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1. 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.

2. 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。

3. 发明授权

US4464374A Substituted guanidine derivatives, processes, pharmaceutical compositions and methods and intermediates 失效
标题翻译：取代的胍衍生物，方法，药物组合物和方法以及中间体
公开(公告)号：US4464374A
公开(公告)日：1984-08-07
申请号：US286064
申请日：1981-07-23
申请人： Tobias O. Yellin , David J. Gilman , Derrick F. Jones , Keith Oldham
发明人： Tobias O. Yellin , David J. Gilman , Derrick F. Jones , Keith Oldham
IPC分类号： A61K31/155 , A61K31/505 , A61P43/00 , C07C67/00 , C07C279/18 , C07C313/00 , C07C317/28 , C07C323/44 , C07D239/42 , C07D277/38 , C07D277/48 , A61K31/425
CPC分类号： C07D239/42 , C07D277/48
摘要： The invention relates to a guanidine derivative of the formula: ##STR1## in which W is a 2-6C alkylene chain optionally substituted by 1 or 2 1-4C alkyls; E is O, S, SO, SO.sub.2 or NR.sup.3 in which R.sup.3 is H or 1-6C alkyl; R.sup.1 is H or a straight chain 1-6C alkyl optionally substituted by 1 or 2 1-4C alkyls; or R.sup.1 and R.sup.3 are joined to form a morpholine, pyrrolidine, piperidine or piperazine ring; X, P, Y, Q and R.sup.2 are as defined in the specification, and the pharmaceutically-acceptable acid-addition salts thereof. Manufacturing process, pharmaceutical compositions and intermediates are also described. The compounds of the formula I are histamine H-2 antagonists.
摘要翻译：本发明涉及下式的胍衍生物：其中W是任选被1或2个1-4C烷基取代的2-6C亚烷基链; E是O，S，SO，SO2或NR3，其中R3是H或1-6C烷基; R1是H或任选被1或2个1-4C烷基取代的直链1-6C烷基; 或R 1和R 3连接形成吗啉，吡咯烷，哌啶或哌嗪环; X，P，Y，Q和R 2如说明书中所定义，及其药学上可接受的酸加成盐。还描述了制造方法，药物组合物和中间体。式I的化合物是组胺H-2拮抗剂。

4. 发明授权

US4696933A Guanidine compounds useful as histamine H2-antagonists 失效
标题翻译：用作组胺H2拮抗剂的胍化合物
公开(公告)号：US4696933A
公开(公告)日：1987-09-29
申请号：US701012
申请日：1985-02-12
申请人： Tobias O. Yellin , David J. Gilman
发明人： Tobias O. Yellin , David J. Gilman
IPC分类号： A61K31/41 , A61K31/415 , A61K31/425 , A61K31/426 , A61K31/44 , A61K31/505 , A61P1/04 , A61P43/00 , C07D213/70 , C07D213/73 , C07D213/75 , C07D213/76 , C07D231/38 , C07D239/42 , C07D239/46 , C07D239/47 , C07D241/40 , C07D249/04 , C07D249/14 , C07D277/20 , C07D277/48 , C07D401/12
CPC分类号： C07D213/76 , C07D239/42 , C07D239/47 , C07D241/40 , C07D249/04 , C07D277/48
摘要： The invention relates to amide derivatives which are histamine H-2 antagonists and which inhibit gastric acid secretion. According to the invention there is provided a guanidine derivative of the formula I: ##STR1## in which R.sup.1 is a hydrogen or 1-10C alkyl, 3-8C cycloalkyl, 4-14C cycloalkyl, 3-6C alkenyl, 3-6C alkynyl, 1-6C alkanoyl, 6-10C aryl, 7-11C aralkyl or 7-11C aroyl, the aryl, aralkyl and aroyl radical being optionally substituted; 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; and R.sup.2 and R.sup.3 are hydrogen 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.

