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1. 发明授权

US4800211A 5-methylthio-3-hydroxybenzo [b]thiophene-2-carboxamide derivatives as cyclooxygenase and lipoxygenase inhibitors 失效
标题翻译： 5-甲硫基-3-羟基苯并[b]噻吩-2-甲酰胺衍生物作为环加氧酶和脂氧合酶抑制剂
公开(公告)号：US4800211A
公开(公告)日：1989-01-24
申请号：US897576
申请日：1986-08-18
申请人： Allan N. Tischler , Philippe L. Durette , Bruce E. Witzel , Thomas J. Lanza, Jr.
发明人： Allan N. Tischler , Philippe L. Durette , Bruce E. Witzel , Thomas J. Lanza, Jr.
IPC分类号： C07D333/70 , A61K31/38
CPC分类号： C07D333/70
摘要： 3-Hydroxybenzo[b]thiophene-2-carboxamide derivatives have been prepared by:(1) treating a substituted 2-halobenzoate with a thioacetamide.(2) treating a substituted thiosalicylate with an appropriately substituted haloacetamide; and(3) further synthetic modification of compounds prepared above.These compounds have been found to be effective inhibitors of both cyclooxygenase and lipoxygenase and thereby useful in the treatment of pain, fever, inflammation, arthritic conditions, asthma, allergic disorders, skin diseases, cardiovascular disorders, psoriasis, inflammatory bowel disease, glaucoma or other prostaglandins and/or leukotriene mediated diseases.
摘要翻译：通过以下方法制备了3-羟基苯并[b]噻吩-2-甲酰胺衍生物：（1）用硫代乙酰胺处理取代的2-卤代苯甲酸酯。（2）用适当取代的卤代乙酰胺处理取代的硫代水杨酸酯; 和（3）进一步合成上述制备的化合物。已经发现这些化合物是环加氧酶和脂氧合酶的有效抑制剂，从而可用于治疗疼痛，发热，炎症，关节炎状况，哮喘，过敏性疾病，皮肤疾病，心血管疾病，牛皮癣，炎性肠病，青光眼或其他前列腺素和/或白三烯介导的疾病。

2. 发明授权

US4760086A N-alkenyl-3-hydroxybenzo[b]thiophene-2-carboxamide derivatives as dual cyclooxygenase and lipoxygenase inhibitors 失效
标题翻译： N-烯基-3-羟基苯并[b]噻吩-2-甲酰胺衍生物作为双重环加氧酶和脂氧合酶抑制剂
公开(公告)号：US4760086A
公开(公告)日：1988-07-26
申请号：US705115
申请日：1985-02-27
申请人： Allan N. Tischler , Bruce E. Witzel , Philippe L. Durette , Kathleen M. Rupprecht , Timothy F. Gallagher , Debra L. Allison , Marvin M. Goldenberg
发明人： Allan N. Tischler , Bruce E. Witzel , Philippe L. Durette , Kathleen M. Rupprecht , Timothy F. Gallagher , Debra L. Allison , Marvin M. Goldenberg
IPC分类号： C07C63/70 , C07D303/04 , C07D333/70 , C07D409/12 , A61K31/38 , C07D333/62
CPC分类号： C07D409/12 , A61K9/0048 , A61K9/0051 , C07C247/00 , C07D303/04 , C07D333/70
摘要： N-Alkenyl-3-hydroxybenzo[b]thiophene-2-carboxamide derivatives have been prepared by:(1) treating a substituted 2-halobenzoate with thioacetamide followed by N-alkenylation with appropriate agents, such as aldehydes, ketones, enol ethers, epoxides, acetals or ketals;(2) treating a substituted thiosalicylate with an appropriately substituted haloacetamide, followed by dehydration; and(3) further synthetic modification of compounds prepared above.These compounds have been found to be effective inhibitors of both cyclooxygenase and lipoxygenase and thereby useful in the treatment of pain, fever, inflammation, arthritic conditions, asthma, allergic disorders, skin diseases, cardiovascular disorders, psoriasis, inflammatory bowel disease, glaucoma or other prostaglandins and/or leukotriene mediated diseases. Furthermore, these compounds have been found to exhibit cytoprotective activity which does not involve the inhibition of gastric acid secretion but can be used at relatively low dosages for increasing the resistance of gastro-intestinal mucosa to strong irritants.
摘要翻译： N-烯基-3-羟基苯并[b]噻吩-2-甲酰胺衍生物通过以下方法制备：（1）用硫代乙酰胺处理取代的2-卤代苯甲酸，然后用合适的试剂如醛，酮，烯醇醚，环氧化物，缩醛或缩酮; （2）用适当取代的卤代乙酰胺处理取代的硫代水杨酸酯，然后脱水; 和（3）进一步合成上述制备的化合物。已经发现这些化合物是环加氧酶和脂氧合酶的有效抑制剂，从而可用于治疗疼痛，发热，炎症，关节炎状况，哮喘，过敏性疾病，皮肤疾病，心血管疾病，牛皮癣，炎性肠病，青光眼或其他前列腺素和/或白三烯介导的疾病。此外，已经发现这些化合物具有不涉及抑制胃酸分泌的细胞保护活性，但可以以相对低的剂量使用以增加胃肠粘膜对强烈刺激物的抵抗力。

