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1. 发明申请

WO1995006636A1 5-ARYLINDOLE DERIVATIVES 审中-公开
公开(公告)号：WO1995006636A1
公开(公告)日：1995-03-09
申请号：PCT/IB1994000195
申请日：1994-07-04
申请人： PFIZER INC. , MACOR, John, E.
发明人： PFIZER INC.
IPC分类号： C07D209/04
CPC分类号： C07D401/14 , C07D403/04 , C07D403/14 , C07F7/2208
摘要： Compounds of formula (I), wherein A, B, D, E, and F are each independently nitrogen or carbon; R1 is hydrogen, C1 to C6 alkyl, -(CH2)nR7, or C1 to C3 alkyl-aryl; R2, R3, R4, R5, and R6 are each independently hydrogen, C1 to C6 alkyl, aryl, C1 to C3 alkyl-aryl, halogen, cyano, nitro, -(CH2)mNR8R9, -(CH2)mOR9, -SR9, -SO2NR8R9, -(CH2)mNR8SO2R9, -(CH2)mNR8CO2R9, -(CH2)mNR8COR9, -(CH2)mCONR7R9, or -(CH2)mCO2R9; R2 and R3, R3 and R4, R4 and R5, and R5 and R6 may be taken together to form a 5- to 7-membered alkyl ring, a 6-membered aryl ring, a 5- to 7-membered heteroalkyl ring, having 1 heteroatom of N, O, or S, or a 5- to 6-membered heteroaryl ring having 1 or 2 heteroatoms of N, O, or S; R7 is -OR10, -SR10, -SO2NR10R11, -NR10SO2R11, -NR10CO2R11, -NR10COR11, -CONR10R11, or -CO2R10; R8, R9, R10 and R11 are each independently hydrogen, C1 to C6 alkyl, or C1 to C3 alkyl-aryl; m is 0, 1, or 2; n is 2, 3, or 4; and the above aryl groups and the aryl moieties of the above alkyl-aryl groups are each independently phenyl or substituted phenyl, wherein said substituted phenyl may be substituted with 1 to 3 of C1 to C4 alkyl, halogen, hydroxy, cyano, carboxamido, nitro, or C1 to C4 alkoxy, and the pharmaceutically acceptable salts thereof. These compounds are useful in treating migraine and other disorders and are new. 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 hermicrania 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：式（I）的化合物，其中A，B，D，E和F各自独立地为氮或碳; R1是氢，C1-C6烷基， - （CH2）nR7或C1-C3烷基 - 芳基; R 2，R 3，R 4，R 5和R 6各自独立地为氢，C 1至C 6烷基，芳基，C 1至C 3烷基 - 芳基，卤素，氰基，硝基， - （CH 2）m NR 8 R 9， - （CH 2）mOR 9，（CH2）mNR8CO2R9， - （CH2）mNR8COR9， - （CH2）mCONR7R9或 - （CH2）mCO2R9; - （CH2）mNR8R9， - （CH2）mNR8SO2R9， - R 2和R 3，R 3和R 4，R 4和R 5以及R 5和R 6可以一起形成5-至7-元烷基环，6-元芳基环，5-至7-元杂烷基环，其具有 1个N，O或S的杂原子，或具有1或2个N，O或S杂原子的5-至6-元杂芳基环; R7是-OR10，-SR10，-SO2NR10R11，-NR10SO2R11，-NR10CO2R11，-NR10COR11，-CONR10R11或-CO2R10; R 8，R 9，R 10和R 11各自独立地为氢，C 1至C 6烷基或C 1至C 3烷基 - 芳基; m为0,1或2; n为2,3或4; 上述芳基和上述烷基 - 芳基的芳基部分各自独立地为苯基或取代的苯基，其中所述取代的苯基可以被1至3个C 1 -C 4烷基，卤素，羟基，氰基，甲酰氨基，硝基或C 1〜C 4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，并且是新的。这些化合物是有用的精神治疗药物，并且是有效的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，疼痛和慢性阵发性乳头瘤和头痛相关血管疾病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。

