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1.发明授权Lipid lowering and anti-thrombotic 6-arylpyridazin-3-ones and a process for their preparation 失效降脂和抗血栓形成6-芳基哒嗪-3-酮及其制备方法
公开(公告)号：US4289774A
公开(公告)日：1981-09-15
申请号：US86604
申请日：1979-10-19
申请人： Erich Schacht , Hans-Adolf Kurmeier , Joachim Gante , Reinhard Lissner , Guido Melzer , Dieter Orth
发明人： Erich Schacht , Hans-Adolf Kurmeier , Joachim Gante , Reinhard Lissner , Guido Melzer , Dieter Orth
IPC分类号： A61K31/50 , A61P3/06 , A61P3/08 , A61P7/02 , A61P9/10 , A61P25/00 , A61P25/04 , A61P29/00 , C07D237/04 , C07D237/14 , C07D237/32 , C07D401/04 , C07D237/26
CPC分类号： C07D237/32 , C07D237/04 , C07D237/14
摘要： Compounds of the formula ##STR1## wherein R.sup.1 is 4-biphenylyl, 4-phenoxyphenyl or 4-biphenylyl or 4-phenoxyphenyl substituted in the 4'-position by F, Cl, Br or I; R.sup.2 is H, C.sub.1-4 -alkyl, hydroxy-C.sub.1-4 -alkyl or pyridyl; R.sup.3 and R.sup.6 are each H or alkyl of 1-4 carbon atoms, or together are--(CH.sub.2).sub.4 --; and R.sup.4 and R.sup.5 are each H or together are a C--C bond; at least one of the radicals R.sup.2, R.sup.3 and R.sup.6 being other than hydrogen, possess valuable pharmacological properties, e.g., lower lipid levels and are anti-thrombotic.
摘要翻译： 其中R 1是被F，Cl，Br或I取代在4'-位的4-联苯基，4-苯氧基苯基或4-联苯基或4-苯氧苯基的式的化合物; R 2是H，C 1-4 - 烷基，羟基-C 1-4 - 烷基或吡啶基; R 3和R 6各自为H或1-4个碳原子的烷基，或一起为 - （CH 2）4 - ; 且R 4和R 5各自为H或一起为C-C键; 基团R 2，R 3和R 6中的至少一个不同于氢，具有有价值的药理学性质，例如较低的脂质水平并且是抗血栓形成的。
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公开(公告)号：US4151294A
公开(公告)日：1979-04-24
申请号：US805045
申请日：1977-06-09
申请人： Hans-Adolf Kurmeier , Erich Schacht , Joachim Gante , Dieter Orth , Zdenek Simane , Albrecht Wild
发明人： Hans-Adolf Kurmeier , Erich Schacht , Joachim Gante , Dieter Orth , Zdenek Simane , Albrecht Wild
IPC分类号： C07C43/295 , A61K31/055 , A61K31/085 , A61K31/35 , A61K31/351 , A61P3/06 , A61P7/02 , A61P25/04 , A61P29/00 , C07C27/00 , C07C33/48 , C07C41/00 , C07C67/00 , C07D309/12 , C07C33/06 , C07C43/28
CPC分类号： C07D309/12
摘要： Alkynols of the formula, ##STR1## wherein X is F, Cl or Br; n is 0 or 1; m is 0 or 1 and R (if m is 0) is hydroxyalkyl of 1-6 carbon atoms or (if m is 1) alkyl, straight-chain hydroxyalkyl or straight-chain tetrahydropyran-2-yloxyalkyl of 2-6 carbon atoms in the alkyl, have anti-inflammatory activity.
摘要翻译： 式中的炔诺酮，其中X为F，Cl或Br; n为0或1; m为0或1，R（如果m为0）为1-6个碳原子的羟烷基或（如果m为1）烷基，直链羟烷基或2-6个碳原子的直链四氢吡喃-2-基氧基烷基 该烷基具有抗炎活性。
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公开(公告)号：US4115456A
公开(公告)日：1978-09-19
申请号：US697579
申请日：1976-06-18
IPC分类号： C07C69/007 , A61K31/065 , A61K31/085 , A61K31/215 , A61K31/22 , A61P3/06 , A61P7/02 , A61P25/04 , A61P29/00 , C07C27/00 , C07C29/42 , C07C33/28 , C07C33/48 , C07C41/00 , C07C43/295 , C07C67/00 , C07C69/145 , C07F1/00 , C07C43/20
CPC分类号： C07C29/42 , C07C69/157 , C07C69/63 , C07F1/005
摘要： Alkyne compounds of the formula ##STR1## wherein R.sup.1 is H, alkyl of up to 4 carbon atoms or phenyl; R.sup.2 is H, aliphatic acyl of up to 6 carbon atoms or aroyl of up to 11 carbon atoms; R.sup.3 and R.sup.4 are H, F, Cl or Br and n is 0 or 1, and physiologicaly acceptable metals salts thereof, have antiinflammatory activity. These compounds can be made from compounds of the formula ##STR2## wherein Q is a functionally-modified hydroxy and R.sup.1, R.sup.3, R.sup.4 and n are as above by treatment with a solvolyzing agent.
