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1. 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

2. 发明申请

WO2005123702A1 NEUTRAL ENDOPEPTIDASE INHIBITOR POLYMORPH 审中-公开
标题翻译：中性内切酶抑制剂多聚体
公开(公告)号：WO2005123702A1
公开(公告)日：2005-12-29
申请号：PCT/IB2005/001911
申请日：2005-06-03
申请人： PFIZER LIMITED , PFIZER INC. , DACK, Kevin, Neil , GYMER, Geoffrey, Edward
发明人： DACK, Kevin, Neil , GYMER, Geoffrey, Edward
IPC分类号： C07D263/32
CPC分类号： C07D263/32
摘要： Disclosed are (2S)-2-{1-[(1S)-1-Isobutoxycarbonyl-2-(5-phenyl-oxazol-2-yl)-ethylcarbamoyl]-cyclopentylmethyl}-4-methoxy-butyric, Potassium-(2S)-2-{1-[(1S)-1-Isobutoxycarbonyl-2-(5-phenyl-oxazol-2-yl)-ethylcarbamoyl]-cyclopentylmethyl}-4-methoxy-butyrate, monohydrate and its Form I polymorph. Also disclosed are compositions of the described forms, kits including the described forms, and methods of using the described forms for the treatment diseases or disorders where the use of a neutral endopeptidase inhibitor is indicated, including cardiovascular diseases and conditions.
摘要翻译：公开了（2S）-2- {1 - [（1S）-1-异丁氧基羰基-2-（5-苯基 - 恶唑-2-基） - 乙基氨基甲酰基] - 环戊基甲基} -4-甲氧基 - 丁酸钾 - （2S ）-2- {1 - [（1S）-1-异丁氧基羰基-2-（5-苯基 - 恶唑-2-基） - 乙基氨基甲酰基] - 环戊基甲基} -4-甲氧基 - 丁酸乙酯，一水合物及其I型多晶型物。还公开了所述形式的组合物，包括所述形式的试剂盒，以及使用所述形式用于治疗使用中性内肽酶抑制剂的疾病或病症（包括心血管疾病和病症）的方法。

3. 发明申请

WO2005049616A1 5,7-DIAMINOPYRAZOLO ‘4,3-D!PYRIMIDINES WITH PDE-5 INHIBITING ACTIVITY 审中-公开
标题翻译：具有PDE-5抑制活性的5,7-二氨基吡唑“4,3-D”嘧啶
公开(公告)号：WO2005049616A1
公开(公告)日：2005-06-02
申请号：PCT/IB2004/003747
申请日：2004-11-12
申请人： PFIZER LIMITED , PFIZER INC. , BELL, Andrew, Simon , BROWN, David, Graham , DACK, Kevin, Neil , FOX, David, Nathan, Abraham , MARSH, Ian, Roger , MORRELL, Andrew, Ian , PALMER, Michael, John , WINSLOW, Carol, Ann
发明人： BELL, Andrew, Simon , BROWN, David, Graham , DACK, Kevin, Neil , FOX, David, Nathan, Abraham , MARSH, Ian, Roger , MORRELL, Andrew, Ian , PALMER, Michael, John , WINSLOW, Carol, Ann
IPC分类号： C07D487/04
CPC分类号： C07D487/04 , Y02P20/582
摘要： This invention relates to compounds of formula (I).
摘要翻译：本发明涉及式（I）化合物。

