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1. 发明授权

US4151294A Alkynols and process for their preparation 失效
标题翻译：炔醇及其制备方法
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。

2. 发明授权

US4239759A Morpholino containing compounds, compositions and use thereof 失效
标题翻译：含吗啉代的化合物，组合物及其用途
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.

3. 发明授权

US4110447A Anti-inflammatory (halo-4-biphenylyl)-alkanolamines 失效
标题翻译：抗炎药（HOLO-4-BIPHENYLYL） - 甘露醇
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。

4. 发明授权

US4115456A Alkyne compounds and method of use 失效
标题翻译：炔烃化合物及其使用方法
公开(公告)号：US4115456A
公开(公告)日：1978-09-19
申请号：US697579
申请日：1976-06-18
申请人： Joachim Gante , Hans-Adolf Kurmeier , Dieter Orth , Erich Schacht , Albrecht Wild
发明人： Joachim Gante , Hans-Adolf Kurmeier , Dieter Orth , Erich Schacht , Albrecht Wild
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。

5. 发明授权

US4196215A Alkyne compounds and method of use 失效
标题翻译：炔烃化合物及其使用方法
公开(公告)号：US4196215A
公开(公告)日：1980-04-01
申请号：US920084
申请日：1978-06-28
申请人： Joachim Gante , Hans-Adolf Kurmeier , Dieter Orth , Erich Schacht , Albrecht Wild
发明人： Joachim Gante , Hans-Adolf Kurmeier , Dieter Orth , Erich Schacht , Albrecht Wild
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。

6. 发明授权

US4151302A Araliphatic dihalogen compounds composition and method of use 失效
标题翻译：脂肪族二卤化合物的组成及使用方法
公开(公告)号：US4151302A
公开(公告)日：1979-04-24
申请号：US826101
申请日：1977-08-19
申请人： Joachim Gante , Hans-Adolf Kurmeier , Dieter Orth , Erich Schacht , Albrecht Wild
发明人： Joachim Gante , Hans-Adolf Kurmeier , Dieter Orth , Erich Schacht , Albrecht Wild
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。

7. 发明授权

US4060633A Phenylalkanol nitriles 失效
标题翻译：苯基链烷醇腈
公开(公告)号：US4060633A
公开(公告)日：1977-11-29
申请号：US681175
申请日：1976-04-28
申请人： Joachim Gante , Hans-Adolf Kurmeier , Dieter Orth , Erich Schacht , Albrecht Wild
发明人： Joachim Gante , Hans-Adolf Kurmeier , Dieter Orth , Erich Schacht , Albrecht Wild
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。

8. 发明授权

US4057647A Araliphatic dihalogen compounds and process for their preparation 失效
标题翻译：脂肪族二卤化合物及其制备方法
公开(公告)号：US4057647A
公开(公告)日：1977-11-08
申请号：US695804
申请日：1976-06-14
申请人： Joachim Gante , Hans-Adolf Kurmeier , Dieter Orth , Erich Schacht , Albrecht Wild
发明人： Joachim Gante , Hans-Adolf Kurmeier , Dieter Orth , Erich Schacht , Albrecht Wild
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。

9. 发明授权

US4136200A Phenylbutanol derivatives, processes for their preparation and compositions containing them 失效
标题翻译：苯乙醇衍生物及其制备方法及其组合物
公开(公告)号：US4136200A
公开(公告)日：1979-01-23
申请号：US810712
申请日：1977-06-28
申请人： Erich Schacht , Werner Mehrhof , Albrecht Wild , Joachim Gante , Hans-Adolf Kurmeier
发明人： Erich Schacht , Werner Mehrhof , Albrecht Wild , Joachim Gante , Hans-Adolf Kurmeier
IPC分类号： C07C43/295 , C07C59/48 , C07C59/68 , C07C43/20
CPC分类号： C07C59/68 , C07C43/295 , C07C59/48
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 1-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.

10. 发明授权

US4049823A Phenylbutanol derivatives and compositions containing them 失效
标题翻译：苯基丁醇衍生物和含有它们的组合物
公开(公告)号：US4049823A
公开(公告)日：1977-09-20
申请号：US552959
申请日：1975-02-25
申请人： Erich Schacht , Werner Mehrhof , Albrecht Wild , Joachim Gante , Hans-Adolf Kurmeier
发明人： Erich Schacht , Werner Mehrhof , Albrecht Wild , Joachim Gante , Hans-Adolf Kurmeier
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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