-
1.发明授权Guanidino-substituted heterocyclic derivatives having histamine H-2 antagonist activity 失效具有组胺H-2拮抗剂活性的胍基取代的杂环衍生物
公开(公告)号：EP0059597B1
公开(公告)日：1986-04-23
申请号：EP82300946.9
申请日：1982-02-24
发明人： Yellin, Tobias Oregon , Gilman, David John , Edwards, Philip Neil , Large, Michael Stewart , Jones, Derrick Fleet , Oldham, Keith
IPC分类号： C07D239/42 , C07D239/46 , C07D251/16 , C07D277/48 , C07D249/04 , C07D417/12 , C07D405/12 , C07D401/12 , C07D403/12 , A61K31/425
CPC分类号： C07D239/42 , C07D239/47 , C07D249/04 , C07D251/16 , C07D277/48
-
2.发明授权Guanidine derivatives, processes for their manufacture and pharmaceutical compositions containing them 失效胍基衍生物，其制备方法及含有它们的药物组合物
公开(公告)号：EP0030092B1
公开(公告)日：1985-02-06
申请号：EP80304023.7
申请日：1980-11-11
IPC分类号： C07D277/48 , C07D213/75 , C07D231/40 , C07D239/42 , C07D239/47 , C07D239/48 , C07D241/20 , C07D251/18 , C07D285/08 , C07D403/12 , C07D417/12
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
-
3.发明公开Heterocyclic guanidines as histamine H-2 antagonists 失效Heterozyklische Guanidinderivate als Histamin-H-2-Antagonisten。
公开(公告)号：EP0065823A1
公开(公告)日：1982-12-01
申请号：EP82302141.5
申请日：1982-04-26
IPC分类号： C07D417/12 , A61K31/395
CPC分类号： C07D417/12
摘要： This invention relates to sulphur 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:-
in which R 1 and R 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 1 and R 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 3 is 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拮抗剂的硫衍生物，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，环烷基或环烷基烷基，任选地带有一个或多个F，Cl或Br原子，条件是R 1和R 2之一是卤素取代的; 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; R 3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。 还描述了制造方法和药物组合物。
-
4.发明公开Guanidino-substituted heterocyclic derivatives having histamine H-2 antagonist activity 失效胍类取代基杂环衍生物组蛋白-H-2拮抗剂Wirkung。
公开(公告)号：EP0059597A2
公开(公告)日：1982-09-08
申请号：EP82300946.9
申请日：1982-02-24
发明人： Yellin, Tobias Oregon , Gilman, David John , Edwards, Philip Neil , Large, Michael Stewart , Jones, Derrick Fleet , Oldham, Keith
IPC分类号： C07D239/42 , C07D239/46 , C07D251/16 , C07D277/48 , C07D249/04 , C07D417/12 , C07D405/12 , C07D401/12 , C07D403/12 , A61K31/425
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:-
in which R' and R 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 1 and R 2 is halogen substituted, or R 2 is hydrogen and R 1 is R 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 2 or NR 6 in which R 6 is H or 1-6C alkyl, R 5 is H or 1-6C alkyl optionally substituted by 1 or 2 1-4C alkyls, or R 5 and R 6 are joined to form a pyrrolidine, piperidine, morpholine, piperazine or N-methylpiperazine ring, or R 2 is H and R 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 4 is H or 1-6C alkyl; R 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，或者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。
