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1.
公开(公告)号:US4774253A
公开(公告)日:1988-09-27
申请号:US917566
申请日:1986-10-10
IPC分类号: C07D261/08 , C07D263/32 , C07D413/04 , A61K31/42 , C07D261/06 , C07D263/30
CPC分类号: C07D413/04 , C07D261/08 , C07D263/32
摘要: Oxazole and isoxazole derivatives of the formula ##STR1## wherein A is C.sub.1-6 -alkylene, Het is a 2-R-oxazol-5-yl, 5-R-oxazol-2-yl, 4-R-oxazol-2-yl, 2-R-oxazol-4-yl, 3-R-isoxazol-5-yl or 5-R-isoxazol-3-yl group which is optionally substituted on the heterocyclic ring by a C.sub.1-6 -alkyl group, R is phenyl or thienyl monosubstituted or disubstituted by halogen, trifluoromethyl or C.sub.1-6 -alkylthio, R.sup.1 and R.sup.2 each is a C.sub.1-6 -alkyl group and R.sup.3 is a hydroxy or C.sub.1-6 -alkoxy group or a group of the formula --NR.sup.4 R.sup.5 in which R.sup.4 and R.sup.5 each is a hydrogen atom or a C.sub.1-6 -alkyl group or R.sup.4 and R.sup.5 together with the nitrogen atom to which they are attached is a 5-membered or 6-membered saturated heteromonocyclic ring which may contain an oxygen or sulphur atom or an additional nitrogen atom, and pharmaceutically acceptable salts of the compounds of formula I in which R.sup.3 is a hydroxy group with bases, have anti-arthritic activity.
摘要翻译: 下式的恶唑和异恶唑衍生物其中A是C 1-6 - 亚烷基,Het是2-R唑恶基,5-R唑-2-基,4-R-恶唑-2 芳基,2-R-恶唑-4-基,3-R-异恶唑-5-基或5-R-异恶唑-3-基,其在杂环上被C 1-6 - 烷基任意取代, R是苯基或被卤素,三氟甲基或C 1-6 - 烷硫基单取代或二取代的噻吩基,R 1和R 2各自是C 1-6 - 烷基,R 3是羟基或C 1-6 - 烷氧基或式 - NR4R5其中R4和R5各自为氢原子或C1-6烷基或R4和R5与它们所连接的氮原子一起为可含有氧的5元或6元饱和杂单环 或硫原子或另外的氮原子,以及其中R3是具有碱基的羟基的式I化合物的药学上可接受的盐具有抗关节炎活性。
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公开(公告)号:US5157041A
公开(公告)日:1992-10-20
申请号:US362621
申请日:1989-06-05
IPC分类号: A61K31/13 , A61K31/33 , A61K31/40 , A61K31/401 , A61K31/403 , A61K31/4035 , A61K31/404 , A61K31/425 , A61K31/426 , A61K31/435 , A61K31/4427 , A61K31/445 , A61K31/47 , A61K31/472 , A61K31/495 , A61K38/00 , A61P31/12 , A61P43/00 , C07C237/10 , C07C237/22 , C07C291/02 , C07C311/05 , C07C311/18 , C07C317/48 , C07C323/60 , C07D207/16 , C07D209/42 , C07D209/48 , C07D209/52 , C07D211/60 , C07D215/48 , C07D217/26 , C07D241/04 , C07D277/04 , C07D277/06 , C07D279/06 , C07D401/12 , C07D403/12 , C07D471/04 , C07D521/00 , C07K5/02
CPC分类号: C07D401/12 , C07D207/16 , C07D209/42 , C07D209/52 , C07D211/60 , C07D215/48 , C07D217/26 , C07D241/04 , C07D277/06 , C07D279/06 , C07D403/12 , C07D471/04 , C07K5/021
