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1. 发明授权

US4746672A Oxides of 1,2,5-thiadiazoles, their use in pharmaceutical compositions 失效
标题翻译： 1,2,5-噻二唑的氧化物，它们在药物组合物中的用途
公开(公告)号：US4746672A
公开(公告)日：1988-05-24
申请号：US376395
申请日：1982-05-10
申请人： Tobias O. Yellin , Philip N. Edwards , Michael S. Large
发明人： Tobias O. Yellin , Philip N. Edwards , Michael S. Large
IPC分类号： A61K31/425 , A61P1/04 , A61P43/00 , C07D417/12 , A61K31/41
CPC分类号： C07D417/12
摘要： Sulphur derivatives which are histamine H-2 antagonists and which inhibit gastric acid secretion of the formula I: ##STR1## in which R.sup.1 and R.sup.2 independently are hydrogen or 1-10C alkyl, 3-8C cycloalkyl or 4-14C cycloalkylalkyl, each alkyl, cycloalkyl or cycloalkylalkyl optionally carrying one or more F, Cl or Br atoms, provided that one of R.sup.1 and R.sup.2 is halogen substituted; ring X is a heterocyclic ring as defined in the specification; A is phenylene or 5-7C cycloalkylene or a 1-8C alkylene chain into which is optionally inserted one or two groups; p is 1 or 2; R.sup.3 is a variety of radicals described in the specification; and the pharmaceutically-acceptable acid-addition salts thereof. Manufacturing processes for the derivatives, intermediates and pharmaceutical compositions are also part of the invention.
摘要翻译：作为组胺H-2拮抗剂的硫衍生物，其抑制式I的胃酸分泌：其中R1和R2独立地为氢或1-10C烷基，3-8C环烷基或4-14C环烷基烷基，每个烷基任选地携带一个或多个F，Cl或Br原子的环烷基或环烷基烷基，条件是R 1和R 2中的一个是卤素取代的; 环X是说明书中定义的杂环; A是亚苯基或5-7C亚环烷基或1-8C亚烷基链，其中任选地插入一个或两个基团; p为1或2; R3是说明书中描述的各种基团; 及其药学上可接受的酸加成盐。衍生物，中间体和药物组合物的制备方法也是本发明的一部分。

2. 发明授权

US4657908A Carbonyl derivatives 失效
标题翻译：羰基衍生物
公开(公告)号：US4657908A
公开(公告)日：1987-04-14
申请号：US700959
申请日：1985-02-12
申请人： Tobias O. Yellin , David J. Gilman , Philip N. Edwards , Michael S. Large , Derrick F. Jones , Keith Oldham
发明人： Tobias O. Yellin , David J. Gilman , Philip N. Edwards , Michael S. Large , Derrick F. Jones , Keith Oldham
IPC分类号： C07D239/42 , C07D239/46 , C07D249/04 , C07D249/10 , C07D251/16 , C07D277/48 , A61K31/53 , A61K31/44 , A61K31/445 , A61K31/455 , A61K31/47 , A61K31/495 , A61K31/505 , C07D215/18 , C07D215/28 , C07D217/22 , C07D241/16 , C07D241/20 , C07D251/40 , C07D401/12
CPC分类号： C07D239/42 , C07D239/47 , C07D249/04 , C07D251/16 , C07D277/48
摘要： The invention relates to carbonyl derivatives which are histamine H-2 antagonists and which inhibit gastric acid secretion. According to the invention where is provided a guanidine derivative of the formula I: ##STR1## in which R.sup.1 and R.sup.2, same or different, are hydrogen or 1-10C alkyl, 3-8C cycloalkyl or 4-14C cycloalkylalkyl, each alkyl, cycloalkyl or cycloalkylalkyl optionally carrying one or more F, Cl or Br atoms, provided that one of R.sup.1 and R.sup.2 is halogen substituted, or R.sup.2 is hydrogen and R.sup.1 is R.sup.5 -E-W in which W is 2-6C alkylene optionally substituted by 1 or 2 1-4C alkyls, E is O, S, SO, SO.sub.2 or NR.sup.6 in which R.sup.6 is H or 1-6C alkyl, R.sup.5 is H or 1-6C alkyl optionally substituted by 1 or 2 1-4C alkyls, or R.sup.5 and R.sup.6 are joined to form a pyrrolidine, piperidine, morpholine, piperazine or N-methylpiperazine ring, or R.sup.2 is H and R.sup.1 is H, 1-10C alkyl, 3-8C cycloalkyl, 4-14C cycloalkylalkyl, 3-6C alkenyl, 3-6C alkynyl, 1-6C alkanoyl, 6-10C aryl, 7-11C aralkyl or 7-11C aroyl; ring X is a heterocyclic ring as defined in the specification; A is phenylene or 5-7C cycloalkylene, or a 1-8C alkylene into which is optionally inserted one or two groups; D is O or S; R.sup.4 is H or 1-6C alkyl; R.sup.3 is H or a variety of radicals described in the specification: and the pharmaceutically-acceptable acid-addition salts thereof. Manufacturing processes and pharmaceutical compositions are also described.