5. 发明授权

US4665073A Haloalkylguanidine compounds, pharmaceutical compositions and methods processes and intermediates 失效
标题翻译：卤代烷基胍化合物，药物组合物和方法方法和中间体
公开(公告)号：US4665073A
公开(公告)日：1987-05-12
申请号：US589345
申请日：1984-03-14
申请人： Tobias O. Yellin , David J. Gilman
发明人： Tobias O. Yellin , David J. Gilman
IPC分类号： C07D213/76 , C07D231/40 , C07D239/42 , C07D239/46 , C07D241/20 , C07D249/04 , C07D249/06 , C07D249/10 , C07D249/14 , C07D251/16 , C07D277/48 , C07D239/47 , A61K31/44 , A61K31/505 , C07D213/70
CPC分类号： C07D213/76 , C07D231/40 , C07D239/42 , C07D239/47 , C07D241/20 , C07D249/04 , C07D249/06 , C07D249/14 , C07D251/16 , C07D277/48
摘要： The invention relates to guanidine derivatives which are histamine H-2 antagonists and which inhibit gastric acid secretion. According to the invention there 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 4-15C 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 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; 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; and R.sup.3 and R.sup.4 are hydrogen 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.

6. 发明授权

US4493840A Antisecretory guanidine derivatives, and pharmaceutical compositions containing them 失效
标题翻译：反分子胍衍生物和含有它们的药物组合物
公开(公告)号：US4493840A
公开(公告)日：1985-01-15
申请号：US314558
申请日：1981-10-26
申请人： Tobias O. Yellin , David J. Gilman
发明人： Tobias O. Yellin , David J. Gilman
IPC分类号： C07D277/20 , A61K31/425 , A61K31/426 , A61K31/44 , A61P1/00 , A61P1/04 , C07D233/88 , C07D263/48 , C07D271/06 , C07D271/07 , C07D277/40 , C07D277/48 , C07D285/08 , C07D417/12
CPC分类号： C07D271/07 , C07D233/88 , C07D263/48 , C07D277/48 , C07D285/08
摘要： This invention relates to quanidine derivatives which are histamine H-2 antagonists and which inhibit gastric acid secretion.The quanidine derivatives are of the formula:Het.sup.1 --(CH.sub.2).sub.m --Y.sup.1 --(CH.sub.2).sub.n --NR.sup.1 --A--NR.sup.2 --(CH.sub.2).sub.q --Y.sup.2 --(CH.sub.2).sub.p --Het.sup.2.