2. 发明申请

WO1993020073A1 INDOLE DERIVATIVES AS 5-HT1 AGONISTS 审中-公开
标题翻译：单独使用衍生物作为5-HT1激动剂
公开(公告)号：WO1993020073A1
公开(公告)日：1993-10-14
申请号：PCT/US1993001967
申请日：1993-03-10
申请人： PFIZER INC. , MACOR, John, E. , WYTHES, Martin, J.
发明人： PFIZER INC.
IPC分类号： C07D413/14
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.
摘要翻译：其中W为（i），（ii），（iii），（iv），（v），（vi）或（vii）的式（I） n为0,1或2; m为0,1,2或3; Y和G各自独立地为氧或硫; Z是-O - ， - S - ， - NH-或-CH 2; R1是氢，C1至C8烷基，被一个羟基取代的C1至C8烷基，C3至C8烯基，C3至C8炔基，芳基，C1至C3烷基芳基，C1至C3烷基杂芳基或-Q-R4; R2和R3各自独立地为氢，C1至C6烷基，芳基，C1至C3烷基芳基或C1至C3烷基杂芳基; R 4是氰基，三氟甲基，-COR 9，-CO 2 R 9，-CONR 9 R 10，-OR 9，-SO 2 NR 9 R 10或-S（O）q R 9; R 9和R 10各自独立地为氢，C 1至C 8烷基，C 1至C 3烷基芳基，芳基或R 9和R 10可以一起取代形成三至七元烷基环或三至七元杂烷基环， 1个O的杂原子; Q为C1至C3烷基; R 11是氢，-OR 12或-NHCOR 12; R 12是氢，C 1至C 6烷基，芳基或C 1至C 3烷基芳基; q是0,1或2; 第一手性碳由星号表示; 第二个手性碳由＃指定; 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，其中所述取代的苯基可以被一至三个选自C 1 -C 4烷基，卤素，羟基，氰基，甲酰胺基，硝基和C1至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，其他疾病是新的。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头痛相关血管疾病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。

3. 发明申请

WO1994021619A1 NAPHTHALENE DERIVATIVES 审中-公开
标题翻译：萘衍生物
公开(公告)号：WO1994021619A1
公开(公告)日：1994-09-29
申请号：PCT/US1994001206
申请日：1994-02-15
申请人： PFIZER INC. , CHENARD, Bertrand, L. , MACOR, John, E. , SEGELSTEIN, Barbara, E.
发明人： PFIZER INC.
IPC分类号： C07D295/135
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R 1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-R4，R4-（CH2）bO（C = O） - （CH2）c-， - （CH2）bO（C = O） - （CH2）c-R4，-NH（C = X） R4，R4-O（C = O）O-，-O（C = O）NH-R4，R4-O（C = O）NH-， - （CH2）b-（C = O） - （CH2） C-R 4，-NH-S（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，所述取代部分由式-R4，-R4R5，-O-R4或-S（O）d-R4部分取代; R3是氢，C1-C6烷基，C1-C6烷基芳基或芳基; R 4和R 5各自独立地为（ⅩⅤ），（ⅩⅥ），（ⅩⅦ），氢，-CF3，C1-C6烷基，C1-C6烷基芳基，条件是当R 2为-OR 4或-OR 4时，或C 1至C 6烷基。这些化合物是有用的精神治疗药物，并且是有效的5-羟色胺（5-HT1）激动剂和拮抗剂，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红素和头痛相关伴有血管疾病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。