4. 发明申请

WO2004056787A1 CYCLOPENTYL GLUTARAMIDES AND THEIR USE AS NEUTRAL ENDOPEPTIDASE INHIBITORS 审中-公开
标题翻译：环戊二烯酸和其作为中性内切酶抑制剂的用途
公开(公告)号：WO2004056787A1
公开(公告)日：2004-07-08
申请号：PCT/IB2003/005981
申请日：2003-12-12
申请人： PFIZER LIMITED , PFIZER INC. , DACK, Kevin, Neil , OWEN, Dafydd, Rhys , WATSON, Christine, Anne, Louise
发明人： DACK, Kevin, Neil , OWEN, Dafydd, Rhys , WATSON, Christine, Anne, Louise
IPC分类号： C07D263/32
CPC分类号： C07D231/12 , C07D263/32 , C07D271/06 , C07D271/10
摘要： The invention relates to NEP inhibitors for treating cardiovascular disorders wherein R 1 is C 1 -C 6 alkyl, C 1 -C 6 alkoxyC 1 -C 3 alkyl or C 1 -C 6 alkoxyC 1 -C 6 alkoxyC,-C 3 alkyl; R 2 is hydrogen or C 1 -C 6 alkyl; L is an aromatic heterocyclic ring, optionally substituted with C, C 6 alkyl or halo; R 3 is C 1 -C 6 alkyl optionally substituted by halo, alkoxy, haloalkoxy, alkylthio, haloalkylthio or nitrile group, or R 3 is phenyl or aromatic heterocyclyl each of which may be independently substituted by one or more alkyl, halo, haloalkyl, alkoxy, haloalkoxy, alkylthio, haloalkylthio or nitrile group; R 4 and R 5 are either both hydrogen, or one of R 4 and R 5 is hydrogen and the other is a biolabile ester-forming group that in the body of a patient is replaced by hydrogen; p is 0, 1 or 2; and q is 1 or 2.
摘要翻译：本发明涉及用于治疗心血管疾病的NEP抑制剂，其中R 1是C 1 -C 6烷基，C 1 -C 6烷氧基C 1 -C 3烷基或C 1 -C 6烷氧基C 1 -C 6烷氧基C 1 -C 3烷基; R 2是氢或C 1 -C 6烷基; L是任选被C 1 -C 6烷基或卤素取代的芳族杂环; R 3是任选被卤素，烷氧基，卤代烷氧基，烷硫基，卤代烷硫基或腈基取代的C 1 -C 6烷基，或R 3是苯基或芳族杂环基，其各自可以被一个或多个烷基，卤素，卤代烷基，烷氧基，卤代烷氧基，烷硫基，卤代烷硫基或腈基; R 4和R 5都是氢，R 4和R 5中的一个是氢，另一个是生物不稳定酯形成基团，在患者体内被氢代替; p为0,1或2; q为1或2。

5. 发明申请

WO2002079203A1 PHARMACEUTICALLY ACTIVE COMPOUNDS 审中-公开
标题翻译：药物活性化合物
公开(公告)号：WO2002079203A1
公开(公告)日：2002-10-10
申请号：PCT/IB2002/000854
申请日：2002-03-19
申请人： PFIZER LIMITED , PFIZER INC. , ALLERTON, Charlotte, Moira, Norfor , DACK, Kevin, Neil , KEMP, Mark, Ian
发明人： ALLERTON, Charlotte, Moira, Norfor , DACK, Kevin, Neil , KEMP, Mark, Ian
IPC分类号： C07D487/04
CPC分类号： C07D487/04
摘要： Compounds of general formula (1): wherein R 1 , R 2 , R 3 , R 4 , X, Y and A have the meanings given herein which are useful in the curative and prophylactic treatment of a medical condition for which inhibition of a cyclic guanosine 3', 5'- monophosphate phosphodiesterase (e.g. cGMP PDE5) is desired.
摘要翻译：通式（1）的化合物：其中R 1，R 2，R 3，R 4，R 5，R 5， X，Y和A具有本文给出的含义，其可用于治疗性和预防性治疗抑制环鸟苷3'，5'-单磷酸磷酸二酯酶（例如cGMP PDE5）的医学病症，是期望的。

6. 发明公开

EP0901470A1 INDOLE DERIVATIVES USEFUL AS ENDOTHELIN RECEPTOR ANTAGONISTS 失效
标题翻译：吲哚衍生物作为内皮素受体拮抗剂USED
公开(公告)号：EP0901470A1
公开(公告)日：1999-03-17
申请号：EP97920690.0
申请日：1997-04-11
申请人： PFIZER INC. , Pfizer Limited
发明人： RAWSON, David, James , DACK, Kevin, Neil , DICKINSON, Roger, Peter , JAMES, Kim
IPC分类号： A61K31 , A61P9 , A61P11 , A61P13 , A61P15 , A61P43 , C07D209 , C07D405 , C07D409 , C07D413
CPC分类号： C07D405/06 , C07D209/18 , C07D405/14 , C07D409/14 , C07D413/14
摘要： Compounds of formula (I), and their pharmaceutically acceptable derivatives, wherein R?1 and R2¿ are optional substituents and independently represent C¿1-6? alkyl, C2-6 alkenyl [optionally substituted by CO2H or CO2(C1-6 alkyl)], C2-6 alkynyl, halogen, C1-3 perfluoroalkyl, (CH2)mAr?1, (CH¿2)mHet1, (CH2)mCONR?7R8, (CH¿2)mCO2R8, O(CH¿2?)qCO2R?8, (CH¿2)mCOR8, (CH2)mOR8, O(CH¿2?)pOR?8, (CH¿2)mNR7R8, CO2(CH2)qNR?7R8, (CH¿2)mCN, S(O)nR8, SO2NR7R8, CONH(CH¿2)mAr?1 or CONH(CH¿2?)mHet?1; R3¿ represents H, C¿1-6? alkyl, (CH2)pNR?9R10, SO¿2R10, SO2NR?9R10, (CH¿2)mCOR10, C2-6 alkenyl, C2-6 alkynyl, (CH2)mCONR?9R10, (CH¿2)mCO2R10, (CH2)pCN, (CH2)pR10 or (CH¿2?)pOR?10; R4¿ represents H or C¿1-6? alkyl; R?5¿ represents H or OH; R6 represents phenyl optionally fused to a heterocyclic ring, the group as a whole being optionally substituted; R7-10 are fully defined herein and may independently represent Ar?2 or Het2¿; Z represents CO¿2?H, CONH(tetrazol-5-yl), CONHSO2O(C1-4 alkyl), CO2Ar?3, CO¿2(C1-6 alkyl), tetrazol-5-yl, CONHSO2Ar3, CONHSO¿2?(CH2)qAr?3¿ or CONHSO¿2?(C1-6 alkyl); Ar?1-3¿ independently represent phenyl, naphthyl, or an aromatic heterocycle, which groups are optionally fused and optionally substituted; and Het1 and Het2 independently represent a non-aromatic heterocycle which is optionally substituted; are useful in the treatment of restenosis, renal failure and pulmonary hypertension.