摘要: Compounds of the formula ##STR1## wherein R.sup.1 is alkoxycarbonyl, aralkoxycarbonyl, alkanoyl, cycloalkylcarbonyl, aralkanoyl, aroyl, heterocyclylcarbonyl, alkylsulphonyl, arylsulphonyl, monoaralkylcarbamoyl, cinnamoyl or .alpha.-aralkoxycarbonylaminoalkanoyl and R.sup.2 is hydrogen or R.sup.1 and R.sup.2 together with the nitrogen atom to which they are attached represent a cyclic imide group of the formula ##STR2## in which P and Q together represent an aromatic system; R.sup.3 is alkyl, cycloalkyl, aryl, aralkyl, heterocyclylalkyl, cyanoalkyl, alkyl- sulphinylalkyl, carbamoylalkyl or alkoxycarbonylalkyl or, when n stands for zero, R.sup.3 can also represent alkylthioalkyl or, when n stands for 1, R.sup.3 can also represent alkylsulphonylalkyl; R.sup.4 is alkyl, cycloalkyl, cycloalkylalkyl, aryl or aralkyl; R.sup.5 is hydrogen and R.sup.6 is hydroxy or R.sup.5 and R.sup.6 together represent oxo; R.sup.7 and R.sup.8 together represent a trimethylene or tetramethylene group which is optionally substituted by hydroxy, alkoxycarbonylamino or acylamino or in which one --CH.sub.2 -- group is replaced by --NH--, --N(alkoxycar- bonyl)--, --N(alkyl)-- or --S-- or which carries a fused cycloalkane, aromatic or heteroaromatic ring; and R.sup.9 is alkoxycarbonyl, monoalkylcarbamoyl, monoaralkylcarbamoyl, monoarylcarbamoyl or a group of the formula ##STR3## in which R.sup.10 and R.sup.11 each represent alkyl; and their pharmaceutically acceptable acid addition salts inhibit proteases of viral origin and can be used as medicaments for the treatment or prophylaxis of viral infections. They can be manufactured according to generally known procedures.
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公开(公告)号:US4649160A
公开(公告)日:1987-03-10
申请号:US773390
申请日:1985-09-06
申请人: Peter J. Machin
发明人: Peter J. Machin
IPC分类号: C07C217/34 , A61K31/135 , A61K31/138 , A61P9/00 , A61P9/06 , A61P9/12 , C07C29/147 , C07C43/178 , C07C43/20 , C07C43/23 , C07C45/71 , C07C49/84 , C07C59/66 , C07C215/00 , C07C215/02 , C07D303/24
CPC分类号: C07C29/147 , C07C43/1782 , C07C43/1786 , C07C43/23 , C07C45/71 , C07C49/84 , C07C59/66
摘要: Substituted phenoxy-aminopropanols of the formula ##STR1## wherein R is a branched-chain alkyl of 3 or 4 carbon atoms, R.sup.1 is hydrogen, halogen or lower alkyl and R.sup.2 and R.sup.3, independently, are hydrogen, halogen, lower alkyl, lower alkoxy or lower alkylthio, and pharmaceutically acceptable acid addition salts thereof, are described. A process for their preparation, as well as pharmaceutical preparations containing them are also described. The compounds of formula I and their salts possess cardioselective .beta.-adrenergic blocking activity and antihypertensive activity.
