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    INDOLE DERIVATIVES AS 5-HT1 AGONISTS
    2.
    发明公开
    INDOLE DERIVATIVES AS 5-HT1 AGONISTS 失效
    衍生ALS INDOL 5-HT1激动剂。

    公开(公告)号：EP0635017A1

    公开(公告)日：1995-01-25

    申请号：EP93907216.0

    申请日：1993-03-10

    申请人： PFIZER INC.

    发明人： MACOR, John, E. ,  WYTHES, Martin, J.

    IPC分类号： A61K31 ,  A61P3 ,  A61P9 ,  A61P25 ,  A61P43 ,  C07D207 ,  C07D209 ,  C07D263 ,  C07D403 ,  C07D413

    CPC分类号： C07D403/06 ,  C07D403/14 ,  C07D413/10 ,  C07D413/12 ,  C07D413/14

    摘要： Compounds of formula (I) where W is (i), (ii), (iii), (iv), (v), (vi), or (vii); n is 0, 1 or 2; m is 0, 1, 2, or 3; Y and G are each independently oxygen or sulfur; Z is -O-, -S-, -NH-, or -CH2; R1 is hydrogen, C1 to C8 alkyl, substituted C1 to C8 alkyl substituted with one hydroxy, C3 to C8 alkenyl, C3 to C8 alkynyl, aryl, C1 to C3 alkylaryl, C1 to C3 alkylheteroaryl, or -Q-R4; R2 and R3 are each independently hydrogen, C1 to C6 alkyl, aryl, C1 to C3 alkylaryl, or C1 to C3 alkylheteroaryl; R4 is cyano, trifluoromethyl, -COR9, -CO2R9, -CONR9R10, -OR9, -SO2NR9R10, or -S(O)qR9; R9 and R10 are each independently hydrogen, C1 to C8 alkyl, C1 to C3 alkylaryl, aryl, or R9 and R10 may together be taken to form a three-to seven-membered alkyl ring or a three-to seven-membered heteroalkyl ring having 1 heteroatom of O; Q is C1 to C3 alkyl; R11 is hydrogen, -OR12, or -NHCOR12; R12 is hydrogen, C1 to C6 alkyl, aryl, or C1 to C3 alkylaryl; q is 0, 1, or 2; a first chiral carbon is designated by an asterisk; a second chiral carbon is designated by #; and the above aryl groups and the aryl moieties of the above alkyl-aryl groups are independently selected from phenyl and substituted phenyl, wherein said substituted phenyl may be substituted with one to three groups selected from C1 to C4 alkyl, halogen, hydroxy, cyano, carboxamido, nitro, and C1 to C4 alkoxy, and the pharmaceutically acceptable salts thereof. These compounds are useful in treating migraine and other disorders are new. These compounds are useful phsychotherapeutics and are potent serotonin (5-HT1) agonists and may be used in the treatment of depression, anxiety, eating disorders, obesity, drug abuse, cluster headache, migraine, pain, and chronic paroxysmal hemicrania and headache associated with vascular disorders, and other disorders arising from deficient serotonergic neurotransmission. The compounds can also be used as centrally acting antihypertensives and vasodilators.

    INDOLE DERIVATIVES AS 5-HT1 AGONISTS
    3.
    发明公开
    INDOLE DERIVATIVES AS 5-HT1 AGONISTS 失效
    INDOL DERIVATE ALS 5-HT1 AGONISTE。

    公开(公告)号：EP0629199A1

    公开(公告)日：1994-12-21

    申请号：EP93906214.0

    申请日：1993-03-03

    申请人： PFIZER INC.

    发明人： MACOR, John, E. ,  NOWAKOWSKI, Jolanta, T.

