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1. 发明授权

US4237133A 1,9-Dihydroxyoctahydrophenanthrenes 失效
标题翻译： 1,9-二羟基焦氢氯苯
公开(公告)号：US4237133A
公开(公告)日：1980-12-02
申请号：US78473
申请日：1979-09-24
申请人： Thomas H. Althuis , Charles A. Harbert , Michael R. Johnson , Lawrence S. Melvin, Jr.
发明人： Thomas H. Althuis , Charles A. Harbert , Michael R. Johnson , Lawrence S. Melvin, Jr.
IPC分类号： C07C41/22 , C07C41/26 , C07C43/225 , C07C43/23 , C07C45/45 , C07C45/46 , C07C45/54 , C07C45/61 , C07C45/67 , C07C45/68 , C07C45/71 , C07C45/72 , C07C45/73 , C07C49/747 , C07C49/755 , C07C49/757 , C07C49/83 , C07D211/32 , C07D213/30 , C07D213/50 , C07D317/22 , C07D317/72 , C07D295/14 , A61K31/22 , A61K31/535 , C07C101/19
CPC分类号： C07D213/30 , C07C41/01 , C07C41/22 , C07C41/26 , C07C45/45 , C07C45/46 , C07C45/54 , C07C45/61 , C07C45/67 , C07C45/68 , C07C45/71 , C07C45/72 , C07C45/73 , C07C49/747 , C07C49/755 , C07C49/757 , C07C49/83 , C07D211/32 , C07D213/50 , C07D317/22 , C07D317/72 , C07C2101/14 , C07C2103/26
摘要： Compounds of the formula ##STR1## wherein R.sub.1 is hydrogen, benzyl, benzoyl, alkanoyl of 1 to 5 carbon atoms or --CO--(CH.sub.2).sub.p --NR'R" wherein p is 0 or an integer from 1 to 4; each of R' and R" when taken individually is hydrogen or alkyl of 1 to 4 carbon atoms; R' and R" when taken together with the nitrogen to which they are attached form a 5- or 6-membered heterocyclic ring selected from piperidino, pyrollo, pyrrolidino, morpholino and N-alkylpiperazino having from 1 to 4 carbon atoms in the alkyl group;R.sub.2 is selected from hydrogen, alkanoyl of 1 to 6 carbon atoms and benzoyl;R.sub.3 is selected from hydrogen, methyl and ethyl;R.sub.4 is selected from hydrogen, alkyl of 1 to 6 carbon atoms and benzyl;Z is selected from:(a) alkylene having from one to nine carbon atoms;(b) --(alk.sub.1).sub.m --X--(alk.sub.2).sub.n -- wherein each of (alk.sub.1) and (alk.sub.2)is alkylene having from 1 to 9 carbon atoms, with the proviso that the summation of carbon atoms in (alk.sub.1) plus (alk.sub.2) is not greater than 9;m and n are each 0 or 1;X is selected from O, S, SO and SO.sub.2 ; andW is selected from hydrogen, methyl, pyridyl, piperidyl, phenyl, monochlorophenyl, monofluorophenyl and ##STR2## wherein W.sub.1 is selected from hydrogen, phenyl, monochlorophenyl and monofluorophenyl; a is an integer from 1 to 5 and b is 0 or an integer from 1 to 4, with the proviso that the sum of a and b is not greater than 5.Compounds I and II are useful as analgesics. Compound III is useful as an intermediate for the preparation of Compounds I and II. Intermediates for the preparation of I, II and III are disclosed. A process for the use of compounds I and II to produce analgesia is also described.
摘要翻译：其中R1是氢，苄基，苯甲酰基，1至5个碳原子的烷酰基或-CO-（CH2）p-NR'R“，其中p是0或 1到4的整数; 当单独使用时，R'和R“各自为氢或1至4个碳原子的烷基; 当与它们所连接的氮一起取代时，R'和R“与烷基中具有1至4个碳原子的5-或6-元杂环选自哌啶子基，吡咯烷基，吡咯烷子基，吗啉代和N-烷基哌嗪基组; R 2选自氢，1至6个碳原子的烷酰基和苯甲酰基; R3选自氢，甲基和乙基; R4选自氢，1至6个碳原子的烷基和苄基; Z选自：（a）具有1至9个碳原子的亚烷基; （b） - （alk1）mX-（alk2）n-其中（alk1）和（alk2）各自为具有1至9个碳原子的亚烷基，条件是（alk1）加（alk2））不大于9; m和n分别为0或1; X选自O，S，SO和SO2; W选自氢，甲基，吡啶基，哌啶基，苯基，一氯苯基，一氟苯基和其中W1选自氢，苯基，一氯苯基和单氟苯基; a为1至5的整数，b为0或1至4的整数，条件是a和b之和不大于5.化合物I和II可用作止痛剂。化合物III可用作制备化合物I和II的中间体。公开了制备I，II和III的中间体。还描述了使用化合物I和II产生止痛的方法。