7. 发明授权

US4262126A Guanidine derivatives of imidazoles and thiazoles 失效
标题翻译：咪唑和噻唑的胍衍生物
公开(公告)号：US4262126A
公开(公告)日：1981-04-14
申请号：US65802
申请日：1979-08-13
申请人： David J. Gilman , James M. Wardleworth , Tobias O. Yellin
发明人： David J. Gilman , James M. Wardleworth , Tobias O. Yellin
IPC分类号： A61K31/415 , A61K31/425 , A61K31/426 , A61P1/04 , A61P43/00 , C07C277/08 , C07D209/48 , C07D233/88 , C07D277/20 , C07D277/38 , C07D277/42 , C07D277/48
CPC分类号： C07D209/48 , C07D233/88 , C07D277/48
摘要： The invention relates to guanidine derivatives of imidazoles and thiazoles which are histamine H-2 antagonists and which inhibit the secretion of gastric acid, to methods for their manufacture, to pharmaceutical compositions containing them and to methods of using such guanidine derivatives and compositions. The guanidine derivatives are of the general formula I: ##STR1## in which X is S or NH, Y is O, S, or SO, m is 1 to 4 and n is suitably 1 to 4, R.sup.1 is hydrogen, halogen or alkyl, R.sup.2 is hydrogen, alkyl, alkanoyl or aroyl, A is a 3,4-dioxocyclobuten-1,2-diyl radical or C.dbd.Z in which Z is O, S, NCN, NNO.sub.2, CHNO.sub.2, NCONH.sub.2, C(CN).sub.2, NCOR.sup.3, NCO.sub.2 R.sup.3, NSO.sub.2 R.sup.3 or NR.sup.4 in which R.sup.3 is alkyl or aryl and R.sup.4 is hydrogen or alkyl, B is alkoxy or alkylthio or NR.sup.5 R.sup.6 in which R.sup.5 and R.sup.6 are independently hydrogen, alkyl, alkenyl, cycloalkyl, hydroxyalkyl, alkoxyalkyl, alkylaminoalkyl or dialkylaminoalkyl; and the salts thereof.
摘要翻译：本发明涉及作为组胺H-2拮抗剂的咪唑和噻唑的胍衍生物，其抑制胃酸的分泌，其制备方法，含有它们的药物组合物以及使用这种胍衍生物和组合物的方法。胍衍生物具有通式I：其中X为S或NH，Y为O，S或SO，m为1至4，n为1至4，R 1为氢，卤素或烷基，R 2为氢，烷基，烷酰基或芳酰基，A为3,4-二氧环戊烯-1,2-二基或C = Z，其中Z为O，S，NCN，NNO2，CHNO2，NCONH2，C ）2，NCOR3，NCO2R3，NSO2R3或NR4，其中R3是烷基或芳基，R4是氢或烷基，B是烷氧基或烷硫基或NR5R6，其中R5和R6独立地是氢，烷基，烯基，环烷基，羟烷基，烷氧基烷基，烷基氨基烷基或二烷基氨基烷基; 及其盐。

8. 发明授权

US4496564A Amide derivatives 失效
标题翻译：酰胺衍生物
公开(公告)号：US4496564A
公开(公告)日：1985-01-29
申请号：US353423
申请日：1982-03-01
申请人： Tobias O. Yellin , David J. Gilman
发明人： Tobias O. Yellin , David J. Gilman
IPC分类号： A61K31/41 , A61K31/415 , A61K31/425 , A61K31/426 , A61K31/44 , A61K31/505 , A61P1/04 , A61P43/00 , C07D213/70 , C07D213/73 , C07D213/75 , C07D213/76 , C07D231/38 , C07D239/42 , C07D239/46 , C07D239/47 , C07D241/40 , C07D249/04 , C07D249/14 , C07D277/20 , C07D277/48 , C07D239/24
CPC分类号： C07D213/76 , C07D239/42 , C07D239/47 , C07D241/40 , C07D249/04 , C07D277/48
摘要： The invention relates to amide derivatives which are histamine H-2 antagonists and which inhibit gastric acid secretion. According to the invention there is provided a guanidine derivative of the formula I: ##STR1## in which R.sup.1 is a hydrogen or 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, the aryl, aralkyl and aroyl radical being optionally substituted; 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; and R.sup.2 and R.sup.3 are hydrogen 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拮抗剂并且抑制胃酸分泌的酰胺衍生物。根据本发明，提供了式I的胍衍生物：其中R1是氢或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，芳基，芳烷基和芳酰基任选被取代; 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; 和R2和R3是氢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。