3. 发明授权

US4362728A Haloguanidine compounds, pharmaceutical compositions and methods of use 失效
标题翻译：卤代胍化合物，药物组合物和使用方法
公开(公告)号：US4362728A
公开(公告)日：1982-12-07
申请号：US206005
申请日：1980-11-12
申请人： Tobias O. Yellin , Philip N. Edwards , Michael S. Large
发明人： Tobias O. Yellin , Philip N. Edwards , Michael S. Large
IPC分类号： C07D251/16 , C07C279/18 , C07C323/44 , C07C335/28 , C07D209/48 , C07D213/74 , C07D213/75 , C07D231/38 , C07D231/40 , C07D239/42 , C07D239/46 , C07D239/47 , C07D239/48 , C07D241/20 , C07D251/18 , C07D277/20 , C07D277/42 , C07D277/48 , C07D285/08 , C07D403/12 , C07D417/12 , G09F13/04 , C07D239/24 , A61K31/495 , A61K31/505
CPC分类号： C07D209/48 , C07C323/44 , C07C335/28 , C07D213/75 , C07D231/40 , C07D239/42 , C07D239/47 , C07D239/48 , C07D241/20 , C07D251/18 , C07D277/48 , C07D285/08
摘要： Compounds useful for inhibiting gastric acid secretion and for the treatment of peptic ulcers caused or exacerbated by gastric acidity having the following formula (I): ##STR1## in which R.sup.1 and R.sup.2, are H, C.sub.1-10 alkyl, C.sub.3-8 cycloalkyl or cycloalkylalkyl in which the alkyl part is C.sub.1-6 and the cycloalkyl part is C.sub.3-8, each of the alkyl, cycloalkyl and cycloalkylalkyls being optionally substituted by one or more halogens selected from F, Cl and Br, provided that at least one of R.sup.1 and R.sup.2 is a halogen substituted alkyl, cycloalkyl or cycloalkylalkyl and provided that there is no halogen substituent on the carbon directly attached to the nitrogen; and X, m, Y, n and R.sup.3 are as described in the specification; and the pharmaceutically-acceptable acid-addition salts thereof. Processes for producing compounds of formula (I), pharmaceutical compositions containing them, methods of utilizing such compositions and intermediates useful for synthesizing compounds of formula (I) are also described.
摘要翻译：可用于抑制胃酸分泌和治疗由胃酸引起或加重的具有下式（I）的消化性溃疡的化合物：其中R 1和R 2为H，C 1-10烷基，C 3-8环烷基或烷基部分为C 1-6且环烷基部分为C 3-8的环烷基烷基，烷基，环烷基和环烷基烷基中的每一个任选被一个或多个选自F，Cl和Br的卤素取代，条件是至少一个 R1和R2是卤素取代的烷基，环烷基或环烷基烷基，条件是在直接与氮连接的碳上不存在卤素取代基; X，m，Y，n和R3如说明书所述; 及其药学上可接受的酸加成盐。还描述了制备式（I）化合物，含有它们的药物组合物，利用这些组合物的方法和用于合成式（I）化合物的中间体的方法。