摘要翻译: 下式的取代的苯氧基 - 氨基丙醇其中R是3或4个碳原子的支链烷基,R1是氢,卤素或低级烷基,R2和R3独立地是氢,卤素,低级烷基,低级 烷氧基或低级烷硫基,及其药学上可接受的酸加成盐。 还描述了其制备方法,以及含有它们的药物制剂。 式I化合物及其盐具有心脏选择性β-肾上腺素能阻断活性和抗高血压活性。
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公开(公告)号:US4577030A
公开(公告)日:1986-03-18
申请号:US475290
申请日:1983-03-14
申请人: Peter J. Machin
发明人: Peter J. Machin
IPC分类号: A61K31/395 , C07C43/23 , C07D231/12 , C07D231/14 , C07D231/16 , C07D231/56 , C07D233/60 , C07D235/06 , C07D249/04 , C07D249/08 , C07D249/18 , C07D521/00
CPC分类号: C07C43/23 , C07D231/12 , C07D231/14 , C07D231/16 , C07D231/56 , C07D233/56 , C07D235/06 , C07D249/04 , C07D249/08 , C07D249/18
摘要: Phenoxy-aminopropanol derivatives of the formula ##STR1## wherein R is lower alkyl, X is oxygen or sulfur, n is the integer zero or 1, Y is methylene, ethylene or propylene or, when n is zero, Y can also be a group of the formula ##STR2## wherein the double-bond is trans and the carbon atom marked with an asterisk is linked to Z, and Z is a 5-membered aromatic heterocyclic ring which contains one or more nitrogen atoms as the sole hetero atom (s), said heterocyclic ring is linked to Y via a nitrogen atom, and may be substituted by halogen, lower alkyl, lower alkoxy, aryl, cyano or carboxamido, or on adjacent carbon atoms by a group of the formula--(CH.sub.2).sub.4 -- (b)or--CH.dbd.CH--CH.dbd.CH--, (c)and pharmaceutically acceptable acid addition salts thereof are described. A process for the preparation of the compound of formula I and pharmaceutical preparations containing them are also described. The aforementioned compounds and salts possess .beta.-adrenergic blocking activity and antihypertensive activity.
摘要翻译: 下式的苯氧基 - 氨基丙醇衍生物其中R为低级烷基,X为氧或硫,n为整数0或1,Y为亚甲基,亚乙基或亚丙基,或当n为零时,Y也可为 式中-CH = CH- * CH 2 - (a)的基团,其中双键是反式,并且带有星号的碳原子与Z连接,Z是含有一个或多个的5元芳族杂环 氮原子作为唯一的杂原子,所述杂环通过氮原子与Y连接,并且可以被卤素,低级烷基,低级烷氧基,芳基,氰基或甲酰氨基取代,或在相邻碳原子上被一个基团 描述了式 - (CH 2)4 - (b)或-CH = CH-CH = CH-,(c)及其药学上可接受的酸加成盐。 还描述了制备式I化合物的方法和含有它们的药物制剂。 上述化合物和盐具有β-肾上腺素能阻断活性和抗高血压活性。
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公开(公告)号:US5620987A
公开(公告)日:1997-04-15
申请号:US398478
申请日:1995-04-10
IPC分类号: A61K31/13 , A61K31/33 , A61K31/40 , A61K31/401 , A61K31/403 , A61K31/4035 , A61K31/404 , A61K31/425 , A61K31/426 , A61K31/435 , A61K31/4427 , A61K31/445 , A61K31/47 , A61K31/472 , A61K31/495 , A61K38/00 , A61P31/12 , A61P43/00 , C07C237/10 , C07C237/22 , C07C291/02 , C07C311/05 , C07C311/18 , C07C317/48 , C07C323/60 , C07D207/16 , C07D209/42 , C07D209/48 , C07D209/52 , C07D211/60 , C07D215/48 , C07D217/26 , C07D241/04 , C07D277/04 , C07D277/06 , C07D279/06 , C07D401/12 , C07D403/12 , C07D471/04 , C07D521/00 , C07K5/02 , C07D217/16
CPC分类号: C07D401/12 , C07D207/16 , C07D209/42 , C07D209/52 , C07D211/60 , C07D215/48 , C07D217/26 , C07D241/04 , C07D277/06 , C07D279/06 , C07D403/12 , C07D471/04 , C07K5/021
摘要: Compounds of the formula ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, and --N(R.sup.7)--CH(R.sup.8)(R.sup.9) are as claimed herein or their pharmaceutically acceptable acid addition salts inhibit proteases of viral origin and can be used as medicaments for the treatment of viral infections. They can be manufactured according to generally known procedures.
