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公开(公告)号:US5215967A
公开(公告)日:1993-06-01
申请号:US443530
申请日:1989-11-30
IPC分类号: A61K38/55 , A61P5/38 , A61P9/00 , A61P9/12 , C07C231/12 , C07C237/12 , C07C237/20 , C07C237/22 , C07C309/12 , C07C309/15 , C07C311/24 , C07C311/29 , C07C311/32 , C07C317/22 , C07C323/18 , C07C323/25 , C07C323/60 , C07C335/06 , C07K1/06 , C07K1/113 , C07K5/02 , C07K5/06 , C07K14/81
CPC分类号: C07K5/0227 , C07K5/0205 , C07K5/0207 , Y10S530/80
摘要: New amino acid derivatives of the formulaR.sup.1 --Z--NR.sup.2 --CHR.sup.3 --CR.sup.4 --(CHR.sup.5).sub.a --CO--E--Q--Ywherein R.sup.1 to R.sup.5, a, Z, E, Q and Y have the meanings defined herein, and salts thereof inhibit the activity of human plasma renin.
摘要翻译: 式R1-Z-NR2-CHR3-CR4-(CHR5)a-CO-EQY的新氨基酸衍生物,其中R1至R5,a,Z,E,Q和Y具有本文定义的含义,其盐抑制 人血浆肾素活性。
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公开(公告)号:US5215966A
公开(公告)日:1993-06-01
申请号:US126060
申请日:1987-11-27
申请人: Gunter Holzemann , Peter Raddatz , Claus J. Schmitges , Klaus Otto Minck , Alfred Jonczyk , Johannes Sombroek , Joachim Gante
发明人: Gunter Holzemann , Peter Raddatz , Claus J. Schmitges , Klaus Otto Minck , Alfred Jonczyk , Johannes Sombroek , Joachim Gante
IPC分类号: C07K14/81 , A61K38/00 , A61P9/12 , C07C67/00 , C07C231/00 , C07C237/12 , C07C237/22 , C07C239/00 , C07C279/14 , C07C311/00 , C07D401/12 , C07K1/02 , C07K1/113 , C07K1/12 , C07K5/02 , C07K5/06 , C07K5/08
CPC分类号: C07D401/12 , C07K5/0227 , Y10S530/80
摘要: Novel amino acid derivatives of the formula IX--Z--NH--CHR.sup.1 --CO--NR.sup.2 --CHR.sup.3 --CR.sup.4 --(CHR.sup.5).sub.n --CO--E--W'--Ywherein X, Z, R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, E, W', Y and n have the meanings defined herein and their salts inhibit the activity of human plasma renin.
摘要翻译: 式I XZ-NH-CHR1-CO-NR2-CHR3-CR4-(CHR5)n-CO-E-W'-Y的新型氨基酸衍生物其中X,Z,R1,R2,R3,R4,R5, E,W',Y和n具有本文定义的含义,其盐抑制人血浆肾素的活性。
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公开(公告)号:US4110447A
公开(公告)日:1978-08-29
申请号:US624762
申请日:1975-10-22
申请人: Joachim Gante , Hans-Adolf Kurmeier , Erich Schacht , Werner Mehrhof , Dieter Orth , Albrecht Wild , Zdenek Simane
发明人: Joachim Gante , Hans-Adolf Kurmeier , Erich Schacht , Werner Mehrhof , Dieter Orth , Albrecht Wild , Zdenek Simane
IPC分类号: A61K31/135 , A61K31/165 , C07C67/00 , C07C213/00 , C07C217/56 , C07C217/62 , C07C217/66 , C07C233/18 , C07D209/48 , C07D233/56 , C07D233/58 , C07D233/60 , C07D295/02 , C07D295/03 , C07D295/073 , C07D295/084 , C07D295/088 , C07D295/096 , C07D521/00 , C07D295/08 , C07C91/06
CPC分类号: C07D209/48 , C07C217/62 , C07D231/12 , C07D233/56 , C07D249/08 , C07D295/03 , C07D295/073 , C07D295/088 , C07D295/092 , C07D295/096
摘要: Compounds of the formulaR--A--Zwherein R is 4-biphenylyl or 4-phenoxyphenyl or a corresponding group monosubstituted or polysubstituted by one or more of F, Cl and Br; A is --CH(CH.sub.3)--CH.sub.2 --(CH.sub.2).sub.n --, --C(CH.sub.3).dbd.CH--(CH.sub.2).sub.n -- or --C(OH) (CH.sub.3)--CH.sub.2 --(CH.sub.2).sub.n --; Z is --NR.sup.1 R.sup.2, imidazol-1-yl, phthalimido or 4,5-dihydro-4-oxophthalazin-1-yl-amino; R.sup.1 and R.sup.2 each are H or alkyl, azaalkyl or acyl, each of 1 - 6 carbon atoms or, collectively, are alkylene of 4 - 7 carbon atoms, 3-oxapentamethylene or 3-R.sup.3 -3-azapentamethylene; R.sup.3 is H or alkyl or hydroxyalkyl each of up to 6 carbon atoms; and n is 0, 1 or 2, and their physiologically acceptable acid addition salts possess anti-inflammatory, anti-arteriosclerotic and serum cholesterol and triglyceride level lowering activities.