2. 发明授权

US4134981A Pyrimidal [2,3,d]Pyrimidin-4(3H)-ones as antiallergy agents 失效
标题翻译： PYRIMIDAL（2,3，D）PYRIMIDIN-4（3H） - 作为抗菌剂
公开(公告)号：US4134981A
公开(公告)日：1979-01-16
申请号：US845816
申请日：1977-10-27
申请人： Thomas H. Althuis , Leonard J. Czuba , Hans-Jurgen E. Hess , Saul B. Kadin
发明人： Thomas H. Althuis , Leonard J. Czuba , Hans-Jurgen E. Hess , Saul B. Kadin
IPC分类号： C07D215/54 , C07D265/26 , A61K31/435 , C07D471/04
CPC分类号： C07D215/54 , C07D265/26
摘要： Fused heterocyclic ring systems in which a quinoline or a pyridine component is "fused" to a pyrimidine having a 2-methyl, 2-ethyl, or 2-acetyl group and a 4-keto group, and to similar ring systems in which a quinoline, a naphthalene or a pyridine component is "fused" to a pyrimidine having a 2-carboxy group and a 4-keto group, derivatives, and pharmaceutically-acceptable cationic salts thereof, and their use as antiallergy agents, and intermediates therefor.

3. 发明授权

US4387229A 3-[2-Hydroxy-4-(substituted)phenyl]azacycloalkanols and derivatives thereof 失效
标题翻译： 3- [2-羟基-4-（取代的）苯基]氮杂环烷醇及其衍生物
公开(公告)号：US4387229A
公开(公告)日：1983-06-07
申请号：US353113
申请日：1982-02-26
申请人： Thomas H. Althuis , Charles A. Harbert , Michael R. Johnson , Lawrence S. Melvin, Jr.
发明人： Thomas H. Althuis , Charles A. Harbert , Michael R. Johnson , Lawrence S. Melvin, Jr.
IPC分类号： C07D211/22 , C07D211/42 , C07D211/44 , C07D211/46 , C07D211/48 , C07D211/70 , C07D211/74 , C07F9/59 , C07D207/12 , C07D223/02 , C07D225/00
CPC分类号： C07D211/42 , C07D211/22 , C07D211/44 , C07D211/46 , C07D211/48 , C07D211/70 , C07D211/74 , C07F9/592
摘要： Azacycloalkanes, and derivatives thereof, including unsaturated analogs, each of which has at the 3-position a 2-hydroxy-4-substituted phenyl group wherein the 4-position substituent is alkyl which can have an oxygen atom as part of the chain, or aralkyl which can have an oxygen atom as part of the alkyl chain, their use for pharmacological and medicinal purposes, intermediates therefor and processes for their preparation.
摘要翻译：氮杂环烷烃及其衍生物，包括不饱和类似物，其各自在3-位上具有2-羟基-4-取代的苯基，其中4-位取代基是可以具有氧原子作为链的一部分的烷基，或可以具有氧原子作为烷基链的一部分的芳烷基，其用于药理和药用目的，其中间体及其制备方法。