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公开(公告)号:US5446161A
公开(公告)日:1995-08-29
申请号:US916812
申请日:1992-07-20
IPC分类号: A61K31/13 , A61K31/33 , A61K31/40 , A61K31/401 , A61K31/403 , A61K31/4035 , A61K31/404 , A61K31/425 , A61K31/426 , A61K31/435 , A61K31/4427 , A61K31/445 , A61K31/47 , A61K31/472 , A61K31/495 , A61K38/00 , A61P31/12 , A61P43/00 , C07C237/10 , C07C237/22 , C07C291/02 , C07C311/05 , C07C311/18 , C07C317/48 , C07C323/60 , C07D207/16 , C07D209/42 , C07D209/48 , C07D209/52 , C07D211/60 , C07D215/48 , C07D217/26 , C07D241/04 , C07D277/04 , C07D277/06 , C07D279/06 , C07D401/12 , C07D403/12 , C07D471/04 , C07D521/00 , C07K5/02 , C07D211/40 , C07D211/36 , C07D211/56
CPC分类号: C07D401/12 , C07D207/16 , C07D209/42 , C07D209/52 , C07D211/60 , C07D215/48 , C07D217/26 , C07D241/04 , C07D277/06 , C07D279/06 , C07D403/12 , C07D471/04 , C07K5/021
摘要: Compounds of the formula ##STR1## wherein and their pharmaceutically acceptable acid addition salts inhibit proteases of vital origin and can be used as medicaments for the treatment or prophylaxis of viral infections. They can be manufactured according to generally known procedures.
摘要翻译: 式Ⅰ的化合物及其药学上可接受的酸加成盐抑制重要起源的蛋白酶,并可用作治疗或预防病毒感染的药物。 它们可以根据通常已知的方法制造。
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公开(公告)号:US5554756A
公开(公告)日:1996-09-10
申请号:US391380
申请日:1995-02-17
IPC分类号: A61K31/13 , A61K31/33 , A61K31/40 , A61K31/401 , A61K31/403 , A61K31/4035 , A61K31/404 , A61K31/425 , A61K31/426 , A61K31/435 , A61K31/4427 , A61K31/445 , A61K31/47 , A61K31/472 , A61K31/495 , A61K38/00 , A61P31/12 , A61P43/00 , C07C237/10 , C07C237/22 , C07C291/02 , C07C311/05 , C07C311/18 , C07C317/48 , C07C323/60 , C07D207/16 , C07D209/42 , C07D209/48 , C07D209/52 , C07D211/60 , C07D215/48 , C07D217/26 , C07D241/04 , C07D277/04 , C07D277/06 , C07D279/06 , C07D401/12 , C07D403/12 , C07D471/04 , C07D521/00 , C07K5/02 , C07D211/32
CPC分类号: C07D401/12 , C07D207/16 , C07D209/42 , C07D209/52 , C07D211/60 , C07D215/48 , C07D217/26 , C07D241/04 , C07D277/06 , C07D279/06 , C07D403/12 , C07D471/04 , C07K5/021
摘要: Compositions containing compounds ##STR1## and their pharmaceutically acceptable acid addition salts inhibit proteases of viral origin and can be used as medicaments for the treatment or prophylaxis of viral infections. They can be manufactured according to generally known procedures.
摘要翻译: 含有化合物的组合物及其药学上可接受的酸加成盐抑制病毒来源的蛋白酶,并且可以用作治疗或预防病毒感染的药物。 它们可以根据通常已知的方法制造。
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8.