7. 发明公开

EP1047665A1 MATRIX METALLOPROTEASE INHIBITORS 有权
标题翻译： MATRIXMETALLOPROTEINASEINHIBITOREN
公开(公告)号：EP1047665A1
公开(公告)日：2000-11-02
申请号：EP98966429.7
申请日：1998-12-23
申请人： Pfizer Limited , PFIZER INC.
发明人： FRAY, Michael, Jonathan , DICKINSON, Roger, Peter , DACK, Kevin, Neil
IPC分类号： C07C237/22 , C07C259/06 , A61K31/16
CPC分类号： C07D213/75 , C07B2200/07 , C07C237/22 , C07C259/06 , C07C259/18 , C07C2602/08 , C07D317/34 , Y02P20/55
摘要： Compounds of formula (I) or pharmaceutically acceptable salts thereof, or solvates of either entity, wherein the substituents have the values described herein, are useful as matrix metalloprotease (MMP) inhibitors.
摘要翻译：式（I）化合物或其药学上可接受的盐，或任一实体的溶剂化物，其中取代基具有本文所述的值，可用作基质金属蛋白酶（MMP）抑制剂

8. 发明授权

EP1047665B1 MATRIX METALLOPROTEASE INHIBITORS 有权
标题翻译：基质金属蛋白酶
公开(公告)号：EP1047665B1
公开(公告)日：2003-10-22
申请号：EP98966429.7
申请日：1998-12-23
申请人： Pfizer Limited , PFIZER INC.
发明人： FRAY, Michael, Jonathan , DICKINSON, Roger, Peter , DACK, Kevin, Neil
IPC分类号： C07C237/22 , C07C259/06 , A61K31/16
CPC分类号： C07D213/75 , C07B2200/07 , C07C237/22 , C07C259/06 , C07C259/18 , C07C2602/08 , C07D317/34 , Y02P20/55
摘要： Compounds of formula (I) or pharmaceutically acceptable salts thereof, or solvates of either entity, wherein the substituents have the values described herein, are useful as matrix metalloprotease (MMP) inhibitors.

