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1. 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。

2. 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：

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

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。

5. 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。

6. 发明授权

US4814501A Process for preparing N,N-dimethyl 2-(methylthio) benzamides and analogs 失效
标题翻译：制备N，N-二甲基2-（甲硫基）苯甲酰胺和类似物的方法
公开(公告)号：US4814501A
公开(公告)日：1989-03-21
申请号：US138251
申请日：1987-12-28
申请人： Bruce E. Witzel , Robert K. Baker , Philippe L. Durette , Robert A. Frankshun
发明人： Bruce E. Witzel , Robert K. Baker , Philippe L. Durette , Robert A. Frankshun
IPC分类号： C07C319/14 , C07C323/62 , C07C333/04 , C07C149/41 , C07C102/06 , C07D213/62
CPC分类号： C07C319/14 , C07C323/62 , C07C333/04
摘要： Pyrolysis of substituted salicylate O(N,N-dialkyl)thiocarbamates yielded the corresponding N,N-dialkyl-2-(methylthio)benzamide. Similarly, substituted 6-azasalicylate O(N,N-dialkyl)thiocarbamates yielded the corresponding N,N-dialkyl-2-(methylthio)-6-aza-benzamide.
摘要翻译：取代的水杨酸酯O（N，N-二烷基）硫代氨基甲酸酯的热解得到相应的N，N-二烷基-2-（甲硫基）苯甲酰胺。类似地，取代的6-氮杂水杨酸O（N，N-二烷基）硫代氨基甲酸酯得到相应的N，N-二烷基-2-（甲硫基）-6-氮杂 - 苯甲酰胺。

7. 发明授权

US5693809A Substituted 4-aza-5.alpha.-androstan-ones as 5.alpha.-reductase inhibitors 失效
标题翻译：取代的4-氮杂-5α-雄甾烷酮作为5α-还原酶抑制剂
公开(公告)号：US5693809A
公开(公告)日：1997-12-02
申请号：US338571
申请日：1995-05-12
申请人： Philippe L. Durette , William Hagmann , Gary H. Rasmusson , Richard L. Tolman , Ihor E. Kopka , Soumya P. Sahoo , Craig K. Esser , Nathan G. Steinberg , Donald W. Graham , Bruce E. Witzel
发明人： Philippe L. Durette , William Hagmann , Gary H. Rasmusson , Richard L. Tolman , Ihor E. Kopka , Soumya P. Sahoo , Craig K. Esser , Nathan G. Steinberg , Donald W. Graham , Bruce E. Witzel
IPC分类号： C07C53/136 , C07C59/82 , C07C59/90 , C07J1/00 , C07J7/00 , C07J9/00 , C07J41/00 , C07J73/00 , C07D221/02 , A61K31/435
CPC分类号： C07J1/0022 , C07C53/136 , C07C59/82 , C07C59/90 , C07J1/0011 , C07J41/0038 , C07J7/003 , C07J7/007 , C07J73/005 , C07J9/00
摘要： Described are new 16-substituted and 7,16-disubstituted 4-aza-5.alpha.-androstan-3-ones and related compounds as 5.alpha.-reductase inhibitors.
摘要翻译：描述了新的16取代和7,16-二取代的4-氮杂-5α-雄甾烷-3-酮和相关化合物作为5α-还原酶抑制剂。