    IPC分类号： A61K31 ,  A61P1 ,  A61P3 ,  A61P9 ,  A61P25 ,  A61P43 ,  C07D207 ,  C07D413 ,  C07D417

    CPC分类号： C07D413/14 ,  C07D417/14

    摘要： Composés de la formule (I) dans laquelle A représente une liaison directe, C1-C4 alkyle, ou C1-C4 alcényle; n vaut 0, 1 ou 2; R1 représente hydrogène, C1-C6 alkyle, aryle, C1-C3 alkylaryle, C1-C3 alkylhétéroaryle, ou -(CH2)mR6; W, X, Y et Z représentent chacun indépendamment oxygène, soufre, azote ou carbone, à condition qu'au moins élément parmi W, X, Y ou Z représente azote; R2, R3, R4 et R5 représentent chacun indépendamment hydrogène, C1-C6 alkyle, aryle, C1-C3 arylaryle, C1-C3 alkylhétéroaryle, halogène, cyano, trifluorométhyle, nitro, -OR7, -NR7R8, -(CH2)sOR7, -SR7, -SO2NR7R8, -NR7SO2R8, -NR7CO2R8, -CONR7R8, ou -CO2R7; R2 et R3, ou R3 et R4, ou R4 et R5 peuvent former ensemble un noyau alkyle contenant 5 à 7 éléments, un noyau aryle à six éléments, un noyau hétéroalkyle contenant de 5 à 7 élements ainsi que 1 ou 2 hétéroatomes de N, O ou S; R6 représente cyano, trifluorométhyle ou -OR9; R7, R8 et R9 représentent chacun indépendamment hydrogène, C1-C6 alkyle, -(CH2)mR10, C1-C3 alkylaryle ou aryle; R7 et R8 peuvent former ensemble un noyau C4-C7 alkyle; R10 représente cyano, trifluorométhyle, ou C1-C4 alcoxy; R11 représente hydrogène, -OR12 ou -NHCOR12; R12 représente C1-C6 alkyle, aryle ou C1-C3 alkyl-aryle; m vaut 1, 2 ou 3; s vaut 0, 1, 2 ou 3; et les groupes aryle et les fractions aryle sus-mentionnés des groupes alkylaryle sont indépendamment choisis entre phényle et phényle substitué, ledit phényle substitué pouvant être substitué avec un à trois groupes choisis entre C1 à C4 alkyle, halogène, hydroxy, cyano, carboxamido, nitro et C1 à C4 alcoxy, et leurs sels pharmaceutiquement acceptables. Ces composés sont utiles comme substances psychothérapeutiques, sont des antagonistes de sérotonine (5-HT) puissants et peuvent être utilisés dans le traitement de la dépression, de l'anxiété, des troubles de l'alimentation, de l'obésité, de la toxicomanie, des céphalées, de la migraine, de douleurs, et de l'hémicrânie paroxystique chronique et des céphalées associées aux troubles vasculaires ainsi que d'autres

    摘要翻译： PCT No.PCT / US93 / 01667 Sec。 371日期：1994年8月19日 102（e）日期1994年8月19日PCT 1993年3月3日PCT公布。 公开号WO93 / 18032 （I）其中A表示直接键的式（I）化合物，C 1 -C 4烷基或C 1 -C 4烯基; n为0,1或2; W，X，Y和Z各自独立地为氧，硫，氮或碳，条件是W，X，Y或Z中的至少一个为氮。 这些化合物是有用的精神治疗药物，是有效的5-羟色胺（5-HT1）激动剂，可用于治疗抑郁症，焦虑症，进食障碍，肥胖症，药物滥用，丛集性头痛，偏头痛，疼痛和慢性阵发性血尿素和与血管相关的头痛 障碍和由血清素能神经传递缺陷引起的其他疾病。 该化合物也可用作中枢作用的抗高血压药和血管扩张剂。

    ACYLAMINOINDOLE DERIVATIVES AS 5-HT1 AGONISTS
    7.
    发明授权
    ACYLAMINOINDOLE DERIVATIVES AS 5-HT1 AGONISTS 失效
    作为5-HT1激动剂的乙酰氨基吲哚衍生物

    公开(公告)号：EP0635015B1

    公开(公告)日：1997-01-29

    申请号：EP93907096.7

    申请日：1993-03-04

    申请人： PFIZER INC.

    发明人： MACOR, John, E.