-
5.发明公开Guanidine derivatives, processes for their manufacture and pharmaceutical compositions containing them 失效胍衍生物，其制备方法和含有它们的药物组合物。
公开(公告)号：EP0030092A1
公开(公告)日：1981-06-10
申请号：EP80304023.7
申请日：1980-11-11
IPC分类号： C07D277/48 , C07D213/75 , C07D231/40 , C07D239/42 , C07D239/47 , C07D239/48 , C07D241/20 , C07D251/18 , C07D285/08 , C07D403/12 , C07D417/12
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： The invention relates to a guanidine of the formula:-
in which R 1 and R 2 are H, Ci-io alkyl, C 3-8 cycloalkyl or cycloalkylalkyl in which the alkyl part is C 1-6 and the cycloalkyl part is C 3-8 , each of the alkyl, cycloalkyl and cycloalkylal- kyls being optionally substituted by one or more halogens selected from F, Cl and Br, provided that at least one of R' and R' is a halogen substituted alkyl, cycloalkyl or cycloalkyl-alkyl and provided that there is no halogen substituent on the carbon directly attached to the nitrogen;
ring X is phenyl carrying 1 or 2 optional substitutents or a 5- or 6-membered heterocyclic aromatic ring containing 1, 2 or 3 hetero atoms selected from 0, N and S, which heterocyclic ring may, carry a single optional substituent selected from F, Cl, Br, I, C 1-6 alkyl, C 1-6 alkoxy, C 1-6 alkylthio, trifluoromethyl, hydroxy and amino;
Y is 0, S, a direct bond, methylene, vinylene, SO or NR 4 in which R 4 is H or C 1-6 alkyl;
m is 0 to 4 and n is 1 to 5, provided that when Y is 0, SO or NR 4 , n is 2 to 5;
R 3 has various significances; and the pharmaceutically-acceptable acid-addition salts thereof.
Manufacturing processes and pharmaceutical compositions are also described.摘要翻译： 本发明涉及下式的胍： - ...
...其中R <2>为H <1>和R，C 1-10烷基，C 3-8环烷基或环烷基烷基，其中烷基部分是C 1-6 和环烷基部分是C 3-8，每一个烷基，环烷基和环烷基烷基通过选自F，Cl和Br中的一种或多种卤素任选substituiertem的，提供并 - [R <1>和R的<2>的至少一个是一个 卤素取代的烷基，环烷基或环烷基 - 烷基和提供thatthere是上连接到氮直接的碳上没有卤素取代基; ...环X是苯基携带1个或2个取代基任选的或5-或6元杂芳环含有1 ，2或3个杂原子选自O，N和S，选择该杂环可以，携带选自F，Cl，溴，我所选择的单一的任选取代基，C1-6烷基，C1-6烷氧基，C1-6烷硫基，三氟甲基 ，羟基和氨基; ... Y是O，S，直接键合，亚甲基，亚乙烯基，SO或NR <4>中R <4>是H或C 1-6烷基; ...... m是0至4和 n为1至5，只要没当Y是O，SO或NR <4>中，n为2至5; ... [R <3>具有多种意义; ...和药学上可接受的酸加成盐。 所以... 制造工艺和药物组合物进行说明。 -
公开(公告)号：EP0163416B1
公开(公告)日：1989-05-31
申请号：EP85302881.9
申请日：1985-04-24
发明人： Bowler, Jean , Glen, Alasdair Thomas , Crawley, Graham Charles , Large, Michael Stewart , Edwards, Philip Neil , Tait, Brian Steele
IPC分类号： C07C103/34 , C07C147/14 , C07C147/02 , C07C149/18 , C07C149/20 , C07C149/26 , C07C149/273 , A61K31/16 , A61K31/215 , A61K31/10