4. 发明授权

US4762932A Haloguanidine intermediates 失效
标题翻译：卤代中间体
公开(公告)号：US4762932A
公开(公告)日：1988-08-09
申请号：US869615
申请日：1986-06-02
申请人： Tobias O. Yellin , Philip N. Edwards , Michael S. Large
发明人： Tobias O. Yellin , Philip N. Edwards , Michael S. Large
IPC分类号： C07D251/16 , C07C279/18 , C07C323/44 , C07C335/28 , C07D209/48 , C07D213/74 , C07D213/75 , C07D231/38 , C07D231/40 , C07D239/42 , C07D239/46 , C07D239/47 , C07D239/48 , C07D241/20 , C07D251/18 , C07D277/20 , C07D277/42 , C07D277/48 , C07D285/08 , C07D403/12 , C07D417/12 , G09F13/04 , C07D277/04
CPC分类号： C07D209/48 , C07C323/44 , C07C335/28 , C07D213/75 , C07D231/40 , C07D239/42 , C07D239/47 , C07D239/48 , C07D241/20 , C07D251/18 , C07D277/48 , C07D285/08
摘要： Compounds useful for inhibiting gastric acid secretion and for the treatment of peptic ulcers caused or exacerbated by gastric acidity having the following formula (I): ##STR1## in which R.sup.1 and R.sup.2, are H, C.sub.1-10 alkyl, C.sub.3-8 cycloalkyl or cycloalkylalkyl in which the alkyl part is C.sub.1-6 and the cycloalkyl part is C.sub.3-8, each of the alkyl, cycloalkyl and cycloalkylalkyls being optionally substituted by one or more halogens selected from F, Cl and Br, provided that at least one of R.sup.1 and R.sup.2 is a halogen substituted alkyl, cycloalkyl or cycloalkylalkyl and provided that there is no halogen substituent on the carbon directly attached to the nitrogen; and X, m, Y, n and R.sup.3 are as described in the specification; and the pharmaceutically-acceptable acid-addition salts thereof. Processes for producing compounds of formula (I), pharmaceutical compositions containing them, methods of utilizing such compositions and intermediates useful for synthesizing compounds of formula (I) are also described.
摘要翻译：本发明涉及下式的胍：其中R 1和R 2为H，C 1-10烷基，C 3-8环烷基或环烷基烷基，其中烷基部分为C 1-6 并且环烷基部分为C3-8，烷基，环烷基和环烷基烷基中的每一个任选被一个或多个选自F，Cl和Br的卤素取代，条件是R 1和R 2中的至少一个为卤素取代的烷基，环烷基或环烷基 - 烷基，条件是在直接与氮连接的碳上不存在卤素取代基;环X是携带1或2个任选的取代基或含有1或2个任选取代基的5-或6-元杂环芳环的苯基，选自O，N和S的2或3个杂原子，该杂环可以携带选自F，Cl，Br，I，C 1-6烷基，C 1-6烷氧基，C 1-6烷硫基，三氟甲基，羟基和氨基; ... Y是O，S，直接键，亚甲基，亚乙烯基，SO或NR 4，其中R 4是H或C 1-6烷基; m是0-4， n为1至5，条件是当Y为O，SO或NR 4时，n为2至5; R 3具有各种含义; ...及其药学上可接受的酸加成盐。还描述了制造方法和药物组合物。

5. 发明授权

US4604465A Haloguanidine intermediates 失效
公开(公告)号：US4604465A
公开(公告)日：1986-08-05
申请号：US420863
申请日：1982-09-21
申请人： Tobias O. Yellin , Philip N. Edwards , Michael S. Large
发明人： Tobias O. Yellin , Philip N. Edwards , Michael S. Large
IPC分类号： C07D251/16 , C07C279/18 , C07C323/44 , C07C335/28 , C07D209/48 , C07D213/74 , C07D213/75 , C07D231/38 , C07D231/40 , C07D239/42 , C07D239/46 , C07D239/47 , C07D239/48 , C07D241/20 , C07D251/18 , C07D277/20 , C07D277/42 , C07D277/48 , C07D285/08 , C07D403/12 , C07D417/12 , G09F13/04 , A61K31/505
CPC分类号： C07D209/48 , C07C323/44 , C07C335/28 , C07D213/75 , C07D231/40 , C07D239/42 , C07D239/47 , C07D239/48 , C07D241/20 , C07D251/18 , C07D277/48 , C07D285/08
摘要： Compounds useful for inhibiting gastric acid secretion and for the treatment of peptic ulcers caused or exacerbated by gastric acidity having the following formula (I): ##STR1## in which R.sup.1 and R.sup.2, are H, C.sub.1-10 alkyl, C.sub.3-8 cycloalkyl or cycloalkylalkyl in which the alkyl part is C.sub.1-6 and the cycloalkyl part is C.sub.3-8, each of the alkyl, cycloalkyl and cycloalkylalkyls being optionally substituted by one or more halogens selected from F, Cl and Br, provided that at least one of R.sup.1 and R.sup.2 is a halogen substituted alkyl, cycloalkyl or cycloalkylalkyl and provided that there is no halogen substituent on the carbon directly attached to the nitrogen; and X, m, Y, n and R.sup.3 are as described in the specification; and the pharmaceutically-acceptable acid-addition salts thereof. Processes for producing compounds of formula (I), pharmaceutical compositions containing them, methods of utilizing such compositions and intermediates useful for synthesizing compounds of formula (I) are also described.