公开(公告)号:US4996358A
公开(公告)日:1991-02-26
申请号:US336264
申请日:1989-04-11
IPC分类号: C12N9/99 , A61K31/16 , A61K31/165 , A61K31/195 , A61K31/22 , A61K31/395 , A61K38/00 , A61P29/00 , A61P43/00 , C07C67/00 , C07C231/00 , C07C237/06 , C07C237/08 , C07C237/12 , C07C237/22 , C07C259/06 , C07C313/00 , C07C323/60 , C07D207/40 , C07D225/02 , C07K1/02 , C07K5/06 , C07K5/065 , C07K5/068
CPC分类号: C07K5/06086 , C07K5/06026 , C07K5/06043 , C07K5/06052 , C07K5/06078 , A61K38/00
摘要: Compounds of the formula ##STR1## wherein A is a group of the formula HN(OH)--CO-- or HCO--N(OH)--; R.sup.1 is a C.sub.2 -C.sub.5 -alkyl; R.sup.2 is the characterizing group of a natural .alpha.-amino acid in which any functional group present may be protected, any amino group present may be acylated and any carboxyl group present may be amidated, with the proviso that R.sup.2 is not hydrogen or methyl; R.sup.3 is hydrogen, amino, hydroxy, mercapto, C.sub.1 -C.sub.6 -alkyl, C.sub.1 -C.sub.4 -alkoxy, C.sub.1 -C.sub.6 -alkylamino, C.sub.1 -C.sub.6 -alkylthio or aryl-(C.sub.1 -C.sub.6 -alkyl), or amino-(C.sub.1 -C.sub.6 -alkyl), hydroxy-(C.sub.1 -C.sub.6 -alkyl), mercapto-(C.sub.1 -C.sub.6 -alkyl) or carboxy-(C.sub.1 -C.sub.6 -alkyl) in which the amino, hydroxy, mercapto or carboxyl group may be protected, the amino group may be acylated or the carboxyl group may be amidated; R.sup.4 is hydrogen or methyl; R.sup.5 is hydrogen or a C.sub.1 -C.sub.6 -alkyl, C.sub.1 -C.sub.6 -alkoxy-C.sub.1 -C.sub.6 -alkyl, di(C.sub.1 -C.sub.6 -alkoxy)-methylene, carboxyl, (C.sub.1 -C.sub.6 -alkyl)-carbonyl, (C.sub.1 -C.sub.6 -alkoxy)carbonyl, arylmethoxycarbonyl, (C.sub.1 -C.sub.6 -alkyl)aminocarbonyl or arylaminocarbonyl; and R.sup.6 is hydrogen or methyl; or R.sup.2 and R.sup.4 taken together are a group of the formula --(CH.sub.2).sub.n -- in which n is a number from 4 to 11; or R.sup.4 and R.sup.6 taken together are a trimethylene; and pharmaceutically acceptable salts of those compounds which are acidic or basic are described. The compounds of formula I possess collagenase inhibitory activity and can be used in the control or prevention of degenerative joint diseases.
摘要翻译: 式(Ⅰ)化合物其中A为式HN(OH)-CO-或HCO-N(OH) - 的基团; R1是C2-C5-烷基; R2是天然α-氨基酸的表征基团,其中存在的任何官能团可以被保护,任何存在的氨基可以被酰化,并且存在的任何羧基可以被酰胺化,条件是R 2不是氢或甲基; R3是氢,氨基,羟基,巯基,C1-C6-烷基,C1-C4-烷氧基,C1-C6-烷基氨基,C1-C6-烷硫基或芳基 - (C1-C6-烷基)或氨基 - (C1- C6烷基),羟基 - (C1-C6-烷基),巯基 - (C1-C6-烷基)或羧基 - (C1-C6-烷基),其中氨基,羟基,巯基或羧基可被保护 氨基可以被酰化或羧基可以酰胺化; R4是氢或甲基; R 5是氢或C 1 -C 6烷基,C 1 -C 6烷氧基-C 1 -C 6烷基,二(C 1 -C 6 - 烷氧基) - 亚甲基,羧基,(C 1 -C 6 - 烷基) - 羰基,(C 1 -C 6 - 烷氧基)羰基,芳基甲氧基羰基,(C 1 -C 6 - 烷基)氨基羰基或芳基氨基羰基; R6为氢或甲基; 或者R 2和R 4一起是式 - (CH 2)n - 的基团,其中n是4至11的数; 或R4和R6一起是三亚甲基; 和描述了那些酸性或碱性化合物的药学上可接受的盐。 式I化合物具有胶原酶抑制活性,可用于控制或预防退行性关节疾病。
