoea.
摘要翻译：式（I）化合物或其药学上可接受的衍生物，其中：R 1表示选自H，CF 3 N和C 1-6的基团，（任选被C 1-6烷氧基或三唑基取代）; R 2表示卤素; 环A表示含有至少一个N原子（该环任选地与两个或多个碳原子桥连）的5-或6-元杂环; R 3表示含有至少一个选自N，O或S的原子的5或6元杂环，该杂环任选被一个或多个选自C 1 -6个烷基，氧代或NH 2，杂环进一步任选地与含有至少一个选自N，O或者O的原子的5-或6-元芳基或杂环稠合 S，稠合的芳基或杂环被一个或多个卤素原子取代; 可用于治疗指示V1a拮抗剂的疾病，特别是痛经。

4. 发明申请

WO2005079808A1 TRIAZOLE DERIVATIVES WHICH INHIBIT VASOPRESSIN ANTAGONISTIC ACTIVITY 审中-公开
标题翻译：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
申请人： PFIZER LIMITED , PFIZER INC. , BRYANS, Justin, Stephen , JOHNSON, Patrick, Stephen , RYCKMANS, Thomas , STOBIE, Alan
发明人： BRYANS, Justin, Stephen , JOHNSON, Patrick, Stephen , RYCKMANS, Thomas , STOBIE, Alan
IPC分类号： A61K31/5517
CPC分类号： C07D401/14
摘要： 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.
摘要翻译：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。

5. 发明申请

WO2005105779A1 3-HETEROCYCLYL-4-PHENYL-TRIAZOLE DERIVATIVES AS INHIBITORS OF THE VASOPRESSIN V1A RECEPTOR 审中-公开
标题翻译：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
申请人： PFIZER LIMITED , PFIZER INC. , BRYANS, Justin, Stephen , JOHNSON, Patrick, Stephen , RYCKMANS, Thomas , STOBIE, Alan
发明人： BRYANS, Justin, Stephen , JOHNSON, Patrick, Stephen , RYCKMANS, Thomas , STOBIE, Alan
IPC分类号： C07D401/04
CPC分类号： C07D401/04 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/14
摘要： 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.
摘要翻译：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。

6. 发明申请

WO2004074291A1 TRIAZOLE COMPOUNDS USEFUL IN THERAPY 审中-公开
标题翻译：三唑化合物有用于治疗
公开(公告)号：WO2004074291A1
公开(公告)日：2004-09-02
申请号：PCT/IB2004/000432
申请日：2004-02-09
申请人： PFIZER LIMITED , PFIZER INC. , BRYANS, Justin, Stephen , JOHNSON, Patrick, Stephen , RYCKMANS, Thomas , STOBIE, Alan
发明人： BRYANS, Justin, Stephen , JOHNSON, Patrick, Stephen , RYCKMANS, Thomas , STOBIE, Alan
IPC分类号： C07D487/04
CPC分类号： C07D401/04 , C07D413/14 , C07D487/04 , C07D513/04
摘要： A compound of formula (I), or a pharmaceutically acceptable derivative thereof, wherein V represents -(CH 2 ) d (O) e -, -CO-, or -CH(C 1-6 alkyl)-; W is -0-, -S(O) a , or -N(R 1 ')-R 1 represents H, C 1-6 alkyl, (CH 2 ) b COR 2 , CO(CH 2 ) b NR 2 R 3 , S0 2 R 2 , ( CH 2 ) c OR 2 , (CH 2 ) c ,NR 2 R 3 , or (CH 2 ) b het 1 ; het 1 represents a saturated or unsaturated heterocycle of from 3 to 8 atoms containing one or more heteroatoms selected from O, N, or S, optionally substituted with C 1-6 alkyl; X and Y independently represent H, C 1-6 alkyl, halogen, OH, CF 3 , OCF 3 , OR 4 ; Z represents -(CH 2 ) f (O) g , -CO- or -CH(C 1-6 alkyl)-; Ring A represents a 4-7 membered, saturated N-containing heterocycle, optionally substituted with OH, and in which optionally at least one ring N is substituted with O;Ring B represents phenyl or a 4-7 membered unsaturated N-containing heterocycle, optionally substituted with OH, halogen, CN, CONH 2 , CF 3 , OCF3, and in which optionally at least one ring N is substituted with O; R 2 and R 3 independently represent H, C 1-6 alkyl [optionally substituted with OH, halogen,N(C 1.6 alkyl) 2 , or C 1.6 alkyloxy], C 1.6 alkyloxy, N(C 1-6 alkyl) 2 , or [C 3-8 cycloalkyl]; or R 2 and R 3 , together with the nitrogen atom to which they are attached independently represent a heterocycle of from 3 to 8 atoms, optionally substituted with C 1-6 alkyl;R4 represents straight or branched C 1-6 alkyl, a and c independently represent 0, 1, or 2; b, e and g independently represent 0 or 1; d and f independently represent 1 or 2;are useful in the treatment of dysmenorrhoea.
摘要翻译：式（I）化合物或其药学上可接受的衍生物，其中V表示 - （CH 2）d（O）e - ， - CO-或-CH（C 1-6烷基） - 。 W是-O - ， - S（O）a或-N（R 1'）-R 1表示H，C 1-6烷基，（CH 2）b -COR 2，CO（CH 2）b NR （CH 2）b CH 2，（CH 2）c，NR 2， het <1>表示3至8个原子的饱和或不饱和杂环，其含有一个或多个选自O，N或S的杂原子，任选被C 1-6烷基取代; X和Y独立地表示H，C 1-6烷基，卤素，OH，CF 3，OCF 3，OR 4; Z表示 - （CH 2）f（O）g，-CO-或-CH（C 1-6烷基） - ; 环A表示任选被OH取代的4-7元饱和的含N的杂环，并且其中任选地至少一个环被O取代;环B表示苯基或4-7元不饱和的含N的杂环，任选地被OH，卤素，CN，CONH 2，CF 3，OCF 3取代，并且其中任选地至少一个环N被O取代; R 2和R 3独立地表示H，C 1-6烷基（任选被OH，卤素，N（C 1-6烷基）2或C 1-6烷氧基取代），C 1-6烷氧基，N（C 1-6 烷基）2或[C 3-8环烷基]; 或R 2和R 3与它们所连接的氮原子一起独立地表示3至8个原子的杂环，任选被C 1-6烷基取代; R 4表示直链或支链C 1-6 烷基，a和c独立地表示0,1或2; b，e和g独立地表示0或1; d和f独立地表示1或2;可用于治疗痛经。