6. 发明授权

US4496571A Histamine H2-antagonists 失效
标题翻译：组胺H2拮抗剂
公开(公告)号：US4496571A
公开(公告)日：1985-01-29
申请号：US353422
申请日：1982-03-01
申请人： Tobias O. Yellin , David J. Gilman , Philip N. Edwards , Michael S. Large , Derrick F. Jones , Keith Oldham
发明人： Tobias O. Yellin , David J. Gilman , Philip N. Edwards , Michael S. Large , Derrick F. Jones , Keith Oldham
IPC分类号： C07D239/42 , C07D239/46 , C07D249/04 , C07D249/10 , C07D251/16 , C07D277/48 , C07D401/12
CPC分类号： C07D239/42 , C07D239/47 , C07D249/04 , C07D251/16 , C07D277/48
摘要： The invention relates to carbonyl derivatives which are histamine H-2 antagonists and which inhibit gastric acid secretion. According to the invention where is provided a guanidine derivative of the formula I: ##STR1## in which R.sup.1 and R.sup.2, same or different, are hydrogen or 1-10C alkyl, 3-8C cycloalkyl or 4-14C cycloalkylalkyl, each alkyl, cycloalkyl or cycloalkylalkyl optionally carrying one or more F, Cl or Br atoms, provided that one of R.sup.1 and R.sup.2 is halogen substituted, or R.sup.2 is hydrogen and R.sup.1 is R.sup.5 -E-W in which W is 2-6C alkylene optionally substituted by 1 or 2 1-4C alkyls, E is O, S, SO, SO.sub.2 or NR.sup.6 in which R.sup.6 is H or 1-6C alkyl, R.sup.5 is H or 1-6C alkyl optionally substituted by 1 or 2 1-4C alkyls, or R.sup.5 and R.sup.6 are joined to form a pyrrolidine, piperidine, morpholine, piperazine or N-methylpiperazine ring, or R.sup.2 is H and R.sup.1 is H, 1-10C alkyl, 3-8C cycloalkyl, 4-14C cycloalkylalkyl, 3-6C alkenyl, 3-6C alkynyl, 1-6C alkanoyl, 6-10C aryl, 7-11C aralkyl or 7-11C aroyl; ring X is a heterocyclic ring as defined in the specification; A is phenylene or 5-7C cycloalkylene, or a 1-8C alkylene into which is optionally inserted one or two groups; D is O or S; R.sup.4 is H or 1-6C alkyl; R.sup.3 is H or a variety of radicals described in the specification: and the pharmaceutically-acceptable acid-addition salts thereof. Manufacturing processes and pharmaceutical compositions are also described.
摘要翻译：本发明涉及作为组胺H-2拮抗剂并抑制胃酸分泌的羰基衍生物。根据本发明，其中提供了式I的胍衍生物：其中R1和R2相同或不同，为氢或1-10C烷基，3-8C环烷基或4-14C环烷基烷基，每个烷基，任选地携带一个或多个F，Cl或Br原子的环烷基或环烷基烷基，条件是R 1和R 2中的一个是卤素取代的，或R 2是氢，R 1是其中W是任选被1或2取代的2-6C亚烷基的R 5-EW 1-4C烷基，E是O，S，SO，SO2或NR6，其中R6是H或1-6C烷基，R5是H或任选被1或2个1-4C烷基取代的1-6C烷基，或R5和R6 连接形成吡咯烷，哌啶，吗啉，哌嗪或N-甲基哌嗪环，或R 2为H，R 1为H，1-10C烷基，3-8C环烷基，4-14C环烷基烷基，3-6C烯基，3-6C 炔基，1-6C烷酰基，6-10C芳基，7-11C芳烷基或7-11C芳酰基; 环X是说明书中定义的杂环; A是亚苯基或5-7C亚环烷基，或其中任选插入一个或两个基团的1-8C亚烷基; D为O或S; R4是H或1-6C烷基; R3是H或本说明书中描述的各种基团及其药学上可接受的酸加成盐。还描述了制造方法和药物组合物。

