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21. 发明授权

US3978124A 6-Substituted 2-naphthyl .alpha.-substituted acetamides 失效
标题翻译： 6-取代的2-萘基 - 取代的乙酰胺
公开(公告)号：US3978124A
公开(公告)日：1976-08-31
申请号：US558583
申请日：1975-03-17
申请人： John H. Fried , Ian J. Harrison
发明人： John H. Fried , Ian J. Harrison
IPC分类号： C07C45/46 , C07C49/697 , C07C49/755 , C07C57/58 , C07C59/64 , C07C59/72 , C07C59/90 , C07C103/22
CPC分类号： C07C59/90 , C07C45/28 , C07C45/46 , C07C57/58 , C07C59/64 , C07C59/72 , Y10S514/916
摘要： 2-Naphthyl acetic acid derivatives and the corresponding amides, esters, hydroxamic acids and addition salts thereof, optionally substituted at the .alpha.-position on the acetic acid moiety and/or at position 6 and/or at positions 1, 4, 7 or 8 on the naphthyl ring and optionally saturated at positions 3 and 4, are anti-inflammatory, analgesic, anti-pyretic and anti-pruritic agents. A pharmaceutical method of effecting treatment of inflammation, pain, pyrexia and pruritus by the administration of naphthyl acetic acid derivatives. A pharmaceutical composition for use in the treatment of the above maladies comprising a naphthyl acetic acid derivative.

22. 发明授权

US3947472A Naphthyl acetaldehyde derivatives 失效
公开(公告)号：US3947472A
公开(公告)日：1976-03-30
申请号：US492378
申请日：1974-07-29
申请人： John H. Fried , Ian T. Harrison
发明人： John H. Fried , Ian T. Harrison
IPC分类号： C07C57/40 , C07C57/42 , C07C57/46 , C07C57/50 , C07C57/58 , C07C57/60 , C07C59/64 , C07C59/84 , C07D317/22 , C07D319/06
CPC分类号： C07C45/41 , C07C45/673 , C07C57/40 , C07C57/42 , C07C57/46 , C07C57/50 , C07C57/58 , C07C57/60 , C07C59/64 , C07C59/84
摘要： 2-(2'-Naphthyl) acetaldehyde derivatives optionally substituted at the 2 position and/or positions C-1',4',5',7' or 8'; and/or position C-6' or positions C-5' and 7' exhibit anti-inflammatory, analgesic, antipyretic and anti-pruritic activity.

23. 发明授权

US5057621A 11-substituted-16-phenoxy and 16-substituted phenoxy-prostatrienoic acid derivatives 失效
标题翻译： 11-取代的-16-苯氧基和16-取代的苯氧基 - 前列腺烯酸衍生物
公开(公告)号：US5057621A
公开(公告)日：1991-10-15
申请号：US39560
申请日：1987-04-16
申请人： Gary F. Cooper , John H. Fried , L. David Waterbury
发明人： Gary F. Cooper , John H. Fried , L. David Waterbury
IPC分类号： C07C405/00 , C07C177/00
CPC分类号： C07C405/00
摘要： This invention covers a compound of the formula ##STR1## wherein R is hydrogen, lower alkyl or a pharmaceutically acceptable, non-toxic salt of a compound wherein R is hydrogen; X is hydrogen, halo, trifluoromethyl, lower alkyl or lower alkoxy, Y is lower alkyl or ##STR2## wherein Z is hydrogen, halo, methyl, methoxy or trifluoromethyl; and the wavy lines represent the .alpha. or .beta. configuration with the proviso that when one wavy line is .alpha. the other is .beta..
摘要翻译：本发明涵盖下式的化合物，其中R是氢，其中R是氢的化合物的低级烷基或药学上可接受的无毒盐; X是氢，卤素，三氟甲基，低级烷基或低级烷氧基，Y是低级烷基或者其中Z是氢，卤素，甲基，甲氧基或三氟甲基; 波浪线表示α或β配置，条件是当一条波浪线为α时，另一条波长为β。