CPC分类号： C07C323/16 , C07C45/46 , C07C45/515 , C07C45/68 , C07C49/755 , C07C49/757 , C07C65/40 , C07C317/18 , C07C2602/10 , C07F7/1856 , C07F9/5031
-
7.发明公开Guanidinoheterocyclic derivatives as histamine H-2 antagonists 失效拮抗剂Guanidinoheterocyclische衍生物作为组胺H-2。
公开(公告)号：EP0061318A2
公开(公告)日：1982-09-29
申请号：EP82301420.4
申请日：1982-03-19
IPC分类号： C07D239/46 , C07D239/42 , C07D239/48 , C07D213/76 , C07D231/40 , C07D249/04 , C07D249/06 , C07D249/14 , C07D241/20 , C07D277/48 , A61K31/395
CPC分类号： C07D213/76 , C07D231/40 , C07D239/42 , C07D239/47 , C07D239/48 , C07D241/20 , C07D249/04 , C07D249/06 , C07D249/14 , C07D277/48
摘要： This invention relates to alcohol 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:-
in which R 1 and R 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 1 and R 2 is halogen-substituted, or R 2 is hydrogen and R 1 is R S- E-W- in which W is 2-6C alkylene optionally substituted by 1 or 2 1-4C alkyl, E is 0, S, SO, S0 2 or NR 6 in which R 6 is H or 1-6C alkyl, R 5 is H or 1-6C alkyl optionally substituted by 1 or 2 1-4C alkyls, or R 5 and R 6 are joined to form a pyrrolidine, piperidine, morpholine, piperazine or N-methylpiperazine ring, or R 2 is hydrogen and R 1 is 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, arylalkyl and aroyl radicals 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 oxygen or sulphur; R 3 , R 4 and R 5 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.-
公开(公告)号：EP0316097A1
公开(公告)日：1989-05-17
申请号：EP88310183.4
申请日：1988-10-28
IPC分类号： C07D405/06 , A61K31/41 , A61K31/505 , A61K31/44 , A61K31/415 , A61K31/34
CPC分类号： C07D231/12 , C07D233/56 , C07D249/08 , C07D405/06
摘要： Naphtho[2,1-b]furan derivatives of the formula:-
wherein
R¹ is a 1 H -1,2,4-triazol-1-yl, 4 H -1,2,4-triazol-4-yl, 3-pyridyl or 5-pyrimidinyl radical or a 1 H -imidazol-1-yl radical optionally substituted in the 5-position by a 1-6C alkyl or halogenoalkyl radical;
R² and R³, which may be the same or different, are each a hydrogen or deuterium atom, a cyano radical, a 1-6C alkyl or halogenoalkyl radical, a phenyl radical optionally substituted by halogen, or one of R² and R³ is a radical of the formula R¹ as defined above, and the other is hydrogen;
R⁴ and R⁵, which may be the same or different, are each a 1-2C alkyl, deuterioalkyl or halogenoalkyl radical;
or R⁴ and R⁵ together with the carbon atom to which they are attached form a 3-6C cycloalkyl radical;
R⁶ and R⁷, which may be the same or different, are each a hydrogen or halogen atom, an amino, carboxy, carbamoyl, cyano, 1-cyano-1-methylethyl or nitro radical, a 1-6C alkyl or halogenoalkyl radical, a mono- or di-(1-6C)alkylcarbamoyl radical, a mono- or di-(1-6C)halogenoalkylcarbamoyl radical, a group of the formula -COR⁸, -SO n R⁸ or -OR⁸, in which n is 0, 1 or 2 and R⁸ is a 1-6C alkyl or halogenoalkyl radical, or a benzoyl radical optionally substituted by halogen;