7. 发明申请

WO2004037809A1 TRIAZOLE COMPOUNDS FOR THE TREATMENT OF DYSMENORRHOEA 审中-公开
标题翻译：三唑类化合物用于治疗脑损伤
公开(公告)号：WO2004037809A1
公开(公告)日：2004-05-06
申请号：PCT/IB2003/004587
申请日：2003-10-14
申请人： PFIZER LIMITED , PFIZER INC. , ARMOUR, Robert, Duncan , BAXTER, Andrew, Douglas , BRYANS, Justin, Stephen , DACK, Kevin, Neil , JOHNSON, Patrick, Stephen , LEWTHWAITE, Russell, Andrew , NEWMAN, Julie , RAWSON, David, James , RYCKMANS, Thomas
发明人： ARMOUR, Robert, Duncan , BAXTER, Andrew, Douglas , BRYANS, Justin, Stephen , DACK, Kevin, Neil , JOHNSON, Patrick, Stephen , LEWTHWAITE, Russell, Andrew , NEWMAN, Julie , RAWSON, David, James , RYCKMANS, Thomas
IPC分类号： C07D401/04
CPC分类号： C07D401/04 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/14 , C07D413/04 , C07D413/06 , C07D413/14
摘要： A compound of formula (I), a pharmaceutically acceptable salt or solvate thereof, wherein R' represents C,-C6 alkyl, -(CH 2 ) c -[C 3 -C 8 cycloalkyl]-, -(CH 2 ) C -W or -(CH 2 ) C -Z-(CH 2 ) d W; W represents C 1 -C 6 alkyl, C 1 -C 6 alkyloxy, -C0 2 [C 1 -C 6 alkyl], -CONR 4 R 5 , an optionally substituted phenyl group, NR 4 R 5 , het 2 or het 3 ; Z represents O or S(O) g ; g represents 0, 1 or 2; R 2 represents a phenyl group, optionally fused to a 5- or 6- membered aryl or heterocyclic group which may contain one or more heteroatoms selected from N, O or S; the phenyl group and the optionally fused group being optionally substituted; Ring A represents a 4-, 5- or 6- membered saturated heterocyclic group containing at least one N; Ring B represents a phenyl group or het 1 , each group being optionally substituted; R 7 independently represents H 1 C 1 -C 6 alkyl, OR 3 , -(CH 2 ) e -R 3 or -(CH 2 ) f -O-(CH 2 ) e -R 3 ; at each occurrence R 3 independently represents H 1 C 1 -C 6 alkyl optionally substituted by Y, -(CH 2 ) g [C 3 -C 8 cycloalkyl], phenyl, benzyl, pyridyl or pyrimidyl; at each occurrence R 4 and R 5 independently represent H 1 C l -C 6 alkyl (optionally substituted with C l -C 6 alkyloxy), (CH 2 ) g C0 2 -[C 1 -C 6 alkyl], -S0 2 Me, -(CH 2 ) g [C 3 -C 8 cycloalkyl], S0 2 Me, phenyl, benzyl, pyridyl or pyrimidyl; or R 4 and R 5 together with the N atom to which they are attached represent a heterocyclic group of from 3 to 8 atoms; Y independently represents a phenyl group, NR 4 R 5 or het 4 , the phenyl group being optionally substituted; het 1 represents a 4-, 5- or 6- membered saturated, or unsaturated, heterocyclic group containing at least one N (but which may also contain one or more O or S atoms); het 