24. 发明授权

US4097674A 2-Naphthylacetic acid derivatives 失效
标题翻译： 2-萘乙酸衍生物
公开(公告)号：US4097674A
公开(公告)日：1978-06-27
申请号：US727082
申请日：1976-09-27
申请人： John H. Fried , Ian T. Harrison
发明人： John H. Fried , Ian T. Harrison
IPC分类号： C07C57/40 , C07C57/58 , C07C59/64 , C07C59/72 , C07C63/36 , C07C69/76
CPC分类号： C07C17/2632 , C07C45/28 , C07C57/40 , C07C57/58 , C07C59/64 , C07C59/72
摘要： 2-Naphthyl acetic acid derivatives and the corresponding amides, esters, hydroxamic acids and addition salts thereof, optionally substituted at the .alpha.-position on the acetic acid moiety and/or at position 6 and/or at positions 1, 4, 7 or 8 on the naphthyl ring and optionally saturated at positions 3 and 4, are anti-inflammatory, analgesic, anti-pyretic and anti-pruritic agents. A pharmaceutical method of effecting treatment of inflammation, pain, pyrexia and pruritus by the administration of naphthyl acetic acid derivatives. A pharmaceutical composition for use in the treatment of the above maladies comprising a naphthyl acetic acid derivative.
摘要翻译： 2-萘基乙酸衍生物和相应的酰胺，酯，异羟肟酸及其加成盐，任选在乙酸部分和/或第6位和/或第1,4,7或8位的α-位上被取代在萘环上并且任选地在3和4位饱和是抗炎，止痛，抗裂解和抗瘙痒剂。通过给予萘基乙酸衍生物来治疗炎症，疼痛，发热和瘙痒的药物方法。一种用于治疗上述疾病的药物组合物，其包含萘基乙酸衍生物。

25. 发明授权

US4080461A 5(6)-Benzene ring substituted benzimidazole-2-carbamate derivatives having anthelmintic activity 失效
标题翻译： 5（6）具有驱虫活性的苯并环取代的苯并咪唑-2-氨基甲酸酯衍生物
公开(公告)号：US4080461A
公开(公告)日：1978-03-21
申请号：US729229
申请日：1976-10-04
申请人： Colin C. Beard , John A. Edwards , John H. Fried
发明人： Colin C. Beard , John A. Edwards , John H. Fried
IPC分类号： C07D235/32 , A61K31/415
CPC分类号： C07D235/32
摘要： Benzene ring substituted benzimidazole-2-carbamate derivatives represented by the formula: ##STR1## where R is a lower alkyl group having 1 to 4 carbon atoms; R.sup.1 is --SOR.sup.2, --SO.sub.2 R.sup.2, --SCN, --SR.sup.5, --OR.sup.5 or M'(CH.sub.2).sub.n MR.sup.7 where M and M' are independently O, S, ##STR2## R.sup.7 is lower alkyl having 1 to 4 carbon atoms or aryl, and n is 1-4; R.sup.2 is lower alkyl having from 1 to 6 carbon atoms, cycloalkyl having 3 to 7 carbon atoms, lower alkenyl or lower alkynyl having 3 to 6 carbon atoms, or aralkyl or aryl; andR.sup.5 is lower alkenyl, lower alkynyl, or aralkyl. The R.sup.1 substitution is at the 5(6)-position.The compounds are useful as pesticides, particularly as anthelmintic and antifungal agents.
摘要翻译：由下式表示的苯环取代的苯并咪唑-2-氨基甲酸酯衍生物：其中R是具有1至4个碳原子的低级烷基; R1是-SOR2，-SO2R2，-SCN，-SR5，-OR5或M'（CH2）nMR7，其中M和M'独立地是O，S，R7是具有1-4个碳原子的低级烷基或芳基， n为1-4; R2是具有1至6个碳原子的低级烷基，具有3至7个碳原子的环烷基，具有3至6个碳原子的低级链烯基或低级炔基，或芳烷基或芳基; 并且R 5为低级链烯基，低级炔基或芳烷基。 R1取代为5（6）位。