9. 发明授权

US4447441A Haloalkylguanidine compounds, pharmaceutical compositions and methods, processes and intermediates 失效
标题翻译：卤代烷基胍化合物，药物组合物和方法，方法和中间体
公开(公告)号：US4447441A
公开(公告)日：1984-05-08
申请号：US353502
申请日：1982-03-01
申请人： Tobias O. Yellin , David J. Gilman
发明人： Tobias O. Yellin , David J. Gilman
IPC分类号： C07D213/76 , C07D231/40 , C07D239/42 , C07D239/46 , C07D241/20 , C07D249/04 , C07D249/06 , C07D249/10 , C07D249/14 , C07D251/16 , C07D277/48 , C07D231/38 , A61K31/41 , A61K31/415
CPC分类号： C07D213/76 , C07D231/40 , C07D239/42 , C07D239/47 , C07D241/20 , C07D249/04 , C07D249/06 , C07D249/14 , C07D251/16 , C07D277/48
摘要： The invention relates to guanidine derivatives which are histamine H-2 antagonists and which inhibit gastric acid secretion. According to the invention there 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 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; 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; and R.sup.3 and R.sup.4 are hydrogen 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：本发明涉及组胺H-2拮抗剂的胍衍生物，其抑制胃酸分泌。根据本发明，提供了式I的胍衍生物：其中R 1和R 2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R 5 -WW，其中W是2-6C亚烷基，其任选地被1或 2 1-4C烷基，E是O，S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，或者R5和R6连接到形成吡咯烷，哌啶，吗啉，哌嗪或N-甲基哌嗪环; 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; 和R3和R4是氢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。

10. 发明授权

US4347370A Guanidine derivatives of imidazoles and thiazoles 失效
标题翻译：咪唑和噻唑的胍衍生物
公开(公告)号：US4347370A
公开(公告)日：1982-08-31
申请号：US172302
申请日：1980-07-25
申请人： David J. Gilman , James M. Wardleworth , Tobias O. Yellin
发明人： David J. Gilman , James M. Wardleworth , Tobias O. Yellin
IPC分类号： A61K31/415 , A61K31/425 , A61K31/426 , A61P1/04 , A61P43/00 , C07C277/08 , C07D209/48 , C07D233/88 , C07D277/20 , C07D277/38 , C07D277/42 , C07D277/48 , C07D277/40 , C07D263/48
CPC分类号： C07D209/48 , C07D233/88 , C07D277/48
摘要： The invention relates to guanidine derivatives of imidazoles and thiazoles which are histamine H-2 antogonists and which inhibit the secretion of gastric acid, to methods for their manufacture, to pharmaceutical compositions containing them and to methods of using such guanidine derivatives and compositions. The guanidine derivatives are of the general formula I: ##STR1## in which X is S or NH, Y is O, S, or SO, m is 1 to 4 and n is suitably 1 to 4, R.sup.1 is hydrogen, halogen or alkyl, R.sup.2 is hydrogen, alkyl, alkanoyl or aroyl, A is a 3,4-dioxocyclobuten-1,2-diyl radical or C.dbd.Z in which Z is O, S, NCN, NNO.sub.2, CHNO.sub.2, NCONH.sub.2, C(CN).sub.2, NCOR.sup.3, NCO.sub.2 R.sup.3, NSO.sub.2 R.sup.3 or NR.sup.4 in which R.sup.3 is alkyl or aryl and R.sup.4 is hydrogen or alkyl, B is alkoxy or alkylthio or NR.sup.5 R.sup.6 in which R.sup.5 and R.sup.6 are independently hydrogen, alkyl, alkenyl, cycloalkyl, hydroxyalkyl, alkoxyalkyl, alkylaminoalkyl or dialkylaminoalkyl; and the salts thereof.
摘要翻译：本发明涉及咪唑和噻唑的胍衍生物，它们是组胺H-2绝育学家，并且其抑制胃酸的分泌，其制备方法，含有它们的药物组合物以及使用这种胍衍生物和组合物的方法。胍衍生物具有通式I：其中X为S或NH，Y为O，S或SO，m为1至4，n为1至4，R 1为氢，卤素或烷基，R 2为氢，烷基，烷酰基或芳酰基，A为3,4-二氧环戊烯-1,2-二基或C = Z，其中Z为O，S，NCN，NNO2，CHNO2，NCONH2，C ）2，NCOR3，NCO2R3，NSO2R3或NR4，其中R3是烷基或芳基，R4是氢或烷基，B是烷氧基或烷硫基或NR5R6，其中R5和R6独立地是氢，烷基，烯基，环烷基，羟烷基，烷氧基烷基，烷基氨基烷基或二烷基氨基烷基; 及其盐。

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