3. 发明授权

US4663344A Anti-inflammatory and analgesic 3-hydroxybenzo[b]thiophene derivatives, compositions, and method of use therefor 失效
标题翻译：抗炎止痛3-羟基苯并[b]噻吩衍生物，组合物及其用途
公开(公告)号：US4663344A
公开(公告)日：1987-05-05
申请号：US710727
申请日：1985-03-11
申请人： Philippe L. Durette , Bruce E. Witzel , Kathleen M. Rupprecht , Allan N. Tischler , Timothy F. Gallagher
发明人： Philippe L. Durette , Bruce E. Witzel , Kathleen M. Rupprecht , Allan N. Tischler , Timothy F. Gallagher
IPC分类号： C07D333/64 , C07D409/04 , C07D409/12 , A61K31/38 , A61K31/415
CPC分类号： C07D409/04 , C07D333/64 , C07D409/12
摘要： 3-Hydroxybenzo[b]thiophene derivatives, such as 2-aralkyl, 2-alkyl and 2-alkenyl-3-hydroxybenzo[b]-thiophenes, were prepared by, among other methods, ring closure of 2-(2-carboxy-phenylthio)-.alpha.-substituted acetic acids. These compounds are found to be useful in the treatment of pain, fever, inflammation, arthritic conditions, asthma, allergic disorders, skin diseases, cardiovascular disorders, psoriasis, inflammatory diseases and other prostaglandin and/or leukotriene mediated diseases.
摘要翻译： 3-羟基苯并[b]噻吩衍生物，例如2-芳烷基，2-烷基和2-烯基-3-羟基苯并[b]噻吩，通过其它方法制备2-（2-羧基 - 苯硫基）-α-取代的乙酸。发现这些化合物可用于治疗疼痛，发热，炎症，关节炎病症，哮喘，过敏性疾病，皮肤疾病，心血管疾病，牛皮癣，炎性疾病和其他前列腺素和/或白三烯介导的疾病。

4. 发明授权

US5068248A N-alkenyl-3-hydroxybenzo[b]thiophene-2-carboxamide derivatives as dual cyclooxygenase and lipoxygenase inhibitors 失效
标题翻译： N-烯基-3-羟基苯并[b]噻吩-2-甲酰胺衍生物作为双重环加氧酶和脂氧合酶抑制剂
公开(公告)号：US5068248A
公开(公告)日：1991-11-26
申请号：US369982
申请日：1989-06-22
申请人： Allan N. Tischler , Philippe L. Durette , Bruce E. Witzel , Kathleen M. Rupprecht , Timothy F. Gallagher , Marvin M. Goldenberg , Debra L. Allison
发明人： Allan N. Tischler , Philippe L. Durette , Bruce E. Witzel , Kathleen M. Rupprecht , Timothy F. Gallagher , Marvin M. Goldenberg , Debra L. Allison
IPC分类号： A61K31/38 , C07C63/70 , C07D303/04 , C07D333/70 , C07D409/12
CPC分类号： C07D409/12 , A61K31/352 , A61K31/381 , A61K31/382 , A61K31/4178 , A61K31/473 , C07C247/00 , C07D303/04 , C07D333/70
摘要： Method for increasing resistance to gastro-intestinal irritation, and for the treatment of pain, fever, inflammation, arthritic conditions, asthma, allergic disorders, skin diseases, cardiovascular disorders, psoriasis, inflammatory bowel disease, glaucoma or other prostaglandin and/or leukotriene mediated diseases comprising the administration to a subject in need of such treatment, a non-toxic therapeutically effective amount of compound of formula I: ##STR1##
摘要翻译：治疗疼痛，发烧，炎症，关节炎病症，哮喘，过敏性疾病，皮肤疾病，心血管疾病，牛皮癣，炎性肠病，青光眼或其他前列腺素和/或白三烯介导的治疗方法包括向需要这种治疗的受试者施用的疾病，无毒性治疗有效量的式I化合物：