2 and het 4 represent an optionally substituted 4-, 5-, 6- or 7- membered saturated, or unsaturated, heterocyclic group containing at least one N (but which may 5 also contain one or more O or S atoms); het3 represents an optionally substituted 4-, 5-, 6- or 7- membered saturated, or unsaturated, heterocyclic group containing at least one O (but which may also contain one or mare N or S atoms); at each occurrence R 6 independently represents H 1 C 1 -C 6 alkyl optionally substituted by Y, =(CH 2 ) g [C 3 -C 8 cycloalkyl], phenyl, benzyl, pyridyl or pyrimidyl; a and b independently represent 0 or 1; c,, d, a end g independently represent 0, 1, 2, 3 or 4; . f índeperldently represents 1, 2, 3 or 4; provided that: (i) a + b cannot equal 0; and províded,that,when R 1 represents -(CH 2 ) c -Z-(CH 2 ) d -W and W represents.NR 4 R 5 or any N linked heterocyclic, group then d must not be, 0 or 1; and (iii), provided that when R 2 represents a phenyl group substituted by a group of, formula -(CH 2 ) e OR 3 , -(CH 2 ) e -OCOR 3 or -(CH 2 ) e ,OCOR 3 ;or het 1 ,and/or het 2 are substituted by a group of formula -(CH 2 ) e OR 3 , (CH 2 ),-CO 2 R 3 or -(CH 2 ) e OCOR 3 ; or when R 7 represents -OR 3 or -(CH 2 ) f -0-(CH 2 ) e -R 3 and e is 0; or when W represents a phenyl group substituted with -OR 3 or - C0 2 R 3 and R 3 represents an alkyl group substituted with Y, and Y represents NR 4 R 5 or an N-Finked het 3 ; then, R 3 , must,represent,C 2 -C 6 alkyl substituted with. Y. are useful in the treatment of dysmenorrhoea.
摘要翻译：式（I）化合物，其药学上可接受的盐或溶剂化物，其中R'表示C 1-6烷基， - （CH 2）c - [C 3 -C 8环烷基] - ， - （CH 2）C-W或 - （ CH2）CZ-（CH 2）一页; W表示C1-C6烷基，C1-C6烷氧基，-CO2 [C1-C6烷基]，-CONR4R5，任选取代的苯基，NR4R5，het2，或het <3>; Z表示O或S（O）g; g表示0,1或2; R 2表示苯基，任选地与可含有一个或多个选自N，O或S的杂原子的5-或6-元芳基或杂环基稠合; 苯基和任选稠合基团任选被取代; 环A表示含有至少一个N的4-，5-或6-元饱和杂环基; 环B表示苯基或het 1，每个基团任选被取代; R 7独立地表示H 1 C 1 -C 6烷基，OR 3， - （CH 2）e -R 3或 - （CH 2）f -O-（CH 2）e -R 3; 在每次出现时，R 3独立地表示任选被Y， - （CH 2）g [C 3 -C 8环烷基]，苯基，苄基，吡啶基或嘧啶基取代的H 1 C 1 -C 6烷基; 在每次出现时，R 4和R 5独立地表示H 1 C 1 -C 6烷基（任选被C 1 -C 6烷氧基取代），（CH 2）g CO 2 - [C 1 -C 6烷基]，-SO 2 Me， - （CH 2） C 3 -C 8环烷基]，SO 2 Me，苯基，苄基，吡啶基或嘧啶基; 或R 4和R 5与它们所连接的N原子一起表示3至8个原子的杂环基; Y独立地表示苯基，NR4R5或het4，苯基任选被取代; 表示含有至少一个N（但也可含有一个或多个O或S原子）的4-，5-或6-元饱和或不饱和杂环基; het 2和het 4代表任选被取代的含有至少一个N（但也可以含有一个或多个O或S的N，R 5，R 6，原子）; het3表示含有至少一个O（但也可含有一个或多个N或S原子）的任选取代的4-，5-，6-或7-元饱和或不饱和杂环基; 在每次出现时，R 6独立地表示任选被Y，=（CH 2）g [C 3 -C 8环烷基]，苯基，苄基，吡啶基或嘧啶基取代的H 1 C 1 -C 6烷基; a和b独立地表示0或1; c，d，末端g独立地表示0,1,2,3或4; 。 f，并且代表1,2,3或4; 条件是：（i）a + b不能等于0; 并证明当R 1表示 - （CH 2）c