    IPC分类号： C07D403/06 ,  A61K31/40 ,  C07D403/14

    CPC分类号： C07D403/06 ,  C07D403/14

    摘要： Compounds of formula (I) where n is 0, 1, or 2; m is 0 or 1; Y and W are each an amino acid residue; R1 is hydrogen, C1-C6 alkyl, C3-C6 alkenyl, C3-C6 alkynyl, aryl, C1-C3 alkylaryl, or C1-C3 alkylheteroaryl, and -(CH2)pR3; R2 is CF3, C1-C6 alkyl, aryl, C1-C3 alkylaryl, and -OR5; R3 is cyano, trifluoromethyl, or -OR4; R4 is hydrogen, C1-C6 alkyl, C1-C3 alkylaryl, or aryl; R5 is C1-C6 alkyl, C1-C3 alkylaryl, or aryl; R6 is hydrogen, -OR7, or -NHCOR7; R7 is hydrogen, C1 to C6 alkyl, aryl, or C1 to C3 alkyl-aryl; p is 1, 2, or 3; and the above aryl groups and the aryl moieties of the above alkyl-aryl groups are independently selected from phenyl and substituted phenyl, wherein said substituted phenyl may be substituted with one to three groups selected from C1 to C4 alkyl, halogen, hydroxy, cyano, carboxamide, nitro, and C1 to C4 alkoxy and the pharmaceutically acceptable salts thereof. These compounds are useful in treating migraine and other disorders. These compounds are useful psychotherapeutics and are potent serotonin (5-HT1) agonists and may be used in the treatment of depression, anxiety, eating disorders, obesity, drug abuse, cluster headache, migraine, pain, and chronic paroxysmal hemicrania and headache associated with vascular disorders, and other disorders arising from deficient serotonergic neurotransmission. The compounds can also be used as centrally acting antihypertensives and vasodilators.

    摘要翻译： 其中n为0,1或2的式（I）化合物; m是0或1; Y和W各自是氨基酸残基; R 1为氢，C 1 -C 6烷基，C 3 -C 6烯基，C 3 -C 6炔基，芳基，C 1 -C 3烷基芳基或C 1 -C 3烷基杂芳基和 - （CH 2）p R 3; R2是CF3，C1-C6烷基，芳基，C1-C3烷基芳基和-OR5; R3是氰基，三氟甲基或-OR4; R4是氢，C1-C6烷基，C1-C3烷基芳基或芳基; R5是C1-C6烷基，C1-C3烷基芳基或芳基; R6是氢，-OR7或-NHCOR7; R7是氢，C1-C6烷基，芳基或C1-C3烷基 - 芳基; p是1,2或3; 并且上述芳基和上述烷基 - 芳基的芳基部分独立地选自苯基和取代的苯基，其中所述的取代的苯基可以被1-3个选自C1-C4烷基，卤素，羟基，氰基， 甲酰胺，硝基和C1-C4烷氧基及其药学上可接受的盐。 这些化合物可用于治疗偏头痛和其他疾病。 这些化合物是有用的精神治疗药物，是有效的血清素（5-HT1）激动剂，可用于治疗抑郁症，焦虑症，进食障碍，肥胖症，药物滥用，丛集性头痛，偏头痛，疼痛以及慢性阵发性偏头痛和头痛 血管疾病以及由于缺乏5-羟色胺能神经传递引起的其他疾病。 该化合物也可以用作中枢作用的抗高血压药和血管扩张药。

    NAPHTHALENE DERIVATIVES
    9.
    发明公开
    NAPHTHALENE DERIVATIVES 失效
    萘衍生物

    公开(公告)号：EP0689536A1

    公开(公告)日：1996-01-03

    申请号：EP94911377.0

    申请日：1994-02-15

    申请人： PFIZER INC.

    发明人： CHENARD, Bertrand, L. ,  MACOR, John, E. ,  SEGELSTEIN, Barbara, E.