摘要翻译： 其中R 1为H，至多4个碳原子的烷基或苯基的式IMA的炔烃化合物; R2是H，最多6个碳原子的脂族酰基或至多11个碳原子的芳酰基; R3和R4是H，F，Cl或Br，n是0或1，并且其生理上可接受的金属盐具有抗炎活性。 这些化合物可以由下式化合物制备：其中Q是官能改性的羟基，R 1，R 3，R 4和n如上所述，用溶剂分解剂处理。
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公开(公告)号：US4239759A
公开(公告)日：1980-12-16
申请号：US895417
申请日：1978-04-11
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 , C07D295/06 , A61K31/535
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 a 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 trigylyceride level lowering activities.
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公开(公告)号：US4196215A
公开(公告)日：1980-04-01
申请号：US920084
申请日：1978-06-28
IPC分类号： C07C29/09 , C07C29/42 , C07C29/68 , C07C33/28 , C07C33/48 , C07C43/295 , C07F1/00 , A61K31/22 , A61K31/235 , C07C69/02 , C07C69/78
CPC分类号： C07C29/68 , C07C29/09 , C07C29/42 , C07C33/28 , C07C33/486 , C07C43/295 , C07C69/157 , C07C69/63 , C07C69/78 , C07F1/005
摘要： Alkyne compounds of the formula ##STR1## wherein R.sup.1 is H, alkyl of up to 4 carbon atoms or phenyl; R.sup.2 is H, aliphatic acyl of up to 6 carbon atoms or aroyl of up to 11 carbon atoms; R.sup.3 and R.sup.4 are H, F, Cl or Br and n is 0 or 1, and physiologically acceptable metals salts thereof, have anti-inflammatory activity. These compounds can be made from compounds of the formula ##STR2## wherein Q is a functionally-modified hydroxy and R.sup.1, R.sup.3, R.sup.4 and n are as above by treatment with a solvolyzing agent.
摘要翻译： 其中R 1为H，至多4个碳原子的烷基或苯基的式IMA的炔烃化合物; R2是H，最多6个碳原子的脂族酰基或至多11个碳原子的芳酰基; R3和R4是H，F，Cl或Br，n是0或1，并且其生理学上可接受的金属盐具有抗炎活性。 这些化合物可以由下式化合物制备：其中Q是官能改性的羟基，R 1，R 3，R 4和n如上所述，用溶剂分解剂处理。
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公开(公告)号：US4151302A
公开(公告)日：1979-04-24
申请号：US826101
申请日：1977-08-19
IPC分类号： C07C43/295 , C07C57/60 , C07C59/56 , C07C59/68 , C07F1/00 , C07F9/40 , A61K31/19 , A61K31/235 , C07C65/02 , C07C101/72
CPC分类号： C07C43/295 , C07C57/60 , 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## 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，其是可以从式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：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：US4125622A
公开(公告)日：1978-11-14
申请号：US860355
申请日：1977-12-14
IPC分类号： A61K31/39 , A61P7/02 , C07D327/06
CPC分类号： C07D327/06 , Y10S514/822
摘要： 1,4-Oxathianes of the formula ##STR1## and the physiologically-acceptable salts thereof wherein R.sup.1 is H or alkyl with 1-4 C-atoms; R.sup.2 is H or alkyl with 1-4 C-atoms; R.sup.3 is H, alkyl with 1-8 C-atoms, phenyl or phenyl substituted by F, Cl, Br, OH, OCH.sub.3, CF.sub.3 or NO.sub.2 ; R.sup.4 is H or CH.sub.3 ; B is a single bond, --CH.sub.2 --, --CH.sub.2 CH.sub.2 -- or --CH.sub.2 O--; and a wavy line ( ) indicates that these bonds can be in the .alpha.- or .beta.- positions possess thrombocyte inhibition properties.
摘要翻译： 具有式“IMAGE”的1,4-氧硫辛酸和其生理学上可接受的盐，其中R 1是H或具有1-4个C原子的烷基; R2是H或具有1-4个C原子的烷基; R3是H，具有1-8个C原子的烷基，被F，Cl，Br，OH，OCH3，CF3或NO2取代的苯基或苯基; R4是H或CH3; B是单键，-CH 2 - ， - CH 2 CH 2 - 或-CH 2 O- 和波浪线（）表示这些键可以在α或β位具有血细胞抑制性质。
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