one of R⁹ and R¹⁰ is hydrogen and the other is a hydroxy or 1-6C alkoxy radical, or R⁹ and R¹⁰ together form an oxo radical; and the pharmaceutically acceptable acid addition salts thereof;
processes for their manufacture; and pharmaceutical compositions containing them.摘要翻译： 萘酚[2,1-b]呋喃衍生物，其分子式为： -
其中R 1为1H-1,2,4-三唑-1-基，4H-1,2,4-三唑-4 环丙基，3-吡啶基或5-嘧啶基或在5-位被1-6C烷基或卤代烷基任意取代的1H-咪唑-1-基; R 2和R 3可以相同或不同，分别为氢或氘原子，氰基，1-6C烷基或卤代烷基，任选被卤素取代的苯基或其中之一 R 2和R 3是如上定义的式R 1的基团，另一个是氢; R 4和R 5可以相同或不同，分别为1-2C烷基，氘代烷基或卤代烷基; 或R 4和R 5与它们所连接的碳原子一起形成3-6C环烷基; R 6和R 7可以相同或不同，分别为氢或卤素原子，氨基，羧基，氨基甲酰基，氰基，1-氰基-1-甲基乙基或硝基，1-6C 烷基或卤代烷基，一或二 - （1-6C）烷基氨基甲酰基，一或二 - （1-6C）卤代烷基氨基甲酰基，式-COR 8，-SO n R 8或 -OR 8，其中n为0,1或2，R 8为1-6C烷基或卤代烷基，或任选被卤素取代的苯甲酰基; R 9和R 10之一是氢，另一个是羟基或1-6C烷氧基，或R 9和R 1一起形成氧代基; 及其药学上可接受的酸加成盐; 制造过程; 和含有它们的药物组合物。 -
公开(公告)号：EP0163416A2
公开(公告)日：1985-12-04
申请号：EP85302881.9
申请日：1985-04-24
发明人： Bowler, Jean , Glen, Alasdair Thomas , Crawley, Graham Charles , Large, Michael Stewart , Edwards, Philip Neil , Tait, Brian Steele
IPC分类号： C07C103/34 , C07C147/14 , C07C147/02 , C07C149/18 , C07C149/20 , C07C149/26 , C07C149/273 , A61K31/16 , A61K31/215 , A61K31/10
CPC分类号： C07C323/16 , C07C45/46 , C07C45/515 , C07C45/68 , C07C49/755 , C07C49/757 , C07C65/40 , C07C317/18 , C07C2602/10 , C07F7/1856 , C07F9/5031
摘要： A phenol derivative of the formula
wherein NU is a defined phenolic nucleus including a phenyl-hydroxynaphthyl; hydroxyphenyl-naphthyl; phenyl- hydroxyindanyl, phenyl-hydroxybenzothienyl or mono- hydroxyphenyl-ethylene or vinylene nucleus; wherein A is alkylene, alkenylene or alkynylene which may be interrupted by phenylene or other linkages, wherein R' is hydrogen, or alkyl, alkenyl, alkynyl, cycloalkyl, halogenoalkyl, alkozyalkyl, halogenoalkoxyalkyl, aryl or arylalkyl, or R' is joined to R 2 , and wherein X is -CONR 2 -, CSNR 2 -, -NR 12 CO-, -NR 12 CS-, -NR 12 CONR 2 -,
-SO 2 NR 2 - or -CO-, or, when R 1 is not hydrogen, is-NR 12 COO-,-(PO)R 2 -, -S-, -SO- or -S0 2 -, wherein R 2 is hydrogen or alkyl, or R 1 and R 2 together form alkylene; wherein R' 2 is hydrogen or alkyl, and wherein R 22 is hydrogen, cyano or nitro, or a salt thereof when appropriate. The compounds possess antioestrogenic activity and may be used for the treatment of hormone-dependent breast tumours or of anovulatory infertility.摘要翻译： 式NU-A-X-R1的酚衍生物，其中NU是包括苯基 - 羟基萘基的定义的酚核; 羟萘; 苯基 - 羟基茚满基，苯基 - 羟基苯并噻吩基或单羟基苯基 - 乙烯或亚乙烯基核; 其中A是可被亚苯基或其它键连接的亚烷基，亚烯基或亚炔基，其中R 1是氢或烷基，烯基，炔基，环烷基，卤代烷基，烷氧基烷基，卤代烷氧基烷基，芳基或芳基烷基，或R 1与R 2连接， 其中X是-CONR 2 + 13，-CSNR 2 - ， - NR 12 CO - ， - NR 12 CS - ， - NR 12 CONR 2 - ， - SO 2 NR 2 - 或-CO-，或者当R 1不是氢时，是-NR 12 COO-， - （ PO）R213，-S-，-SO-或-SO2-，其中R2是氢或烷基，或R1和R2一起形成亚烷基; 其中R 12是氢或烷基，并且其中R 22是氢，氰基或硝基; 或其盐。 该化合物具有抗雌激素活性，可用于治疗激素依赖性乳腺肿瘤或无排卵性不育症。