    IPC分类号： C07D295 ,  A61K31 ,  A61P9 ,  A61P25 ,  A61P43 ,  C07D207 ,  C07D211 ,  C07D213 ,  C07D215 ,  C07D235 ,  C07D239 ,  C07D277 ,  C07D401 ,  C07D471

    CPC分类号： C07D213/74 ,  C07D207/09 ,  C07D211/26 ,  C07D211/34 ,  C07D213/75 ,  C07D213/84 ,  C07D213/85 ,  C07D235/06 ,  C07D239/26 ,  C07D277/42 ,  C07D295/033 ,  C07D295/073 ,  C07D295/096 ,  C07D295/112 ,  C07D295/135 ,  C07D295/155 ,  C07D401/10 ,  C07D471/04

    摘要： Compounds of formula (I) where R1 is of formulae (II), (III), or (IV), or (V); R2 is -R4, -O-R4, -O-S(O)2-R4, -NR4R5, R4-(CH2)b-NH(C=X)-(CH2)c-, R4-(CH2)b-O(C=O)NH-(CH2)c-(C=O)NH-, R4-(C=O)NH-(C=O)NH-, -(CH2)b-NH(C=X)-(CH2)c-R4, R4-(CH2)b-O(C=O)-(CH2)c-, -(CH2)b-O(C=O)-(CH2)c-R4, -NH(C=X)NH-R4, R4-O(C=O)O-, -O(C=O)NH-R4, R4-O(C=O)NH-, -(CH2)b-(C=O)-(CH2)c-R4, -NH-S(O)2-R4, -C(OH)R4R5, -CH(OH)-R4, -(C=O)-NR4R5, -CN, -NO2, substituted C1 to C6 alkyl, substituted or unsubstituted C1 to C6 alkenyl, or substituted or unsubstituted C1 to C6 alkynyl, said substituted moieties substituted with a moiety of the formulae -R4, -R4R5, -O-R4, or -S(O)d-R4; R3 is hydrogen, C1 to C6 alkyl, C1 to C6 alkylaryl, or aryl; R4 and R5 are each independently (XV), (XVI), (XVII), hydrogen, -CF3, C1 to C6 alkyl, C1 to C6 alkylaryl, with the proviso that when R2 is -R4 or -OR4, R4 is not hydrogen or C1 to C6 alkyl. These compounds are useful psychotherapeutics and are potent serotonin (5-HT1) agonists and antagonists and may be used in the treatment of depression, anxiety, eating disorders, obesity, drug abuse, cluster headache, migraine, pain and chronic paroxysmal hemicrania and headache associated with vascular disorders, and other disorders arising from deficient serotonergic neurotransmission. The compounds can also be used as centrally acting antihypertensives and vasodilators.

    摘要翻译： 其中R1为式（II），（III）或（IV）或（V）的式（I）化合物; R2是-R4，-O-R4，-OS（O）2-R4，-NR4R5，R4-（CH2）b-NH（C = X） - （CH2）c-，R4-（CH2） （C = O）NH-，（C = O）NH-，（C = O）NH-， - （CH 2）b -NH（C = X） - （CH 2） （C = O） - （CH 2）b -O（C = O） - （CH 2） （C = O）O-，-O（C = O）NH-R 4，R 4 -O（C = O）NH-， - （CH 2）b - （O）2 -R 4，-C（OH）R 4 R 5，-CH（OH）-R 4， - （C = O）-NR 4 R 5，-CN，-NO 2，取代的C 1至C 6烷基 取代或未取代的C1至C6烯基或取代或未取代的C1至C6炔基，所述取代的部分被式-R4，-R4R5，-O-R4或-S（O）d-R4的部分取代; R3是氢，C1-C6烷基，C1-C6烷基芳基或芳基; （XV），（XVI），（XVII），氢，-CF 3，C 1 -C 6烷基，C 1 -C 6烷基芳基，条件是当R 2是-R 4或-OR 4时，R 4不是氢 或C1至C6烷基。 这些化合物是有用的精神治疗药物并且是有效的血清素（5-HT1）激动剂和拮抗剂，并且可以用于治疗抑郁症，焦虑症，饮食失调，肥胖症，药物滥用，丛集性头痛，偏头痛，疼痛和慢性阵发性偏头痛以及头痛相关 伴有血管障碍和由于缺乏5-羟色胺能神经传递引起的其他障碍。 该化合物也可以用作中枢作用的抗高血压药和血管扩张药。