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公开(公告)号:US4663462A
公开(公告)日:1987-05-05
申请号:US788186
申请日:1985-10-16
申请人: Peter J. Machin
发明人: Peter J. Machin
IPC分类号: A61K31/395 , C07C43/23 , C07D231/12 , C07D231/14 , C07D231/16 , C07D231/56 , C07D233/60 , C07D235/06 , C07D249/04 , C07D249/08 , C07D249/18 , C07D521/00
CPC分类号: C07C43/23 , C07D231/12 , C07D231/14 , C07D231/16 , C07D231/56 , C07D233/56 , C07D235/06 , C07D249/04 , C07D249/08 , C07D249/18
摘要: Phenoxy-aminopropanol derivatives of the formula ##STR1## wherein R is lower alkyl, X is oxygen or sulfur, n is the integer zero or 1, Y is methylene, ethylene or propylene or, when n is zero, Y can also be a group of the formula--CH.dbd.CH--C*H.sub.2 --, (a) wherein the double-bond is trans and the carbon atom marked with an asterisk is linked to Z, and Z is a 5-membered aromatic heterocyclic ring which contains one or more nitrogen atoms as the sole hetero atom (s), said heterocyclic ring is linked to Y via a nitrogen atom, and may be substituted by halogen, lower alkyl, lower alkoxy, aryl, cyano or carboxamido, or on adjacent carbon atoms by a group of the formula--(CH.sub.2).sub.4 -- (b)or--CH.dbd.CH--CH.dbd.CH--, (c)and pharmaceutically acceptable acid addition salts thereof are described. A process for the preparation of the compound of formula I and pharmaceutical preparations containing them are also described. The aforementioned compounds and salts possess .beta.-adrenergic blocking activity and antihypertensive activity.
摘要翻译: 下式的苯氧基 - 氨基丙醇衍生物其中R为低级烷基,X为氧或硫,n为整数0或1,Y为亚甲基,亚乙基或亚丙基,或当n为零时,Y也可为 基团-CH = CH-C * H 2 - ,(a)其中双键是反式,并且带有星号的碳原子与Z连接,Z是含有一个的5元芳族杂环 或更多的氮原子作为唯一的杂原子,所述杂环通过氮原子与Y连接,并且可以被卤素,低级烷基,低级烷氧基,芳基,氰基或甲酰氨基取代,或在相邻碳原子上被 描述了式 - (CH 2)4 - (b)或-CH = CH-CH = CH-,(c)的基团及其药学上可接受的酸加成盐。 还描述了制备式I化合物的方法和含有它们的药物制剂。 上述化合物和盐具有β-肾上腺素能阻断活性和抗高血压活性。
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公开(公告)号:US5006651A
公开(公告)日:1991-04-09
申请号:US410779
申请日:1989-09-22
申请人: Michael J. Broadhurst , Balraj K. Handa , William H. Johnson , Geoffrey Lawton , Peter J. Machin
发明人: Michael J. Broadhurst , Balraj K. Handa , William H. Johnson , Geoffrey Lawton , Peter J. Machin
CPC分类号: C07K5/06191 , A61K38/00
摘要: The invention relates compounds of the formula ##STR1## wherein R.sup.1 -R.sup.5 and X have the significance given in the description, and their pharmaceutically acceptable salts. The compounds of formula I inhibit the enzyme collagenase and can be used in the form of medicaments for the control or prevention of degenerative joint diseases such as rheumatoid arthritis and osteoarthritis.
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