4. 发明授权

US4188495A 1,9-Dihydroxyoctahydrophenanthrenes and intermediates therefor 失效
标题翻译： 1,9-二羟基八氢菲和其中间体
公开(公告)号：US4188495A
公开(公告)日：1980-02-12
申请号：US851503
申请日：1977-11-14
申请人： Thomas H. Althuis , Charles A. Harbert , Michael R. Johnson , Lawrence S. Melvin, Jr.
发明人： Thomas H. Althuis , Charles A. Harbert , Michael R. Johnson , Lawrence S. Melvin, Jr.
IPC分类号： C07C69/017 , A61K31/045 , A61K31/075 , A61K31/12 , A61K31/13 , A61K31/215 , A61K31/395 , A61P1/00 , A61P7/10 , A61P9/12 , A61P25/04 , A61P25/20 , A61P37/06 , C07C35/42 , C07C41/00 , C07C41/22 , C07C41/26 , C07C43/178 , C07C43/196 , C07C43/20 , C07C43/225 , C07C43/23 , C07C45/00 , C07C45/45 , C07C45/46 , C07C45/54 , C07C45/59 , C07C45/61 , C07C45/67 , C07C45/68 , C07C45/71 , C07C45/73 , C07C49/417 , C07C49/587 , C07C49/643 , C07C49/733 , C07C49/737 , C07C49/747 , C07C49/755 , C07C49/757 , C07C49/82 , C07C49/83 , C07C67/00 , C07C69/013 , C07C229/06 , C07C313/00 , C07C317/00 , C07C317/18 , C07C317/22 , C07C323/20 , C07C323/22 , C07D211/00 , C07D211/22 , C07D211/32 , C07D213/00 , C07D213/30 , C07D213/50 , C07D317/22 , C07D317/72 , A61K31/085
CPC分类号： C07D213/30 , C07C255/00 , C07C323/00 , C07C41/01 , C07C41/22 , C07C41/26 , C07C45/45 , C07C45/46 , C07C45/54 , C07C45/59 , C07C45/61 , C07C45/67 , C07C45/673 , C07C45/68 , C07C45/71 , C07C45/73 , C07C49/747 , C07C49/755 , C07C49/757 , C07C49/83 , C07D211/32 , C07D213/50 , C07D317/22 , C07D317/72 , C07C2101/14 , C07C2103/26
摘要： Compounds of the formula ##STR1## wherein R.sub.1 is hydrogen, benzyl, benzoyl, alkanoyl of 1 to 5 carbon atoms or --CO--(CH.sub.2).sub.p --NR'R" wherein p is 0 or an integer from 1 to 4; each of R' and R" when taken individually is hydrogen or alkyl of 1 to 4 carbon atoms; R' and R" when taken together with the nitrogen to which they are attached form a 5- or 6-membered heterocyclic ring selected from piperidino, pyrollo, pyrrolidino, morpholino and N-alkylpiperazino having from 1 to 4 carbon atoms in the alkyl group;R.sub.2 is selected from hydrogen, alkanoyl of 1 to 6 carbon atoms and benzoyl;R.sub.3 is selected from hydrogen, methyl and ethyl;R.sub.4 is selected from hydrogen, alkyl of 1 to 6 carbon atoms and benzyl;Z is selected from:(a) alkylene having from one to nine carbon atoms;(b) --(alk.sub.1).sub.m --X--(alk.sub.2).sub.n -- wherein each of (alk.sub.1) and (alk.sub.2) is alkylene having from 1 to 9 carbon atoms, with the proviso that the summation of carbon atoms in (alk.sub.1) plus (alk.sub.2) is not greater than 9;m and n are each 0 or 1;X is selected from O, S, SO, and SO.sub.2 ; andW is selected from hydrogen, methyl, pyridyl, piperidyl, phenyl, monochlorophenyl, monofluorophenyl and ##STR2## wherein W.sub.1 is selected from hydrogen, phenyl, monochlorophenyl and monofluorophenyl; a is an integer from 1 to 5 and b is 0 or an integer from 1 to 4, with the proviso that the sum of a and b is not greater than 5.Compounds I and II are useful as analgesics. Compound III is useful as an intermediate for the preparation of Compounds I and II. Intermediates for the preparation of I, II and III are disclosed. A process for the use of compounds I and II to produce analgesia is also described.
摘要翻译：其中R 1为氢，苄基，苯甲酰基，1至5个碳原子的烷酰基或-CO-（CH 2）p -NR'R“，其中p为0或1至 4; 当单独使用时，R'和R“各自为氢或1至4个碳原子的烷基; 当与它们所连接的氮一起取代时，R'和R“与烷基中具有1至4个碳原子的5-或6-元杂环选自哌啶子基，吡咯烷基，吡咯烷子基，吗啉代和N-烷基哌嗪基组; R 2选自氢，1至6个碳原子的烷酰基和苯甲酰基; R3选自氢，甲基和乙基; R4选自氢，1至6个碳原子的烷基和苄基; Z选自：（a）具有1至9个碳原子的亚烷基; （b） - （alk1）mX-（alk2）n-其中（alk1）和（alk2）各自为具有1至9个碳原子的亚烷基，条件是（alk1）加（alk2））不大于9; m和n分别为0或1; X选自O，S，SO和SO2; W选自氢，甲基，吡啶基，哌啶基，苯基，一氯苯基，一氟苯基和其中W1选自氢，苯基，一氯苯基和单氟苯基; a为1至5的整数，b为0或1至4的整数，条件是a和b之和不大于5.化合物I和II可用作止痛剂。化合物III可用作制备化合物I和II的中间体。公开了制备I，II和III的中间体。还描述了使用化合物I和II产生止痛的方法。