    5-(HETERO- OR CARBOCYCLYLAMINO)-INDOLE DERIVATIVES, THEIR PREPARATION AND THEIR USE AS 5-HT1 AGONISTS
    10.
    发明授权
    5-(HETERO- OR CARBOCYCLYLAMINO)-INDOLE DERIVATIVES, THEIR PREPARATION AND THEIR USE AS 5-HT1 AGONISTS 失效
    5-（异或CARBOCYCLYLAMINO） - 吲哚衍生物，其制备及其作为5-HT1激动剂

    公开(公告)号：EP0619805B1

    公开(公告)日：2000-03-15

    申请号：EP92922831.0

    申请日：1992-10-06

    申请人： PFIZER INC.

    发明人： MACOR, John, E.

    IPC分类号： C07D209/16 ,  C07D401/12 ,  C07D403/06 ,  C07D403/12 ,  C07D413/12 ,  C07D417/12 ,  C07D473/34 ,  A61K31/40

    CPC分类号： C07D401/04 ,  C07D209/16 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/06 ,  C07D403/12 ,  C07D413/10 ,  C07D413/12 ,  C07D417/12 ,  C07D417/14 ,  C07D473/34

    摘要： Compounds of formula (I) wherein Z is (a) or (b); R1 is (c), (d), (e) or (f); X is O, NH or S; A, B, D, E, and F are each independently C, N, O, or S; R2, R3, R4, R5 and R6 are each independently hydrogen, C1 to C6 alkyl, aryl, C1 to C3 alkyl-aryl, halogen, cyano, nitro, -NR7R8, -(CH2)mOR9, -SR9, -SO2R9, -SO2NR7R8, -NR7SO2R8, -NR7CO2R9, -NR7COR9, -CONR7R8, or -CO2R9; one of R2 and R3, R3 and R4, R4 and R5, or R5 and R6 may be taken together to form a five- to seven-membered alkyl ring, a six-membered aryl ring, a five- to seven-membered heteroalkyl ring having 1 heteroatom of N, O, or S, or a five- or six-membered heteroaryl ring having 1 or 2 heteroatoms of N, O, or S; R7 and R8 are each independently hydrogen, C1 to C6 alkyl, -(CH2)qR10, C1 to C3 alkyl-aryl, aryl, or may be taken together to form a four- to six-membered ring; R9 is hydrogen, C1 to C6 alkyl, C1 to C3 alkyl-aryl, aryl, or -(CH2)wR11; R10 and R11 are each independently -OH, -OR12, -CO2R12, -CONHR12, or cyano; R12 is hydrogen, C1 to C6 alkyl, aryl, or C1 to C6 alkyl-aryl; R13 is hydrogen, -OR14, or -NHCOR14; R14 is C1 to C6 alkyl, or C1 to C3 alkyl-aryl; n is 0, 1, or 2; m is 1, 2, or 3; q is 2, 3, or 4; w is 2, 3, or 4; the above aryl groups and the aryl moieties of the above alkyl-aryl groups are independently phenyl or substituted phenyl, wherein said substituted phenyl may be substituted with one to three of C1 to C4 alkyl, halogen, hydroxy, cyano, carboxamido, nitro, and C1 to C4 alkoxy; and a broken line represents an optional double bond, and the pharmaceutically acceptable salts thereof. These compounds are useful psychotherapeutics and are potent serotonin (5-HT1) agonists and may be used in the treatment of depression, anxiety, eating disorders, obesity, drug abuse, cluster headache, migraine, pain, chronic paroxysmal hemicrania and headache associated with vascular disorders, and other disorders arising from deficient serotonergic neurotransmission. The compounds can also be used as centrally acting antihypertensives and vasodilators.