7. 发明授权

US5334614A Hydroxylamine derivatives 失效
标题翻译：羟胺衍生物
公开(公告)号：US5334614A
公开(公告)日：1994-08-02
申请号：US59313
申请日：1993-05-11
申请人： Philip N. Edwards , Michael S. Large
发明人： Philip N. Edwards , Michael S. Large
IPC分类号： A61K31/135 , A61K31/27 , A61K31/275 , A61K31/35 , A61K31/496 , A61K31/505 , A61P37/08 , A61P43/00 , C07C239/20 , C07D213/63 , C07D263/36 , C07D277/22 , C07D307/42 , C07D309/10 , C07D405/12 , C07D417/04 , A61K31/34 , C07D307/20
CPC分类号： C07D405/12 , C07D309/10
摘要： The invention concerns hydroxylamine derivatives of the formula I ##STR1## wherein R.sup.4 is hydrogen, carbamoyl, (1-4C)alkyl, cyclopentyl, cyclohexyl, tetrahydrofuran-3-yl, tetrahydropyran-4-yl, piperidin-4-yl, N-(1-4C)alkylpiperidin-4-yl, (2-5C)alkanoyl, (1-4C)alkylsulphonyl, N-(1-4C)alkylcarbamoyl, N,N-di-(1-4C)alkylcarbamoyl, phenyl, phenyl-(1-4C)alkyl, di-phenyl-(1-4C)alkyl, benzoyl, phenylsulphonyl or a heteroarylmethyl group;R.sup.5 is hydrogen, (1-4C)alkyl, (3-4C)alkenyl, (3-4C)alkynyl, cyano-(1-4C)alkyl, phenyl or phenyl-(1-4C)alkyl;A.sup.4 is (1-4C)alkylene;Ar.sup.1 is phenylene, pyridinediyl or pyrimidinediyl;A.sup.1 is a direct link to X.sup.1, or A.sup.1 is (1-4C)alkylene;X.sup.1 is oxy, thio, sulphinyl or sulphonyl;Ar.sup.2 is phenylene, pyridinediyl, pyrimidinediyl, thiophenediyl, furandiyl or thiazolediyl;R.sup.1 is hydrogen, (1-4C)alkyl, (3-4C)alkenyl or (3-4C)alkynyl; andR.sup.2 and R.sup.3 together form a group of the formula -A.sup.2 -X.sup.2 -A.sup.3 -wherein each of A.sup.2 and A.sup.3 is independently (1-3C)alkylene and X.sup.2 is oxy, thio, sulphinyl, sulphonyl or imino;or a pharmaceutically-acceptable salt thereof; processes for their manufacture; pharmaceutical compositions containing them and their use as 5-lipoxygenase inhibitors.
摘要翻译：本发明涉及式I的羟胺衍生物，其中R 4是氢，氨基甲酰基，（1-4C）烷基，环戊基，环己基，四氢呋喃-3-基，四氢吡喃-4-基，哌啶-4-基，N （1-4C）烷基哌啶-4-基，（2-5C）烷酰基，（1-4C）烷基磺酰基，N-（1-4C）烷基氨基甲酰基，N，N-二（1-4C）烷基氨基甲酰基，苯基，苯基 - （1-4C）烷基，二 - 苯基 - （1-4C）烷基，苯甲酰基，苯基磺酰基或杂芳基甲基; R5是氢，（1-4C）烷基，（3-4C）烯基，（3-4C）炔基，氰基 - （1-4C）烷基，苯基或苯基 - （1-4C）烷基; A4是（1-4C）亚烷基; Ar1是亚苯基，吡啶二基或嘧啶二基; A1是直接连接到X1，或A1是（1-4C）亚烷基; X1是氧基，硫基，亚磺酰基或磺酰基; Ar 2是亚苯基，吡啶二基，嘧啶二基，噻吩二基，呋喃二基或噻唑二基; R1为氢，（1-4C）烷基，（3-4C）烯基或（3-4C）炔基; 并且R2和R3一起形成式-A2-X2-A3-的基团，其中A2和A3各自独立地为（1-3C）亚烷基，X2为氧基，硫基，亚磺酰基，磺酰基或亚氨基; 或其药学上可接受的盐; 制造过程; 含有它们的药物组合物及其作为5-脂肪氧合酶抑制剂的用途。