5. 发明授权

US4120962A Fused pyrimidin-4(3H)-ones as antiallergy agents 失效
标题翻译：融合的嘧啶-4（3H） - 酮作为抗过敏剂
公开(公告)号：US4120962A
公开(公告)日：1978-10-17
申请号：US786185
申请日：1977-04-11
申请人： Thomas H. Althuis , Leonard J. Czuba , Hans-Jurgen E. Hess , Saul B. Kadin
发明人： Thomas H. Althuis , Leonard J. Czuba , Hans-Jurgen E. Hess , Saul B. Kadin
IPC分类号： C07D215/54 , C07D265/26 , C07D239/90 , A61K31/505
CPC分类号： C07D215/54 , C07D265/26
摘要： Fused heterocyclic ring systems in which a quinoline or a pyridine component is "fused" to a pyrimidine having a 2-methyl, 2-ethyl, or 2-acetyl group and a 4-keto group, and to similar ring systems in which a quinoline, a naphthalene or a pyridine component is "fused" to a pyrimidine having a 2-carboxy group and a 4-keto group, derivatives, and pharmaceutically-acceptable cationic salts thereof, and their use as antiallergy agents, and intermediates therefor.
摘要翻译：其中喹啉或吡啶组分与具有2-甲基，2-乙基或2-乙酰基和4-酮基的嘧啶“稠合”的稠合杂环体系，以及类似的环体系，其中喹啉萘或吡啶成分与具有2-羧基和4-酮基的嘧啶基，衍生物和药学上可接受的阳离子盐“融合”，以及它们作为抗过敏剂及其中间体的用途。