摘要翻译: 式R-A-Z的化合物,其中R是4-联苯基或4-苯氧基苯基或被F,Cl和Br中的一个或多个单取代或多取代的相应基团; A是-CH(CH 3)-CH 2 - (CH 2)n - , - C(CH 3)= CH-(CH 2)n - 或-C(OH)(CH 3)-CH 2 - (CH 2) NR1R2,咪唑-1-基,苯二甲酰亚氨基或4,5-二氢-4-氧代酞嗪-1-基 - 氨基; R1和R2各自为H或烷基,氮杂烷基或酰基,各自为1-6个碳原子或统称为4-7个碳原子的亚烷基,3-氧杂戊撑或3-R3-3-氮杂三亚甲基; R3是H或至多6个碳原子的烷基或羟基烷基; 并且n为0,1或2,并且它们的生理上可接受的酸加成盐具有抗炎,抗动脉硬化和血清胆固醇和甘油三酯水平降低活性。
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公开(公告)号:US4060633A
公开(公告)日:1977-11-29
申请号:US681175
申请日:1976-04-28
IPC分类号: A61K31/06 , A61K31/085 , C07C27/00 , C07C33/46 , C07C41/00 , C07C43/295 , C07C67/00 , C07C253/00 , C07C255/36 , C07C255/37 , A61K31/275 , C07C121/75
CPC分类号: C07C43/295
摘要: Phenylalkanols of the formula ##STR1## wherein Ar is phenyl or phenyl monosubstituted or disubstituted by F, Cl, Br and/or CH.sub.3 ; X is F, Cl, Br or CN; m is 0 or 1; and n 2 or 3; possess antiinflammatory activity and can be produced by treating a compound of formula ##STR2## wherein Q is a functionally modified hydroxy group and Ar, X, m and n have the values given above, with a solvolyzing agent.
摘要翻译: 其中Ar是苯基的苯基链烷醇或由F,Cl,Br和/或CH 3单取代或二取代的苯基; X是F,Cl,Br或CN; m为0或1; 和n 2或3; 具有抗炎活性,可以通过用溶剂分解剂处理式为“IMAGE”的化合物,其中Q是官能改性羟基,Ar,X,m和n具有上述给出的值。
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公开(公告)号:US4057647A
公开(公告)日:1977-11-08
申请号:US695804
申请日:1976-06-14
IPC分类号: C07C69/73 , A61K31/045 , A61K31/085 , A61K31/19 , A61K31/215 , A61K31/22 , A61P3/06 , A61P7/04 , A61P25/04 , A61P29/00 , C07C27/00 , C07C29/14 , C07C29/141 , C07C29/147 , C07C29/60 , C07C33/46 , C07C41/00 , C07C43/295 , C07C51/00 , C07C57/58 , C07C57/60 , C07C57/76 , C07C59/56 , C07C59/68 , C07C67/00 , C07C69/025 , C07C69/65 , C07F1/00 , C07F9/40 , C07C31/02 , C07C43/20
CPC分类号: C07C29/60 , C07C29/147 , C07C43/295 , C07C57/58 , C07C57/60 , C07C57/76 , C07C59/56 , C07C59/68 , C07F1/005 , C07F9/4056
摘要: Compounds of the formula ##STR1## wherein R.sup.1 and R.sup.2 are the same or different and are F, Cl or Br;Q is --CH(CH.sub.3)-CH.sub.2 --, --C(OH) (CH.sub.3)-CH.sub.2 -- or --C(CH.sub.3) .dbd.CH--;Y is COOH, COOR.sup.3, CH.sub.2 OH or CH.sub.2 OAc;n is 0 or 1;R.sup.3 is alkyl or aryl of up to 8 carbon atoms or C.sub.6 H.sub.4 NHCOCH.sub.3 ; andAc is acyl of 1-8 carbon atoms;And physiologically acceptable salts thereof, are anti-inflammatory agents, which can be made from compounds of the formula Z -- X, wherein Z is ##STR2## AND X can be converted to --Q-Y.
