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1. 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。

2. 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。

3. 发明授权

US4200652A Alkanolamine derivatives 失效
标题翻译：烷醇胺衍生物
公开(公告)号：US4200652A
公开(公告)日：1980-04-29
申请号：US930164
申请日：1978-08-02
申请人： Michael S. Large , Leslie H. Smith
发明人： Michael S. Large , Leslie H. Smith
IPC分类号： C07D213/40 , C07D307/52 , C07D307/79 , C07D309/04 , C07D319/18 , C07D333/54 , A61K31/165 , C07C103/22
CPC分类号： C07D213/40 , C07D307/52 , C07D307/79 , C07D309/04 , C07D319/18 , C07D333/54
摘要： Novel 1-aryloxy-3-carbamoylalkylamino-2-propanol derivatives, processes for their manufacture, pharmaceutical compositions containing them and methods of using them in the treatment of heart diseases. The compounds possess .beta.-adrenergic blocking activity. Representative of the compounds disclosed is 1-(2-cyanophenoxy)-3-.beta.-(N-2-furfurylcarbamoyl)ethylamino-2-propanol.
摘要翻译：新的1-芳氧基-3-氨基甲酰基烷基氨基-2-丙醇衍生物，其制备方法，含有它们的药物组合物和使用它们用于治疗心脏病的方法。该化合物具有β-肾上腺素能阻滞活性。所公开的化合物的代表是1-（2-氰基苯氧基）-3-β-（N-2-糠基氨基甲酰基）乙基氨基-2-丙醇。

4. 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.

5. 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.

6. 发明授权

US4751240A Phenol derivatives 失效
标题翻译：苯酚衍生物
公开(公告)号：US4751240A
公开(公告)日：1988-06-14
申请号：US726824
申请日：1985-04-24
申请人： Jean Bowler , Graham C. Crawley , Philip N. Edwards , Alasdair T. Glen , Michael S. Large , Brian S. Tait
发明人： Jean Bowler , Graham C. Crawley , Philip N. Edwards , Alasdair T. Glen , Michael S. Large , Brian S. Tait
IPC分类号： C07D307/38 , A61K31/165 , A61K31/17 , A61K31/18 , A61K31/19 , A61K31/195 , A61K31/215 , A61K31/22 , A61K31/275 , A61K31/33 , A61P35/00 , C07C45/00 , C07C45/46 , C07C45/51 , C07C45/68 , C07C49/24 , C07C49/255 , C07C49/755 , C07C49/757 , C07C51/00 , C07C65/32 , C07C65/40 , C07C67/00 , C07C69/738 , C07C233/04 , C07C253/00 , C07C255/56 , C07C269/00 , C07C275/24 , C07C279/00 , C07C301/00 , C07C303/38 , C07C311/16 , C07C313/00 , C07C317/00 , C07C317/18 , C07C317/46 , C07C321/06 , C07C323/03 , C07C323/04 , C07C323/65 , C07C325/00 , C07C327/38 , C07D311/02 , C07D333/54 , C07F7/18 , C07F9/50 , A61K31/235 , A61K31/10
CPC分类号： C07C323/16 , C07C317/18 , C07C45/46 , C07C45/515 , C07C45/68 , C07C49/755 , C07C49/757 , C07C65/40 , C07F7/1856 , C07F9/5031 , C07C2102/10
摘要： A phenol derivative of the formulaNU--A--X--R.sup.1wherein 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.sup.1 is hydrogen, or alkyl, alkenyl, alkynyl, cycloalkyl, halogenoalkyl, alkoxyalkyl, halogenoalkoxyalkyl, aryl or arylalkyl, or R.sup.1 is joined to R.sup.2, and wherein X is --CONR.sup.2 --, --CSNR.sup.2 --, --NR.sup.12 CO--, --NR.sup.12 CS--, --NR.sup.12 CONR.sup.2 --, ##STR1## --SO.sub.2 NR.sup.2 --or --CO--, or, when R.sup.1 is not hydrogen, is --NR.sup.12 COO--, --(PO)R.sup.2 13 , --S--, --SO--or --SO.sub.2 --, wherein R.sup.2 is hydrogen or alkyl, or R.sup.1 and R.sup.2 together form alkylene; wherein R.sup.12 is hydrogen or alkyl, and wherein R.sup.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 tumors 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; 羟基苯基 - 萘基; 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是可以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不育症。

7. 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.