8. 发明申请

WO2004080964A1 INDOLE DERIVATIVES USEFUL FOR THE TREATMENT OF DISEASES 审中-公开
标题翻译：用于治疗病症的单独使用衍生物
公开(公告)号：WO2004080964A1
公开(公告)日：2004-09-23
申请号：PCT/IB2004/000591
申请日：2004-03-01
申请人： PFIZER LIMITED , PFIZER INC. , BROWN, Alan, Daniel , BRYANS, Justin, Stephen , BUNNAGE, Mark, Edward , GLOSSOP, Paul, Alan , LANE, Charlotte, Alice, Louise , LEWTHWAITE, Russell, Andrew , MANTELL, Simon, John
发明人： BROWN, Alan, Daniel , BRYANS, Justin, Stephen , BUNNAGE, Mark, Edward , GLOSSOP, Paul, Alan , LANE, Charlotte, Alice, Louise , LEWTHWAITE, Russell, Andrew , MANTELL, Simon, John
IPC分类号： C07D209/42
CPC分类号： C07D209/42 , C07D401/12 , C07D417/12
摘要： The invention relates to indole derivatives of formula and to processes for the preparation of, intermediates used in the preparation of, compositions containing and the uses of, such derivatives. The indole derivatives according to the present invention are useful in numerous diseases, disorders and conditions, in particular inflammatory, allergic and respiratory diseases, disorders and conditions.
摘要翻译：本发明涉及式的吲哚衍生物以及制备用于制备含有这些衍生物的组合物和用途的中间体的方法。根据本发明的吲哚衍生物可用于许多疾病，病症和病症，特别是炎症，过敏和呼吸道疾病，病症和病症。

9. 发明申请

WO2005090288A1 PHENYLAMINOETHANOL DERIVATES AS BETA2 RECEPTOR AGONISTS 审中-公开
标题翻译：苯甲酰胺醇作为BETA2受体激动剂衍生物
公开(公告)号：WO2005090288A1
公开(公告)日：2005-09-29
申请号：PCT/IB2005/000611
申请日：2005-03-10
申请人： PFIZER LIMITED , PFIZER INC. , BROWN, Alan, Daniel , BRYANS, Justin, Stephen , GLOSSOP, Paul, Alan , LANE, Charlotte, Alice, Louise , MANTELL, Simon, John
发明人： BROWN, Alan, Daniel , BRYANS, Justin, Stephen , GLOSSOP, Paul, Alan , LANE, Charlotte, Alice, Louise , MANTELL, Simon, John
IPC分类号： C07C237/42
CPC分类号： C07C237/42 , C07C237/20 , C07C275/24 , C07C311/46
摘要： The invention relates to compounds of formula (1) and to processes for the preparation of, intermediates used in the preparation of, compositions containing and the uses of, such derivatives. The compounds according to the present invention are useful in numerous diseases, disorders and conditions, in particular inflammatory, allergic and respiratory diseases, disorders and conditions.
摘要翻译：本发明涉及式（1）化合物以及制备用于制备含这些衍生物的组合物和用途的中间体的方法。根据本发明的化合物可用于许多疾病，病症和病症，特别是炎症，过敏和呼吸道疾病，病症和病症。

10. 发明申请

WO2004108675A1 2-AMINO-PYRIDINE DERIVATIVES AS BETA-2 ADRENORECEPTOR AGONISTS 审中-公开
标题翻译： 2-氨基吡啶衍生物作为2-ADRENORECEPTOR AGONISTS
公开(公告)号：WO2004108675A1
公开(公告)日：2004-12-16
申请号：PCT/IB2004/001735
申请日：2004-05-21
申请人： PFIZER LIMITED , PFIZER INC. , BROWN, Alan, Daniel , BRYANS, Justin, Stephen , LANE, Charlotte, Alice, Louise , MANTELL, Simon, John
发明人： BROWN, Alan, Daniel , BRYANS, Justin, Stephen , LANE, Charlotte, Alice, Louise , MANTELL, Simon, John
IPC分类号： C07D213/73
CPC分类号： C07D213/73
摘要： The invention relates to compounds of formula (1) and to processes for the preparation of, intermediates used in the preparation of, compositions containing and the uses of, such derivatives. The compounds according to the present invention are useful in numerous diseases, disorders and conditions, in particular inflammatory, allergic and respiratory diseases, disorders and conditions.
摘要翻译：本发明涉及式（1）化合物以及制备用于制备含这些衍生物的组合物和用途的中间体的方法。根据本发明的化合物可用于许多疾病，病症和病症，特别是炎症，过敏和呼吸道疾病，病症和病症。

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