5. 发明授权

US4621091A 3-hydroxybenzo[b]thiophene-2-sulfide derivatives compositions, and method of use therefor 失效
标题翻译： 3-羟基苯并[b]噻吩-2-硫化物衍生物组合物及其用途
公开(公告)号：US4621091A
公开(公告)日：1986-11-04
申请号：US658859
申请日：1984-10-09
申请人： Allan N. Tischler , Thomas J. Lanza, Jr.
发明人： Allan N. Tischler , Thomas J. Lanza, Jr.
IPC分类号： C07D521/00 , A61K31/38 , A61K31/381 , A61P1/00 , A61P29/00 , A61P37/08 , A61P43/00 , C07D333/64 , C07D333/66 , C07D333/68 , A61K31/34 , C07D401/12
CPC分类号： C07D333/64 , C07C323/00
摘要： 3-hydroxybenzo[b]thiophene-2-sulfide derivatives have been prepared by ring closure of an appropriately substituted 2--R.sup.1 SCH.sub.2 S-- benzoic acid ester in the presence of a strong base. These compounds have been found to be specific inhibitors of 5-lipoxygenase and thereby useful in the treatment of inflammation, pain and fever associated with inflammation, arthritic conditions, asthma, allergic disorders such as allergic rhinitis and chronic bronchitis, skin diseases like psoriasis and atopic exzema, cardiovascular or vascular disorders, and other leukotriene mediated diseases. Furthermore, these compounds have been found to exhibit cytoprotective activity which does not involve the inhibition of gastric acid secretion but can be used at relatively low dosages for increasing the resistance of gastro-intestinal mucosa to strong irritants.
摘要翻译： 3-羟基苯并[b]噻吩-2-硫化物衍生物已经通过在强碱存在下闭合适当取代的2-R 1 CH 2 S-苯甲酸酯来制备。已经发现这些化合物是5-脂氧合酶的特异性抑制剂，从而可用于治疗与炎症，关节炎状况，哮喘，过敏性鼻炎和慢性支气管炎等过敏性疾病，牛皮癣和特应性皮肤病有关的炎症，疼痛和发热心血管或血管疾病，以及其他白细胞三烯介导的疾病。此外，已经发现这些化合物具有不涉及抑制胃酸分泌的细胞保护活性，但可以以相对低的剂量使用以增加胃肠粘膜对强烈刺激物的抵抗力。

6. 发明授权

US4720503A N-substituted fused-heterocyclic carboxamide derivatives as dual cyclooxygenase and lipoxygenase inhibitors 失效
标题翻译： N-取代的稠合 - 杂环羧酰胺衍生物作为双重环加氧酶和脂氧合酶抑制剂
公开(公告)号：US4720503A
公开(公告)日：1988-01-19
申请号：US761946
申请日：1985-08-02
申请人： Bruce E. Witzel , Allan N. Tischler , Debra L. Allison
发明人： Bruce E. Witzel , Allan N. Tischler , Debra L. Allison
IPC分类号： C07D493/04 , C07D495/04 , A61K31/38 , A61K31/34 , C07D493/00 , C07D495/02
CPC分类号： C07D493/04 , C07D495/04
摘要： N-substituted fused-heterocyclic carboxamide derivatives, for example, N-(2,2-diphenylethenyl)-3-hydroxythieno[3,2-b]thiophene-2-carboxamide can be prepared by ring closure between an appropriately substituted halo-thiophene ester, e.g., methyl 3-bromo-thiophene-2-carboxylate, and mercaptoacetamide followed by condensation with diphenylacetaldehyde. Alternatively, the ring closure can be carried out between an appropriately substituted mercaptothiophene ester, e.g., methyl 3-mercaptothiophene-2-carboxylate and a haloacetamide to afford the fused-heterocyclic intermediate, 3-hydroxythieno[3,2-b]thiophene-2-carboxamide. N-alkenylation of the intermediate will then lead to the final products.These compounds have been found to be effective inhibitors of both cyclooxygenase and lipoxygenase and thereby useful in the treatment of pain, fever, inflammation, arthritic conditions, eye inflammation caused by glaucoma or other eye diseases, asthma, allergic disorders, skin diseases, cardiovascular disorders, psoriasis, inflammatory bowel disease, or other prostaglandin and/or leukotriene mediated diseases.
摘要翻译： N-取代的稠合杂环甲酰胺衍生物，例如N-（2,2-二苯基乙烯基）-3-羟基噻吩并[3,2-b]噻吩-2-甲酰胺可以通过在适当取代的卤代噻吩酯，例如3-溴 - 噻吩-2-甲酸甲酯和巯基乙酰胺，随后与二苯基乙醛缩合。或者，闭环可以在适当取代的巯基噻吩酯例如3-巯基噻吩-2-羧酸甲酯和卤代乙酰胺之间进行，得到稠合杂环中间体3-羟基噻吩并[3,2-b]噻吩-2 甲酰胺。中间体的N-烯基化将导致最终产物。已经发现这些化合物是环加氧酶和脂氧合酶的有效抑制剂，从而可用于治疗疼痛，发热，炎症，关节炎病症，由青光眼或其他眼睛疾病引起的眼睛炎症，哮喘，过敏性疾病，皮肤疾病，心血管疾病，牛皮癣，炎症性肠病或其他前列腺素和/或白三烯介导的疾病。

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