8. 发明授权

US4574123A 4,4'-Alkylenedipiperidine derivatives 失效
标题翻译： 4,4'-亚烷基二哌啶衍生物
公开(公告)号：US4574123A
公开(公告)日：1986-03-04
申请号：US606688
申请日：1984-05-03
申请人： Philip N. Edwards , Michael S. Large
发明人： Philip N. Edwards , Michael S. Large
IPC分类号： A01N47/44 , A61K31/445 , A61P31/04 , C07C279/28 , C07D211/06 , C07D211/16 , C07D401/14 , A01N43/40
CPC分类号： C07C279/28 , C07D211/06 , C07D211/16
摘要： A 4,4'-alkylenebis[piperidine-1-(N-amidinoamidine)] derivative of the formula: ##STR1## or a tautomeric form thereof, wherein each of R.sup.1, R.sup.2, R.sup.3 and R.sup.4, which may be the same or different, is hydrogen or an alkyl, alkenyl or alkoxyalkyl radical of up to 20 carbon atoms; or R.sup.1, R.sup.2 and the nitrogen atom to which they are attached, or R.sup.3 and R.sup.4 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; a 3-20C cycloalkyl radical; or an optionally substituted phenyl or phenylalkyl radical; provided that at least one of R.sup.1, R.sup.2, R.sup.3 and R.sup.4 is other than hydrogen; X is a direct bond or a 1-6C straight- or branched-chain alkylene radical which is linked to the 3- or 4-positions of the piperidine rings; and R.sup.5 and R.sup.6, which may be the same or different, are each hydrogen or a 1-8C alkyl radical; and the acid addition salts thereof, processes for their manufacture, and antibacterial and antifungal compositions and methods using said compounds.
摘要翻译：具有下式的4,4'-亚烷基双[哌啶-1-（N-脒基脒））衍生物或其互变异构形式，其中R 1，R 2，R 3， R 2，R 3和R 4可以相同或不同，是氢或至多20个碳原子的烷基，烯基或烷氧基烷基; 或它们所连接的R 1，R 2和它们所连接的氮原子，或者R 3和R 4及它们所连接的氮原子可以相同或不同，分别为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; 3-20C环烷基; 或任选取代的苯基或苯基烷基; 条件是R 1，R 2，R 3和R 4中的至少一个不是氢; X是与哌啶环的3-或4-位连接的直接键或1-6C直链或支链亚烷基; R 5和R 6可以相同或不同，分别为氢或1-8C烷基; 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。

9. 发明授权

US06441012B1 Chemical compounds 失效
标题翻译：化合物
公开(公告)号：US06441012B1
公开(公告)日：2002-08-27
申请号：US09744331
申请日：2001-01-23
申请人： David R Brittain , Craig Johnstone , Michael S Large , Gareth M Davies
发明人： David R Brittain , Craig Johnstone , Michael S Large , Gareth M Davies
IPC分类号： C07D26358
CPC分类号： C07D263/58 , C07D413/04
摘要： Compound of formula (I) wherein: A is a bicyclic heteroaryl, optionally substituted with one or more substituents; B is linker group connecting group A to group D and comprising a 3 or 4 atom linker where each atom is independently selected from carbon, oxygen, nitrogen and sulphur and is optionally subsituted with one or more C1-6 alkyl groups or two of such adjacent alkyl substituents may form a ring; C is aryl or a mono or bicyclic heteroaryl, each of which can be optionally substituted; D is an aryl or heteroaryl, both of which are optionally substituted R1 is hydrogen, C1-5 alkyl, C1-3 alkanoyl or C1-3 alkoxycarbonyl; R2 to R5 are each independently selected from hydrogen, C1-6 alkyl, aryl and heteroaryl containing up to 2 heteroatoms chosen from oxygen, sulphur and nitrogen, the aryl and heteroaryl optionally substituted with C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-4 alkoxy, C1-4 alkanoyl, C1-6 alkylamino, C1-4alkylC1-6alkyoxyl, C1-6alkylaminoC1-6alkyl, nitro, cyano, halogeno, trifluoromethyl, hydroxy, (CH2)pOH where p is 1 or 2, —CO2Ra, and —CONRaRb, where Ra and Rb are independently selected from hydrogen and C1-6 alkyl or two of R2 to R5 can be taken together to form a 3 to 7 membered ring; R6 is an acidic functional group; r and s are each independently 0 or 1 with the proviso that r and s cannot both be 0; or a pharmaceutically acceptable salt or in vivo hydrolysable derivative thereof.
摘要翻译：式（I）的化合物，其中：A是任选被一个或多个取代基取代的二环杂芳基; B是连接基团A与D组并且包含3或4个原子连接体的连接基团，其中每个原子独立地选自碳，氧，氮和硫，并且任选被一个或多个C 1-6烷基取代或两个相邻的烷基取代基可以形成环; C是芳基或单或双环杂芳基，其各自可任选被取代; D是芳基或杂芳基，它们都是任选取代的R 1是氢，C 1-5烷基，C 1-3烷酰基或C 1-3烷氧基羰基; R 2至R 5各自独立地选自氢，C 1-6烷基，芳基和含有至多2个选自氧，硫和氮的杂原子的杂芳基，芳基和杂芳基任选被C 1-6烷基，C 2-6烯基， 6-炔基，C 1-4烷氧基，C 1-4烷酰基，C 1-6烷基氨基，C 1-4烷基C 1-6烷氧基，C 1-6烷基氨基C 1-6烷基，硝基，氰基，卤代，三氟甲基，羟基，（CH 2）p OH其中p为1或2 ，-CO 2 R a和-CONR a R b，其中R a和R b独立地选自氢和C 1-6烷基，或者R 2至R 5中的两个可以一起形成3至7元环; R6是酸性官能团; r和s各自独立地为0或1，条件是r和s不能都是0; 或其药学上可接受的盐或体内可水解的衍生物。

10. 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。

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