摘要翻译: 其中R 1和R 2相同或不同,为F,Cl或Br; Q是-CH(CH 3)-CH 2 - , - C(OH)(CH 3)-CH 2 - 或-C(CH 3)= CH-; Y是COOH,COOR 3,CH 2 OH或CH 2 OAc; N IS 0或1; R3是至多8个碳原子的烷基或芳基或C6H4NHCOCH3; Ac是1-8个碳原子的酰基; 和其生物学上可接受的盐,它是可以从公式Z-X的化合物制备的抗炎剂,其中Z是
,X可以转化为-Q-Y。 -
公开(公告)号:US4049823A
公开(公告)日:1977-09-20
申请号:US552959
申请日:1975-02-25
IPC分类号: C07C69/734 , C07C29/03 , C07C29/09 , C07C29/10 , C07C29/14 , C07C29/147 , C07C29/40 , C07C33/26 , C07C33/28 , C07C41/00 , C07C43/295 , C07C51/00 , C07C59/48 , C07C59/64 , C07C59/68 , C07C67/00 , C07C69/76
CPC分类号: C07C29/03 , C07C29/09 , C07C29/095 , C07C29/10 , C07C29/14 , C07C29/147 , C07C29/40 , C07C33/26 , C07C33/28 , C07C43/295 , C07C59/48 , C07C59/68
摘要: Phenylbutanol derivatives of the formula Z--C(CH.sub.3) (OH)--CH.sub.2 --Y wherein Z is 4-biphenyl or 4-phenoxyphenyl wherein the phenoxy group is unsubstituted or substituted by F, Cl or Br and Y is COOR.sup.2 or CH.sub.2 OR.sup.3 wherein R.sup.2 is H or alkyl of 1 to 6 carbon atoms and R.sup.3 is H or alkanoyl of 1 to 6 carbon atoms, and their physiologically acceptable salts, possess anti-inflammatory activity and are produced by (a) treating with a solvolyzing agent a compound of the formula Z--C(CH.sub.3) (OH)--CH.sub.2 --W or Z--CX(CH.sub.3)--CH.sub.2 --Y wherein W is a functionally modified carboxy or methylol group different from Y and X is Cl, Br or I or a functionally modified hydroxyl group; or (b) reducing a compound otherwise corresponding to a desired final product but having instead of one of the hydrogen atoms a group which can be reduced or replaced by a hydrogen atom; or (c) oxidizing a compound otherwise corresponding to a desired final product but lacking the tertiary hydroxyl group; or (d) converting a compound otherwise corresponding to a desired final product wherein Z is a 4-phenoxyphenyl group but having instead a 4--OH--, Cl--, Br-- or I-substituted phenyl group into a desired final product; or (e) diazotizing a compound otherwise corresponding to a desired final product wherein Z is a halogen-substituted 4-phenoxyphenyl group but having an --NH.sub.2 -substituted phenoxy group and reacting the resulting diazonium salt with a halogenating agent.
摘要翻译: 式ZC(CH3)(OH)-CH2-Y的苯基丁醇衍生物,其中Z为4-联苯基或4-苯氧基苯基,其中苯氧基未被取代或被F,Cl或Br取代,Y为COOR2或CH2OR3,其中R2为H 或1〜6个碳原子的烷基,R 3为H或1〜6个碳原子的烷酰基,其生理学上可接受的盐具有抗炎活性,并通过(a)用溶剂分解剂处理式ZC化合物 (CH 3)(OH)-CH 2 -W或Z-CX(CH 3)-CH 2 -Y,其中W是不同于Y的官能改性羧基或羟甲基,X是Cl,Br或I或官能改性羟基; 或者(b)还原与所需最终产物相对应的化合物,但是其中一个氢原子可以被氢原子还原或取代的基团取代; 或(c)氧化其它对应于所需最终产物但不含叔羟基的化合物; 或(d)将其它对应于所需最终产物的化合物转化成所需的最终产物,其中Z是4-苯氧基苯基,但代之以4-OH-,Cl-,Br-或I-取代的苯基转化成所需的最终产物; 或(e)重氮化其它对应于所需最终产物的化合物,其中Z是卤素取代的4-苯氧基苯基但具有-NH 2取代的苯氧基,并使所得重氮盐与卤化剂反应。
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公开(公告)号:US3980795A
公开(公告)日:1976-09-14
申请号:US628933
申请日:1975-11-05
IPC分类号: C07D231/08 , A61K31/415
CPC分类号: C07D231/08
摘要: Pyrazolidinones of the formula ##SPC1##Wherein R is a phenyl, phenoxy or a corresponding group monosubstituted or polysubstituted by one or more of F, Cl and Br possess anti-inflammatory activity.
摘要翻译: 式WHEREIN R是苯基,苯氧基或被F,Cl和Br中的一个或多个单取代或多取代的相应基团的吡唑烷酮具有抗炎活性。
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公开(公告)号:US3975403A
公开(公告)日:1976-08-17
申请号:US395980
申请日:1973-09-10
申请人: Joachim Gante , Werner Mehrhof , Albrecht Wild
发明人: Joachim Gante , Werner Mehrhof , Albrecht Wild
IPC分类号: B01J23/00 , B01J31/00 , C07B61/00 , C07D327/08 , C07D335/12 , C07D339/08
CPC分类号: C07D327/08 , C07D339/08 , Y10S514/916
摘要: Compounds of the formula ##SPC1##Wherein R.sub.1 is COOH, COO-alkyl, CH.sub.2 OH or CH.sub.2 -alkanoyl; R.sub.2 is CH.sub.3 or C.sub.2 H.sub.5 ; R.sub.3 is H, F, Cl or Br; and Y is CH.sub.2, O or S, at least one Y being S, and the physiologically acceptable salts thereof, possesses antiphlogistic activity.
摘要翻译: 式WHERE R1的化合物是COOH,COO-烷基,CH2OH或CH2-烷酰基; R2是CH3或C2H5; R3是H,F,Cl或Br; Y为CH 2,O或S,至少一个Y为S,且其生理上可接受的盐具有消炎活性。
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