8. 发明授权

US5420298A Pyrrolidine derivatives 失效
标题翻译：吡咯烷衍生物
公开(公告)号：US5420298A
公开(公告)日：1995-05-30
申请号：US114187
申请日：1993-09-01
申请人： Philip N. Edwards , Michael S. Large
发明人： Philip N. Edwards , Michael S. Large
IPC分类号： A61K31/40 , A61K31/4025 , A61K31/425 , A61K31/47 , A61P29/00 , A61P37/08 , A61P43/00 , C07D207/12 , C07D401/12 , C07D409/04 , C07D409/12 , C07D409/14 , C07D417/04 , C07D417/14 , C07D471/04 , C07D491/052 , C07D207/06 , C07D207/14
CPC分类号： C07D401/12 , C07D207/12 , C07D409/12
摘要： The invention concerns pyrrolidine derivatives of the formula ##STR1## wherein Ar.sup.1 is optionally-substituted phenyl, naphthyl or a 10-membered bicyclic heterocyclic moiety containing one or two nitrogen heteroatoms and optionally containing a further heteroatom selected from nitrogen, oxygen and sulphur;A is a direct link to the group X or A is (1-4C)alkylene;X is oxy, thio, sulphinyl or sulphonyl;Ar.sup.2 is phenylene, pyridinediyl, pyrimidinediyl, thiophendiyl, furandiyl or thiazolediyl;R.sup.1 is (1-4C)alkyl, (3-4C)alkenyl or (3-4C)alkynyl;R.sup.2 is (1-4C)alkyl, (2-4C)alkenyl, (2-4C)alkynyl, halogeno-(1-4C)alkyl, halogeno-(2-4C)alkenyl, halogeno-(2-4C)alkynyl, (1-4C)alkoxy-(2-4C)alkyl, hydroxy-(2-4C)alkyl, cyano-(1-4C)alkyl, carboxy-(1-4C)alkyl, carbamoyl-(1-4C)alkyl, (1-4C)alkoxycarbonyl-(1-4C)alkyl, N-(1-4C)alkylcarbamoyl-(1-4C)alkyl or N,N-di-(1-4C)alkylcarbamoyl-(1-4C)alkyl; andn is 1 or 2 and each R.sup.3 is independently hydrogen, hydroxy, (1-4C)alkyl or (1-4C)alkoxy;or a pharmaceutically-acceptable salt thereof;processes for their manufacture; pharmaceutical compositions containing them and their use as 5-lipoxygenase inhibitors.
摘要翻译：本发明涉及式Ia的吡咯烷衍生物，其中Ar1是任选取代的苯基，萘基或含有一个或两个氮杂原子并且任选地含有另外选自氮，氧和硫的杂原子的10元双环杂环部分; A是直接连接到基团X或A是（1-4C）亚烷基; X是氧基，硫基，亚磺酰基或磺酰基; Ar 2是亚苯基，吡啶二基，嘧啶二基，噻吩二基，呋喃二基或噻唑二基; R1是（1-4C）烷基，（3-4C）烯基或（3-4C）炔基; R2是（1-4C）烷基，（2-4C）烯基，（2-4C）炔基，卤代 - （1-4C）烷基，卤代 - （2-4C）烯基，卤代 - （2-4C）（1-4C）烷基，（2-4C）烷基，氰基 - （1-4C）烷基，羧基 - （1-4C）烷基，氨基甲酰基 - （1-4C）（1-4C）烷氧基羰基 - （1-4C）烷基，N-（1-4C）烷基氨基甲酰基 - （1-4C）烷基或N，N-二（1-4C）烷基氨基甲酰基 - （1-4C）烷基; 并且n为1或2，并且每个R 3独立地为氢，羟基，（1-4C）烷基或（1-4C）烷氧基; 或其药学上可接受的盐; 制造过程; 含有它们的药物组合物及其作为5-脂肪氧合酶抑制剂的用途。