6. 发明授权

US4310529A Intermediates to 1,9-dihydroxyoctahydrophenanthrenes 失效
标题翻译：中间体至1,9-二羟基焦合氢离子
公开(公告)号：US4310529A
公开(公告)日：1982-01-12
申请号：US218712
申请日：1980-12-22
申请人： Thomas H. Althuis , Charles A. Harbert , Michael R. Johnson , Lawrence S. Melvin, Jr.
发明人： Thomas H. Althuis , Charles A. Harbert , Michael R. Johnson , Lawrence S. Melvin, Jr.
IPC分类号： C07C41/22 , C07C41/26 , C07C43/225 , C07C43/23 , C07C45/45 , C07C45/54 , C07C45/61 , C07C45/67 , C07C45/68 , C07C45/71 , C07C45/73 , C07C49/747 , C07C49/755 , C07D211/32 , C07D213/30 , C07D213/50 , C07D317/22 , C07D317/72 , A61K31/44 , A61K31/445 , C07D213/55
CPC分类号： C07D213/30 , C07C41/01 , C07C41/22 , C07C41/26 , C07C45/45 , C07C45/54 , C07C45/61 , C07C45/67 , C07C45/68 , C07C45/71 , C07C45/73 , C07C49/747 , C07C49/755 , C07D211/32 , C07D213/50 , C07D317/22 , C07D317/72 , C07C2101/14
摘要： Compounds of the formula ##STR1## wherein R.sub.1 is hydrogen, benzyl, benzoyl, alkanoyl of 1 to 5 carbon atoms or --CO--(CH.sub.2).sub.p --NR'R" wherein p is 0 or an integer from 1 to 4; each of R' and R" when taken individually is hydrogen or alkyl of 1 to 4 carbon atoms; R' and R" when taken together with the nitrogen to which they are attached form a 5- or 6-membered heterocyclic ring selected from piperidino, pyrrolo, pyrrolidino, morpholino and N-alkylpiperazino having from 1 to 4 carbon atoms in the alkyl group;R.sub.2 is selected from hydrogen, alkanoyl of 1 to 6 carbon atoms and benzoyl;R.sub.3 is selected from hydrogen, methyl and ethyl;R.sub.4 is selected from hydrogen, alkyl of 1 to 6 carbon atoms and benzyl;Z is selected from:(a) alkylene having from one to nine carbon atoms;(b) --(alk.sub.1).sub.m --X--(alk.sub.2).sub.n --wherein each of (alk.sub.1) and (alk.sub.2) is alkylene having from 1 to 9 carbon atoms, with the proviso that the summation of carbon atoms in (alk.sub.1) plus (alk.sub.2) is not greater than 9;m and n are each 0 or 1;X is selected from O, S, SO and SO.sub.2 ; andW is selected from hydrogen, methyl, pyridyl, piperidyl, phenyl, monochlorophenyl, monofluorophenyl and ##STR2## wherein W.sub.1 is selected from hydrogen, phenyl, monochlorophenyl and monofluorophenyl; a is an integer from 1 to 5 and b is 0 or an integer from 1 to 4, with the proviso that the sum of a and b is not greater than 5.Compounds I and II are useful as analgesics. Compound III is useful as an intermediate for the preparation of Compounds I and II. Intermediates for the preparation of I, II and III are disclosed. A process for the use of compounds I and II to produce analgesia is also described.
摘要翻译：其中R 1为氢，苄基，苯甲酰基，1至5个碳原子的烷酰基或-CO-（CH 2）p -NR'R“，其中p为0 或1到4的整数; 当单独使用时，R'和R“各自为氢或1至4个碳原子的烷基; 当与它们所连接的氮一起取代时，R'和R“与烷基中具有1至4个碳原子的5-或6-元杂环选自哌啶子基，吡咯烷基，吡咯烷子基，吗啉代和N-烷基哌嗪基组; R 2选自氢，1至6个碳原子的烷酰基和苯甲酰基; R3选自氢，甲基和乙基; R4选自氢，1至6个碳原子的烷基和苄基; Z选自：（a）具有1至9个碳原子的亚烷基; （b） - （alk1）mX-（alk2）n - 其中（alk1）和（alk2）各自为具有1至9个碳原子的亚烷基，条件是（alk1）加（alk2））不大于9; m和n分别为0或1; X选自O，S，SO和SO2; W选自氢，甲基，吡啶基，哌啶基，苯基，一氯苯基，一氟苯基和其中W1选自氢，苯基，一氯苯基和单氟苯基; a为1至5的整数，b为0或1至4的整数，条件是a和b之和不大于5.化合物I和II可用作止痛剂。化合物III可用作制备化合物I和II的中间体。公开了制备I，II和III的中间体。还描述了使用化合物I和II产生止痛的方法。