4. 发明申请

WO1993018032A1 INDOLE DERIVATIVES AS 5-HT1 AGONISTS 审中-公开
标题翻译：单独使用衍生物作为5-HT1激动剂
公开(公告)号：WO1993018032A1
公开(公告)日：1993-09-16
申请号：PCT/US1993001667
申请日：1993-03-03
申请人： PFIZER INC. , MACOR, John, E. , NOWAKOWSKI, Jolanta, T.
发明人： PFIZER INC.
IPC分类号： C07D417/14
CPC分类号： C07D413/14 , C07D417/14
摘要： Compounds of formula (I) where A represents a direct bond, C1-C4 alkyl, or C1-C4 alkenyl; n is 0, 1, or 2; R1 is hydrogen, C1-C6 alkyl, aryl, C1-C3 alkylaryl, C1-C3 alkylheteroaryl, or -(CH2)mR6; W, X, Y, and Z are each independently oxygen, sulfur, nitrogen or carbon, provided that at least one of W, X, Y or Z is nitrogen; R2, R3, R4, and R5 are each independently hydrogen, C1-C6 alkyl, aryl, C1-C3 alkylaryl, C1-C3 alkylheteroaryl, halogen, cyano, trifluoromethyl, nitro, -OR7, -NR7R8, -(CH2)sOR7, -SR7, -SO2NR7R8, -NR7SO2R8, -NR7CO2R8, -CONR7R8, or -CO2R7; one of R2 and R3, R3 and R4, or R4 and R5 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- to six-membered heteroaryl ring having 1 or 2 heteroatoms of N, O, or S; R6 is cyano, trifluoromethyl, or -OR9; R7, R8, and R9 are each independently hydrogen, C1 to C6 alkyl, -(CH2)mR10, C1 to C3 alkylaryl, or aryl; R7 and R8 may be taken together to form a C4-C7 alkyl ring; R10 is cyano, trifluoromethyl, or C1-C4 alkoxy; R11 is hydrogen, -OR12, or -NHCOR12; R12 is C1 to C6 alkyl, aryl, or C1 to C3 alkyl-aryl; m is 1, 2, or 3; s is 0, 1, 2, or 3; and the above aryl groups and the aryl moieties of the above alkylaryl 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 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; R 1是氢，C 1 -C 6烷基，芳基，C 1 -C 3烷基芳基，C 1 -C 3烷基杂芳基或 - （CH 2）m R 6; 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; R2，R3，R4和R5各自独立地为氢，C1-C6烷基，芳基，C1-C3烷基芳基，C1-C3烷基杂芳基，卤素，氰基，三氟甲基，硝基，-OR7，-NR7R8， - （CH2） -SR 7，-SO 2 NR 7 R 8，-NR 7 SO 2 R 8，-NR 7 CO 2 R 8，-CONR 7 R 8或-CO 2 R 7; R 2和R 3之一，R 3和R 4或R 4和R 5可以一起形成五元至七元烷基环，六元芳环，五元至七元杂烷基环， N，O或S，或具有1或2个N，O或S杂原子的5至6元杂芳基环; R6是氰基，三氟甲基或-OR9; R 7，R 8和R 9各自独立地为氢，C 1至C 6烷基， - （CH 2）m R 10，C 1至C 3烷基芳基或芳基; R 7和R 8可以一起形成C 4 -C 7烷基环; R 10是氰基，三氟甲基或C 1 -C 4烷氧基; R 11是氢，-OR 12或-NHCOR 12; R 12是C 1至C 6烷基，芳基或C 1至C 3烷基 - 芳基; m为1,2或3; s为0,1,2或3; 上述芳基和芳基部分独立地选自苯基和取代的苯基，其中所述取代的苯基可以被一至三个选自C 1 -C 4烷基，卤素，羟基，氰基，甲酰氨基，硝基和C1〜C4烷氧基，及其药学上可接受的盐。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，疼痛和慢性阵发性血尿素和与血管相关的头痛疾病，以及其它由缺乏血清素能神经传递引起的疾病。该化合物也可用作中枢作用的抗高血压药和血管扩张剂。

5. 发明申请

WO1995021836A1 5-HETEROARYLINDOLE DERIVATIVES AS BENZODIAZEPINE RECEPTOR SITE AGONISTS AND ANTAGONISTS 审中-公开
标题翻译：作为苯二氮卓类受体位点激动剂和拮抗剂的5-异构体衍生物
公开(公告)号：WO1995021836A1
公开(公告)日：1995-08-17
申请号：PCT/IB1994000407
申请日：1994-12-08
申请人： PFIZER INC. , MACOR, John, E.
发明人： PFIZER INC.
IPC分类号： C07D403/04
CPC分类号： C07D403/04 , C07D471/04
摘要： The present invention relates to compounds of formula (I). The present invention also relates to intermediates for the preparation of compounds of formula (I), pharmaceutical compositions and method of use.
摘要翻译：本发明涉及式（I）化合物。本发明还涉及制备式（I）化合物，药物组合物和使用方法的中间体。

6. 发明申请

WO1996000720A1 ARYL AND HETEROARYL ALKOXYNAPHTHALENE DERIVATIVES 审中-公开
标题翻译： ARYL和HETEROARYL ALKOXYNPHTHALENE DERIVATIVES
公开(公告)号：WO1996000720A1
公开(公告)日：1996-01-11
申请号：PCT/IB1995000381
申请日：1995-05-18
申请人： PFIZER INC. , CHENARD, Bertrand, L. , DESAI, Kishor, A. , HOWARD, Harry, R., Jr. , MACOR, John, E. , SHENK, Kevin, D.
发明人： PFIZER INC.
IPC分类号： C07C271/06
CPC分类号： C07D213/30 , C07D209/34 , C07D213/64 , C07D213/85 , C07D215/14 , C07D237/14 , C07D239/34 , C07D239/42 , C07D257/04 , C07D263/56 , C07D271/06 , C07D271/107 , C07D277/24 , C07D277/64 , C07D295/155 , C07D333/28 , C07D401/12 , C07D413/12 , C07D417/12
摘要： Compounds of formula (I) wherein R , R , R , R , R , R and R are defined as in the specification. These compounds are useful psychotherapeutics and are potent serotonin (5-HT1) agonists and antagonists.
摘要翻译：其中R 1，R 2，R 4，R 23，R 24，R 25和R 26的式（I）化合物如说明书中所定义。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）激动剂和拮抗剂。