9. 发明授权

EP0901470B1 INDOLE DERIVATIVES USEFUL AS ENDOTHELIN RECEPTOR ANTAGONISTS 失效
标题翻译：吲哚衍生物作为内皮素受体拮抗剂USED
公开(公告)号：EP0901470B1
公开(公告)日：2004-03-31
申请号：EP97920690.1
申请日：1997-04-11
申请人： PFIZER INC. , Pfizer Limited
发明人： RAWSON, David, James , DACK, Kevin, Neil , DICKINSON, Roger, Peter , JAMES, Kim
IPC分类号： C07D209/18 , C07D405/06 , A61K31/40
CPC分类号： C07D405/06 , C07D209/18 , C07D405/14 , C07D409/14 , C07D413/14
摘要： Compounds of formula (I), and their pharmaceutically acceptable derivatives, wherein R?1 and R2¿ are optional substituents and independently represent C¿1-6? alkyl, C2-6 alkenyl [optionally substituted by CO2H or CO2(C1-6 alkyl)], C2-6 alkynyl, halogen, C1-3 perfluoroalkyl, (CH2)mAr?1, (CH¿2)mHet1, (CH2)mCONR?7R8, (CH¿2)mCO2R8, O(CH¿2?)qCO2R?8, (CH¿2)mCOR8, (CH2)mOR8, O(CH¿2?)pOR?8, (CH¿2)mNR7R8, CO2(CH2)qNR?7R8, (CH¿2)mCN, S(O)nR8, SO2NR7R8, CONH(CH¿2)mAr?1 or CONH(CH¿2?)mHet?1; R3¿ represents H, C¿1-6? alkyl, (CH2)pNR?9R10, SO¿2R10, SO2NR?9R10, (CH¿2)mCOR10, C2-6 alkenyl, C2-6 alkynyl, (CH2)mCONR?9R10, (CH¿2)mCO2R10, (CH2)pCN, (CH2)pR10 or (CH¿2?)pOR?10; R4¿ represents H or C¿1-6? alkyl; R?5¿ represents H or OH; R6 represents phenyl optionally fused to a heterocyclic ring, the group as a whole being optionally substituted; R7-10 are fully defined herein and may independently represent Ar?2 or Het2¿; Z represents CO¿2?H, CONH(tetrazol-5-yl), CONHSO2O(C1-4 alkyl), CO2Ar?3, CO¿2(C1-6 alkyl), tetrazol-5-yl, CONHSO2Ar3, CONHSO¿2?(CH2)qAr?3¿ or CONHSO¿2?(C1-6 alkyl); Ar?1-3¿ independently represent phenyl, naphthyl, or an aromatic heterocycle, which groups are optionally fused and optionally substituted; and Het1 and Het2 independently represent a non-aromatic heterocycle which is optionally substituted; are useful in the treatment of restenosis, renal failure and pulmonary hypertension.

10. 发明公开

EP0579618A1 PYRIDINE- AND IMIDAZOLE-DERIVED AGENTS FOR CARDIOVASCULAR DISEASES 失效
标题翻译：吡啶和咪唑试剂衍生的心血管疾病。
公开(公告)号：EP0579618A1
公开(公告)日：1994-01-26
申请号：EP92906439.0
申请日：1992-03-17
申请人： Pfizer Limited , PFIZER INC.
发明人： DICKINSON, Roger, Peter , DACK, Kevin, Neil , STEELE, John
IPC分类号： A61K31 , A61P7 , A61P9 , A61P43 , C07D213 , C07D233 , C07D401 , C07D405 , C07D409 , C07D521
CPC分类号： C07D231/12 , C07D213/55 , C07D213/65 , C07D233/56 , C07D249/08 , C07D401/12 , C07D409/12
摘要： On décrit des composés de formule (I), ou un ester biolabile de ces composés, ou un de leurs sels pharmaceutiquement acceptables où R1, R2, R3 et R4 sont chacun choisis indépendamment parmi H ou C1-C4 alkyle; R5 est (CH2)mSO2R6, (CH2)mNHSO2R6 où (CH2)mNHCOR7; R6 et R7 sont C1-C6 alkyle, C1-C3 perfluoroalkyle(CH2)n, C3-C6 cycloalkyle(CH2)n, aryle (CH2)n ou hétéroaryle(CH2)n; ou bien R6 est NR8R9; R8 est H ou C1-C4 alkyle; R9 est C1-C6 alkyle, C3-C6 cycloalkyle(CH2)n, aryle (CH2)n ou hétéroaryle (CH2)n; ou bien R8 et R9 forment, avec l'atome d'azote auquel ils sont liés, un anneau hétérocyclique à 5 - 7 membres, qui peut éventuellement comporter une liaison double carbone-carbone ou une autre liaison d'hétéroatomes choisis parmi O, S, NH, N(C1-C4 alkyle) et N(C1-C5 alcanoyle), et qui peuvent être substitués éventuellement par un à trois substituants, chacun étant sélectionné indépendamment parmi C1-C4 alkyle et C1-C4 alcoxy, et qui peuvent éventuellement être fusionnés au benzo; X est CH2, CHCH3, C(OH)CH3, C=CH2 ou O; m est 0 ou 1; n est 0, 1, 2, ou 3; et Het est 3- ou 4- pyridyle ou 1-imidaxolyle; sous réserve que lorsque Het est 1-imidazolyle, alors X soit CH2 ou CHCH3. Lesdits composés sont à la fois des inhibiteurs de synthétase de thromboxane A2 et des antagonistes de thromboxane A2/endoperoxyde, et sont utiles pour le traitement de maladies dans lesquelles la thromboxane A2 est l'agent pathogène.

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