7. 发明授权

US4268523A 1,9-Dihydroxyoctahydrophenanthrenes and intermediates therefor 失效
标题翻译： 1,9-二羟基八氢菲和其中间体
公开(公告)号：US4268523A
公开(公告)日：1981-05-19
申请号：US78476
申请日：1979-09-24
申请人： Thomas H. Althuis , Charles A. Harbert , Michael R. Johnson , Lawrence S. Melvin, Jr.
发明人： Thomas H. Althuis , Charles A. Harbert , Michael R. Johnson , Lawrence S. Melvin, Jr.
IPC分类号： C07C41/22 , C07C41/26 , C07C43/225 , C07C43/23 , C07C45/45 , C07C45/46 , C07C45/54 , C07C45/61 , C07C45/67 , C07C45/68 , C07C45/71 , C07C45/73 , C07C49/747 , C07C49/755 , C07C49/83 , C07D211/32 , C07D213/30 , C07D213/50 , C07D317/22 , C07D317/72 , A01N35/00 , C07C49/788
CPC分类号： C07D213/30 , C07C41/01 , C07C41/22 , C07C41/26 , C07C45/45 , C07C45/46 , C07C45/54 , C07C45/61 , C07C45/67 , C07C45/68 , C07C45/71 , C07C45/73 , C07C49/747 , C07C49/755 , C07C49/83 , C07D211/32 , C07D213/50 , C07D317/22 , C07D317/72 , C07C2101/14 , C07C2103/26
摘要： Compounds of the formula ##STR1## wherein R.sub.1 is hydrogen, benzyl, benzoyl, alkanoyl of 1 to 5 carbon atoms or --CO--(CH.sub.2).sub.p --NR'R" wherein p is 0 or an integer from 1 to 4; each of R' and R" when taken individually is hydrogen or alkyl of 1 to 4 carbon atoms; R' and R" when taken together with the nitrogen to which they are attached form a 5- or 6-membered heterocyclic ring selected from piperidino, pyrollo, pyrrolidino, morpholino and N-alkylpiperazino having from 1 to 4 carbon atoms in the alkyl group;R.sub.2 is selected from hydrogen, alkanoyl of 1 to 6 carbon atoms and benzoyl;R.sub.3 is selected from hydrogen, methyl and ethyl;R.sub.4 is selected from hydrogen, alkyl of 1 to 6 carbon atoms and benzyl;Z is selected from:(a) alkylene having from one to nine carbon atoms;(b) -(alk.sub.1).sub.m -X-(alk.sub.2).sub.n - wherein each of (alk.sub.1) and (alk.sub.2) is alkylene having from 1 to 9 carbon atoms, with the proviso that the summation of carbon atoms in (alk.sub.1) plus (alk.sub.2) is not greater than 9;m and n are each 0 or 1;X is selected from O, S, SO and SO.sub.2 ; andW is selected from hydrogen, methyl, pyridyl, piperidyl, phenyl, monochlorophenyl, monofluorophenyl and ##STR2## wherein W.sub.1 is selected from hydrogen, phenyl, monochlorophenyl and monofluorophenyl; a is an integer from 1 to 5 and b is 0 or an integer from 1 to 4, with the proviso that the sum of a and b is not greater than 5.Compounds I and II are useful as analgesics. Compound III is useful as an intermediate for the preparation of Compounds I and II. Intermediates for the preparation of I, II and III are disclosed. A process for the use of compounds I and II to produce analgesia is also described.
摘要翻译：其中R1是氢，苄基，苯甲酰基，1至5个碳原子的烷酰基或-CO-（CH2）p-NR'R“，其中p是0或 1到4的整数; 当单独使用时，R'和R“各自为氢或1至4个碳原子的烷基; 当与它们所连接的氮一起取代时，R'和R“与烷基中具有1至4个碳原子的5-或6-元杂环选自哌啶子基，吡咯烷基，吡咯烷子基，吗啉代和N-烷基哌嗪基组; R 2选自氢，1至6个碳原子的烷酰基和苯甲酰基; R3选自氢，甲基和乙基; R4选自氢，1至6个碳原子的烷基和苄基; Z选自：（a）具有1至9个碳原子的亚烷基; （b） - （alk1）mX-（alk2）n-其中（alk1）和（alk2）各自为具有1至9个碳原子的亚烷基，条件是（alk1）加（alk2））不大于9; m和n分别为0或1; X选自O，S，SO和SO2; W选自氢，甲基，吡啶基，哌啶基，苯基，一氯苯基，一氟苯基和其中W1选自氢，苯基，一氯苯基和单氟苯基; a为1至5的整数，b为0或1至4的整数，条件是a和b之和不大于5.化合物I和II可用作止痛剂。化合物III可用作制备化合物I和II的中间体。公开了制备I，II和III的中间体。还描述了使用化合物I和II产生止痛的方法。