7. 发明申请

WO1993021180A1 ACYLAMINOINDOLE DERIVATIVES AS 5-HT1 AGONISTS 审中-公开
公开(公告)号：WO1993021180A1
公开(公告)日：1993-10-28
申请号：PCT/US1993001807
申请日：1993-03-04
申请人： PFIZER INC. , MACOR, John, E.
发明人： PFIZER INC.
IPC分类号： C07D403/06
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为0或1; Y和W各自为氨基酸残基; R 1是氢，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; R 7为氢，C 1至C 6烷基，芳基或C 1至C 3烷基 - 芳基; p为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，其中所述取代的苯基可以被一至三个选自C 1 -C 4烷基，卤素，羟基，氰基，甲酰胺，硝基和C1至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头痛相关血管疾病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。

8. 发明公开

EP1373231A1 3-HETEROCYCLYLPROPANOHYDROXAMIC ACID PCP INHIBITORS 有权
标题翻译： 3-杂环PROPANOHYDROXAMSÄURE衍生物作为抑制剂PCP
公开(公告)号：EP1373231A1
公开(公告)日：2004-01-02
申请号：EP02707045.7
申请日：2002-03-18
申请人： Pfizer Limited , PFIZER INC.
发明人： FISH, Paul Vincent , KENDALL, Jackie Diane , WHITLOCK, Gavin Alistair , PFIZER INC.
IPC分类号： C07D271/06 , A61K31/4245 , C07D413/12 , A61P17/02
CPC分类号： C07D263/34 , C07D271/06 , C07D271/07 , C07D413/12
摘要： Compounds of formula (I): (I), and their salts, solvates, prodrugs, etc., wherein the substituents have the values mentioned herein, are Procollagen C-Proteinase (PCP) inhibitors and have utility in conditions mediated by PCP.

9. 发明授权

EP1373231B1 3-HETEROCYCLYL-PROPANO-HYDROXAMIC ACID AS PCP INHIBITORS 有权
标题翻译： 3-杂环PROPANOHYDROXAMSÄURE衍生物作为抑制剂PCP
公开(公告)号：EP1373231B1
公开(公告)日：2005-06-08
申请号：EP02707045.7
申请日：2002-03-18
申请人： Pfizer Limited , PFIZER INC.
发明人： FISH, Paul Vincent , KENDALL, Jackie Diane , WHITLOCK, Gavin Alistair , PFIZER INC.
IPC分类号： C07D271/06 , A61K31/4245 , C07D413/12 , A61P17/02
CPC分类号： C07D263/34 , C07D271/06 , C07D271/07 , C07D413/12
摘要： Compounds of formula (I): (I), and their salts, solvates, prodrugs, etc., wherein the substituents have the values mentioned herein, are Procollagen C-Proteinase (PCP) inhibitors and have utility in conditions mediated by PCP.

10. 发明申请

WO1998030209A1 RAPIDLY RELEASING AND TASTE-MASKING PHARMACEUTICAL DOSAGE FORM 审中-公开
标题翻译：快速释放和吸收药物药物剂型
公开(公告)号：WO1998030209A1
公开(公告)日：1998-07-16
申请号：PCT/IB1997001471
申请日：1997-11-20
申请人： PFIZER PHARMACEUTICALS INC. , PFIZER INC. , ITOH, Akinori , NIWA, Toshiyuki
发明人： PFIZER PHARMACEUTICALS INC. , PFIZER INC.
IPC分类号： A61K09/54
CPC分类号： A61K9/5078 , A61K9/1623 , A61K9/1652 , A61K9/5015 , A61K9/5026 , A61K9/5073
摘要： The present invention provides a rapidly releasing and taste-masking pharmaceutical dosage form comprising a core containing a pharmaceutically active ingredient, low-substituted hydroxypropyl cellulose and microcrystalline cellulose, the amount of the microcrystalline cellulose being at least 26.0 weight percent based on the total weight of the core; an inner coating layer formed on the core and containing a water-soluble polymer; and an outer coating layer formed on the inner coating layer and containing a saliva-insoluble polymer. A process for preparing such oral dosage form is also disclosed.
摘要翻译：本发明提供了一种快速释放和掩味的药物剂型，其包含含有药物活性成分，低取代羟丙基纤维素和微晶纤维素的核心，微晶纤维素的量基于总重量的至少26.0重量％核心; 形成在芯上并含有水溶性聚合物的内涂层; 以及形成在内涂层上并含有唾液不溶性聚合物的外涂层。还公开了制备这种口服剂型的方法。

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