9. 再颁专利

USRE36617E (Substituted aralkyl) heterocyclic compounds 失效
公开(公告)号：USRE36617E
公开(公告)日：2000-03-14
申请号：US627311
申请日：1996-04-03
申请人： Philip N. Edwards , Michael S. Large
发明人： Philip N. Edwards , Michael S. Large
IPC分类号： A61K31/395 , A61K31/40 , A61K31/41 , A61K31/415 , A61K31/44 , A61K31/4406 , A61K31/4418 , A61K31/445 , A61K31/505 , A61K31/535 , A61K31/5375 , A61P3/00 , A61P13/02 , A61P15/00 , A61P35/00 , C07D213/46 , C07D213/57 , C07D233/60 , C07D233/61 , C07D233/64 , C07D233/90 , C07D239/26 , C07D249/08 , C07D295/18 , C07D521/00
CPC分类号： C07D239/26 , C07D213/57 , C07D231/12 , C07D233/56 , C07D233/90 , C07D249/08
摘要： A (substituted-aralkyl)heterocyclic compound of the formula I ##STR1## wherein R.sup.1 is an azido, carbamoyl, cyano, formyl, hydroxy or nitro radical, a 1-6C 1-hydroxyalkyl, alkoxy, alkylcarbamoyl, alkylthio, alkylsulphinyl or alkylsulphonyl radical, a 2-cyanoethyl radical, optionally bearing one to four 1-6C alkyl substituents, or a 2-6C alkanoyl, halogenoalkanoyl, alkanoyloxy, alkanoylamino, dialkylcarbamoyl or alkoxycarbonyl radical; R.sup.2 and R.sup.3, which may be the same or different, are each a hydrogen atom, a 1-6C alkyl, dueterioalkyl or halogenoalkyl radical, or a phenyl or phenyl(1-6C alkyl) radical, in each of which the phenyl may optionally bear one or more substituents; or R.sup.2 and R.sup.3, together with the carbon atom to which they are attached, may form a 3- to 6-membered ring; or R.sup.1 R.sup.2 R.sup.3 C- is a 1,1-dicyanoethyl or trifluoromethylsulphonyl radical; R.sup.4 is a hydrogen or halogen atom, a cyano or nitro radical or a 1-6C alkyl or halogenoalkyl radical; R.sup.5 has any of the values defined above for the group R.sup.1 R.sup.2 R.sup.3 C but is not necessarily the same as R.sup.1 R.sup.2 R.sup.3 C, or has any of the values defined above for R.sup.4 but is not necesarily the same as R.sup.4, or is a carbamoyl, 1-pyrrolidinyl-carbonyl, piperidinocarbonyl, morpholinocarbonyl or nitro radical, a 1-6C alkoxy or halogenoalkoxy radical or a 2-6C alkanoyl or alkoxy-carbonyl radical; A is a methylene or ethylene radical optionally bearing one or more substituents selected from deuterium and halogen atoms, carbamoyl, cyano and hydroxy radicals, 1-6C alkyl and alkoxy radicals, and 2-6C alkanoyloxy radicals provided that when A is linked to R.sup.6 through a nitrogen atom thereof, it may not bear a hydroxy, alkoxy or alkanoyloxy substituent on the carbon atom adjacent to such nitrogen atoms; and R.sup.6 is a 1H-1,2,4-triazol-1-yl, 4H-1,2,4-triazol-4-yl, 1H-imidazol-1-yl, 5-cyano-1H-imidazol-1-yl, 3-pyridyl or 5-pyrimidinyl radical, or a 1H-imidazol-1-yl radical, bearing at the 5-position thereof a 1-6C alkyl substituent which is itself optionally substituted by one or more carbamoyl, cyano, hydroxy or 2-6C alkoxycarbonyl radicals; and provided that when R.sup.2, R.sup.3, R.sup.4 and R.sup.5 are hydrogen, A is a methylene radical and R.sup.6 is a 3-pyridyl radical, R.sup.1 is not a cyano, hydroxy or hydroxymethyl radical, and when R.sup.1 is a hydroxy radical, R.sup.3, R.sup.4 and R.sup.5 are hydrogen, A is a methylene radical and R.sup.6 is 3-pyridyl, R.sup.2 is not a methyl or a 2-chloro-1-methylethyl radical, and provided that when R.sup.1 is a methoxycarbonyl radical, R.sup.2, R.sup.3, R.sup.4 and R.sup.5 are hydrogen and A is a methylene radical, R.sub.1 is not a 1H-imidazol-1-yl radical; and the pharmaceutically acceptable acid addition salts thereof.