8. 发明授权

US4044134A Fused pyrimidin-4(3H)-ones as antiallergy agents 失效
标题翻译：融合的嘧啶-4（3H） - 酮作为抗过敏剂
公开(公告)号：US4044134A
公开(公告)日：1977-08-23
申请号：US667515
申请日：1976-03-16
申请人： Thomas H. Althuis , Leonard J. Czuba , Hans-Jurgen E. Hess , Saul B. Kadin
发明人： Thomas H. Althuis , Leonard J. Czuba , Hans-Jurgen E. Hess , Saul B. Kadin
IPC分类号： C07D215/54 , C07D265/26 , C07D471/04 , A61K31/505
CPC分类号： C07D471/04 , C07D215/54 , C07D265/26
摘要： Fused heterocyclic ring systems in which a quinoline or a pyridine component is "fused" to a pyrimidine having a 2-methyl, 2-ethyl, or 2-acetyl group and a 4-keto group, and to similar ring systems in which a quinoline, a naphthalene or a pyridine component is fused to a pyrimidine having a 2-carboxy group and a 4-keto group, derivatives, and pharmaceutically-acceptable cationic salts thereof, and their use as antiallergy agents, and intermediates therefor.
摘要翻译：其中喹啉或吡啶组分与具有2-甲基，2-乙基或2-乙酰基和4-酮基的嘧啶“稠合”的稠合杂环体系，以及类似的环体系，其中喹啉，萘或吡啶成分与具有2-羧基和4-酮基的嘧啶，其衍生物和药学上可接受的阳离子盐，以及它们作为抗过敏剂及其中间体的用途融合。

9. 发明授权

US4011324A Esters and amides of pyrimido[4,5-b]quinolin-4(3H)-one-2-carboxylic acids as antiulcer agents 失效
标题翻译：吡啶二酮（4,5-B）喹啉-4（3H） - 酮-2-羧酸作为抗菌剂的酯和氨基
公开(公告)号：US4011324A
公开(公告)日：1977-03-08
申请号：US650714
申请日：1976-01-20
申请人： Thomas H. Althuis
发明人： Thomas H. Althuis
IPC分类号： A61K31/505 , A61P1/04 , C07D213/64 , C07D471/04 , C07D491/147
CPC分类号： C07D213/64 , C07D471/04
摘要： A series of alkyl ester and amide derivatives of pyrimido[4,5-b]quinolin-4(3H)-one-2-carboxylic acids, salts thereof and their preparation and use as antiulcer agents.

10. 发明授权

US4332942A 3-(2-Hydroxy-4-(substituted)phenyl)azacycloalkanes as analgesics 失效
标题翻译： 3-（2-羟基-4-（取代的）苯基）氮杂环烷烷作止痛剂
公开(公告)号：US4332942A
公开(公告)日：1982-06-01
申请号：US198742
申请日：1980-10-20
申请人： Thomas H. Althuis , Charles A. Harbert , Michael R. Johnson , Lawrence S. Melvin, Jr.
发明人： Thomas H. Althuis , Charles A. Harbert , Michael R. Johnson , Lawrence S. Melvin, Jr.
IPC分类号： C07D211/22 , C07D211/42 , C07D211/44 , C07D211/46 , C07D211/48 , C07D211/70 , C07D211/74 , C07D211/34
CPC分类号： C07D211/46 , C07D211/22 , C07D211/42 , C07D211/44 , C07D211/48 , C07D211/70 , C07D211/74
摘要： Azacycloalkanes, and derivatives thereof, including unsaturated analogs, each of which has at the 3-position a 2-hydroxy-4-substituted phenyl group wherein the 4-position substituent is alkyl which can have an oxygen atom as part of the chain, or aralkyl which can have an oxygen atom as part of the alkyl chain, their use for pharmacological and medicinal purposes, intermediates therefor and processes for their preparation.
摘要翻译：氮杂环烷烃及其衍生物，包括不饱和类似物，其各自在3-位上具有2-羟基-4-取代的苯基，其中4-位取代基是可以具有氧原子作为链的一部分的烷基，或可以具有氧原子作为烷基链的一部分的芳烷基，其用于药理和药用目的，其中间体及其制备方法。

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