-
公开(公告)号：EP0126567A1
公开(公告)日：1984-11-28
申请号：EP84302927.3
申请日：1984-05-01
IPC分类号： C07C129/16 , C07D295/20 , A01N47/44 , A61K7/22
CPC分类号： C07D295/215 , A01N47/44 , C07C279/265
摘要： A bis(1-substituted biguanide) derivative of the formula:
or a tautomeric form thereof, wherein R 1 , R 2 and R 9 , which may be the same or different, are each hydrogen, a 1-16C alkyl radical, a 3-16C cycloalkyl radical, a (3-12C cycloalkyl)-1--(1-4C alkyl) radical, an optionally substituted phenyl or naphthyl radical, an optionally substituted phenyl(1-4C)alkyl or naphthyl(1-4C)alkyl radical or an optionally substituted diphenylmethyl radical, provided that at least one of R 1 , R 2 and R 9 is other than hydrogen; R 3 , R 4 , R 7 and R 8 , which may be the same or different are each hydrogen, or an alkyl, cycloalkyl, (cycloalkyl)alkyl, phenyl, naphthyl, phenylalkyl, naphthylalkyl, or diphenylmethyl radical as defined above, or a 2-16 alkoxyalkyl radical, or R 3 , R 4 and the nitrogen atom to which they are attached, or R 7 and R 8 and the nitrogen atom to which they are attached, which may be the same or different, are each a 1-azetidinyl, 1-pyrrolidinyl, piperidino, hexamethyleneimino, heptamethyleneimino, morpholino or 4-(1-8C alkanoyl)-1--piperazinyl radical, each of which may bear 1-3C alkyl substituents; R 5 and R 6 , which may be the same or different, are each hydrogen or a 1-8C alkyl radical; and X is a 2-16C linking group which is a straight chain alkylene radical, or a straight chain alkylene radical bearing one or more 1-16C alkyl substituents, of which any pair or pairs which are attached to different carbon atoms, may be joined so as to form, together with the intervening carbon atom or atoms of the alkylene radical, a (5-7C)-cycloalkyl radical or radicals; and the acid addition salts thereof, processes for their manufacture, and antibacterial and antifungal compositions and methods using said compounds.摘要翻译： 衍生化学式为：R 3 R 4 NC（NR 5）NHC（：NHC（NR 9））NR 1 -X -NR 2 C（（NR 9））-NHC（NR 6 6）-NR 7 R 8 V或其互变异构形式，其中R 1，R 2 和R 9可以相同或不同，分别为氢，1-16C烷基，3-16C环烷基，（3-12C环烷基）-1-（1-4C烷基）基团 ，任选取代的苯基或萘基，任选取代的苯基（1-4C）烷基或萘基（1-4C）烷基或任选取代的二苯基甲基，条件是R 1，R 2， R 9不是氢; R 3，R 4，R 7和R 8可以相同或不同，各自为氢或烷基，环烷基，（环烷基） 烷基，苯基，萘基，苯基烷基，萘基烷基或二苯基甲基，或2-16个烷氧基烷基或R 3，R 4及其连接的氮原子，或R 7， 和R 8和它们所连接的氮原子 各自为1-氮杂环丁烷基，1-吡咯烷基，哌啶子基，六亚甲基亚氨基，七亚甲基亚氨基，吗啉代或4-（1-8C烷酰基）-1-哌嗪基，其各自可以具有1-3C烷基取代基; R 5和R 6可以相同或不同，分别为氢或1-8C烷基; X是直链亚烷基的2-16C连接基团，或具有一个或多个1-16C烷基取代基的直链亚烷基，其中连接到不同碳原子上的任何一对或二对可以连接 与间插碳原子或亚烷基的原子一起形成（5-7C） - 环烷基或基团; 及其酸加成盐，其制备方法以及使用所述化合物的抗菌和抗真菌组合物和方法。
-
-
-
-
-
-
-
-
-
搜索结果
15 条记录 (耗时 0.017 秒)