8. 发明授权

US4380645A Process for preparing Benzoxepino- or Benzthiapino[4,3-b]pyrrole-2-acetic acids 失效
标题翻译：制备苯并西泮或苯硫噻嗪[4,3-b]吡咯-2-乙酸的方法
公开(公告)号：US4380645A
公开(公告)日：1983-04-19
申请号：US329842
申请日：1981-12-11
申请人： Bruce E. Witzel , Paul E. Finke , Debra L. Allison
发明人： Bruce E. Witzel , Paul E. Finke , Debra L. Allison
IPC分类号： C07D207/34 , C07D209/70 , C07D313/08 , C07D487/04 , C07D491/04 , C07D491/044 , C07D495/04
CPC分类号： C07D487/04 , C07D207/34 , C07D209/70 , C07D313/08 , C07D491/04 , C07D495/04
摘要： Improved yields of Benzoxepino- or Benzthiapino[4,3-b]pyrrole-2-acetic acids have been achieved from processes based on modifications performed on a pyrrole carboxylic ester rather than on a pyrrole-.alpha.-oxoacetate.
摘要翻译：通过基于对吡咯羧酸酯而不是吡咯-α-氧代乙酸酯进行的改性的方法，已经获得了苯并西泮或苯硫基亚氨基[4,3-b]吡咯-2-乙酸的产率的提高。

9. 发明授权

US4999436A Aryl-substituted thiophene 3-ols, derivatives and analogs useful as lipoxgenase inhibitors 失效
标题翻译：芳基取代的噻吩3-ols，可用作脂氧合酶抑制剂的衍生物和类似物
公开(公告)号：US4999436A
公开(公告)日：1991-03-12
申请号：US397325
申请日：1989-08-22
申请人： Bruce E. Witzel , Debra L. Allison , Charles G. Caldwell , Kathleen Rupprecht
发明人： Bruce E. Witzel , Debra L. Allison , Charles G. Caldwell , Kathleen Rupprecht
IPC分类号： C07D333/32 , C07D333/50 , C07D333/64 , C07D333/78 , C07D333/80 , C07D409/04
CPC分类号： C07D409/04 , C07D333/32 , C07D333/50 , C07D333/64 , C07D333/78 , C07D333/80
摘要： Aryl substituted thiophenes 3-ols, its dihydro derivatives, 1-oxide and 1,1-dioxide analogs, as well as aryl substituted furans, are 5-lipoxygenase inhibitors useful in the treatment of inflammation and other leukotriene-mediated diseases.
摘要翻译：芳基取代的噻吩3-ols，其二氢衍生物，1-氧化物和1,1-二氧化物类似物以及芳基取代的呋喃是可用于治疗炎症和其它白三烯介导的疾病的5-脂氧合酶抑制剂。

10. 发明授权

US4440779A Tricyclic derivatives of substituted pyrrole acids as analgesic and anti-inflammatory agents 失效
标题翻译：取代吡咯酸的三环衍生物作为止痛剂和抗炎剂
公开(公告)号：US4440779A
公开(公告)日：1984-04-03
申请号：US385232
申请日：1982-06-04
申请人： James B. Doherty , Conrad P. Dorn , Bruce E. Witzel , Debra L. Allison , Tsung-Ying Shen
发明人： James B. Doherty , Conrad P. Dorn , Bruce E. Witzel , Debra L. Allison , Tsung-Ying Shen
IPC分类号： C07D209/70 , C07D207/34 , C07D313/08 , C07D487/04 , C07D491/04 , C07D491/044 , C07D495/04 , A61K31/55 , C07D209/94
CPC分类号： C07D487/04 , C07D207/34 , C07D209/70 , C07D313/08 , C07D491/04 , C07D495/04 , Y10S514/899 , Y10S514/916
摘要： Tricyclic derivatives of substituted pyrrole acids, e.g., substituted 4,10-dihydro-10-oxo-1H-[1]benzoxepino[4,3-b]pyrrole-2-acetic acids or the 5-thia analogs thereof have been prepared via hydrolysis of a precursor or decarboxylation of a precursor-diacid. These tricyclic compounds are found to have high analgesic and anti-inflammatory activities but low ulcerogenic side effects.
摘要翻译：取代的吡咯酸的三环衍生物，例如取代的4,10-二氢-10-氧代-1H- [1]苯并氧杂环[4,3-b]吡咯-2-乙酸或其5-硫杂类似物已经通过前体二酸的前体水解或脱羧。发现这些三环化合物具有高镇痛作用和抗炎活性，但具有低溃疡性副作用。

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