10. 发明授权

US4935437A (Substituted aralkyl) heterocyclic compounds 失效
标题翻译：（取代的芳烷基）杂环化合物
公开(公告)号：US4935437A
公开(公告)日：1990-06-19
申请号：US204743
申请日：1988-06-10
申请人： Philip N. Edwards , Michael S. Large
发明人： Philip N. Edwards , Michael S. Large
IPC分类号： A61K31/395 , A61K31/40 , A61K31/41 , A61K31/415 , A61K31/44 , A61K31/4406 , A61K31/4418 , A61K31/445 , A61K31/505 , A61K31/535 , A61K31/5375 , A61P3/00 , A61P13/02 , A61P15/00 , A61P35/00 , C07D213/46 , C07D213/57 , C07D233/60 , C07D233/61 , C07D233/64 , C07D233/90 , C07D239/26 , C07D249/08 , C07D295/18 , C07D521/00
CPC分类号： C07D239/26 , C07D213/57 , C07D231/12 , C07D233/56 , C07D233/90 , C07D249/08
摘要： A (substituted-aralkyl)heterocyclic compound of the formula I ##STR1## wherein R.sup.1 is an azido, carbamoyl, cyano, formyl, hydroxy or nitro radical, a 1-6C 1-hydroxyalkyl, alkoxy, alkylcarbamoyl, alkylthio, alkylsulphinyl or alkylsulphonyl radical, a 2-cyanoethyl radical, optionally bearing one to four 1-6C alkyl substituents, or a 2-6C alkanoyl, halogenoalkanoyl, alkanoyloxy, alkanoylamino, dialkylcarbamoyl or alkoxycarbonyl radical; R.sup.2 and R.sup.3, which may be the same or different, are each a hydrogen atom, a 1-6C alkyl, dueterioalkyl or halogenoalkyl radical, or a phenyl or phenyl(1-6C alkyl) radical, in each of which the phenyl may optionally bear one or more substituents; or R.sup.2 and R.sup.3, together with the carbon atom to which they are attached, may form a 3- to 6-membered ring; or R.sup.1 R.sup.2 R.sup.3 C- is a 1,1-dicyanoethyl or trifluoromethylsulphonyl radical; R.sup.4 is a hydrogen or halogen atom, a cyano or nitro radical or a 1-6C alkyl or halogenoalkyl radical; R.sup.5 has any of the values defined above for the group R.sup.1 R.sup.2 R.sup.3 C but is not necessarily the same as R.sup.1 R.sup.2 R.sup.3 C, or has any of the values defined above for R.sup.4 but is not necesarily the same as R.sup.4, or is a carbamoyl, 1-pyrrolidinyl-carbonyl, piperidinocarbonyl, morpholinocarbonyl or nitro radical, a 1-6C alkoxy or halogenoalkoxy radical or a 2-6C alkanoyl or alkoxy-carbonyl radical; A is a methylene or ethylene radical optionally bearing one or more substituents selected from deuterium and halogen atoms, carbamoyl, cyano and hydroxy radicals, 1-6C alkyl and alkoxy radicals, and 2-6C alkanoyloxy radicals provided that when A is linked to R.sup.6 through a nitrogen atom thereof, it may not bear a hydroxy, alkoxy or alkanoyloxy substituent on the carbon atom adjacent to such nitrogen atoms; and R.sup.6 is a 1H-1,2,4-triazol-1-yl, 4H-1,2,4-triazol-4-yl, 1H-imidazol-1-yl, 5-cyano-1H-imidazol-1-yl, 3-pyridyl or 5-pyrimidinyl radical, or a 1H-imidazol-1-yl radical, bearing at the 5-position thereof a 1-6C alkyl substituent which is itself optionally substituted by one or more carbamoyl, cyano, hydroxy or 2-6C alkoxycarbonyl radicals; and provided that when R.sup.2, R.sup.3, R.sup.4 and R.sup.5 are hydrogen, A is a methylene radical and R.sup.6 is a 3-pyridyl radical, R.sup.1 is not a cyano, hydroxy or hydroxymethyl radical, and when R.sup.1 is a hydroxy radical, R.sup.3, R.sup.4 and R.sup.5 are hydrogen, A is a methylene radical and R.sup.6 is 3-pyridyl, R.sup.2 is not a methyl or a 2-chloro-1-methylethyl radical, and provided that when R.sup.1 is a methoxycarbonyl radical, R.sup.2, R.sup.3, R.sup.4 and R.sup.5 are hydrogen and A is a methylene radical, R.sub.1 is not a 1H-imidazol-1-yl radical; and the pharmaceutically acceptable acid addition salts thereof.

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