26. 发明授权

US4072696A 5(6)-Benzene ring substituted benzimidazole-2-carbamate derivatives having anthelmintic activity 失效
标题翻译： 5（6）具有驱虫活性的苯并环取代的苯并咪唑-2-氨基甲酸酯衍生物
公开(公告)号：US4072696A
公开(公告)日：1978-02-07
申请号：US434656
申请日：1974-01-18
申请人： Colin C. Beard , John A. Edwards , John H. Fried
发明人： Colin C. Beard , John A. Edwards , John H. Fried
IPC分类号： C07C335/28 , C07C147/00 , C07C147/06 , C07C149/40
CPC分类号： C07C335/28
摘要： Carbalkoxythioureidobenzene derivatives represented by the following formula: ##STR1## where R is a lower alkyl group having 1 to 4 carbon atoms; R.sup.1 is --SR.sup.2, --SOR.sup.2, --SO.sub.2 R.sup.2, --OR.sup.2, --SCN, --SC(O)NR.sup.3 R.sup.4, or --M'(CH.sub.2).sub.n MR.sup.7 where n is 1-4; R.sup.2 is lower alkyl having 1 to 6 carbon atoms, cycloalkyl having 3 to 7 carbon atoms, lower alkenyl or lower alkynyl having 3 to 6 carbon atoms, aralkyl or aryl, provided that when R.sup.1 is --SO.sub.2 R.sup.2, R.sup.2 is not aralkyl or phenyl; R.sup.3 and R.sup.4 are independently hydrogen or lower alkyl having 1 to 6 carbon atoms; Y is amino, nitro, acylamino where the acyl portion has 1 to 6 carbon atoms, --NHC(O) (CH.sub.2).sub.m COOH where m is 1-6, or --NHC(S)NHCOOR; M and M' are independently O, S or ##STR2## and R.sup.7 is lower alkyl having 1 to 4 carbon atoms or aryl. The R.sup.1 substitution is either at the 4- or 5-position.The compounds are useful as pesticides, particularly as anthelmintic and antifungal agents.
摘要翻译：由下式表示的碳烷氧基硫代脲基苯衍生物：其中R是具有1至4个碳原子的低级烷基; R1是-SR2，-SOR2，-SO2R2，-OR2，-SCN，-SC（O）NR3R4或-M'（CH2）nMR7，其中n是1-4; R2是具有1至6个碳原子的低级烷基，具有3至7个碳原子的环烷基，具有3至6个碳原子的低级链烯基或低级炔基，芳烷基或芳基，条件是当R 1是-SO 2 R 2时，R 2不是芳烷基或苯基; R3和R4独立地是氢或具有1至6个碳原子的低级烷基; Y是酰基部分具有1-6个碳原子的氨基，硝基，酰基氨基，-NHC（O）（CH 2）m COOH，其中m是1-6，或-NHC（S）NHCOOR; M和M'独立地为O，S或，并且R 7为具有1至4个碳原子的低级烷基或芳基。 R1取代在4-或5-位。

27. 发明授权

US4051233A 2-Naphthylacetic acid derivatives and compositions and methods thereof 失效
标题翻译： 2-萘甲酸衍生物及其组合物及其方法
公开(公告)号：US4051233A
公开(公告)日：1977-09-27
申请号：US684993
申请日：1976-05-10
申请人： John H. Fried , Ian T. Harrison
发明人： John H. Fried , Ian T. Harrison
IPC分类号： C07C57/40 , C07C59/64 , C07C59/72 , A61K31/19 , C07C63/36
CPC分类号： C07C59/72 , C07C45/28 , C07C57/40 , C07C59/64 , Y10S514/916
摘要： 2-Naphthyl acetic acid derivatives and the corresponding amides, esters, hydroxamic acids and addition salts thereof, optionally substituted at the .alpha.-position on the acetic acid moiety and/or at position 6 and/or at positions 1, 4, 7 or 8 on the naphthyl ring and optionally saturated at positions 3 and 4, are anti-inflammatory, analgesic, anti-pyretic and anti-pruritic agents. A pharmaceutical method of effecting treatment of inflammation, pain, pyrexia and pruritus by the administration of naphthyl acetic acid derivatives. A pharmaceutical composition for use in the treatment of the above maladies comprising a naphthyl acetic acid derivative.

28. 发明授权

US4048330A Compositions containing 2-(6'-substituted-2'-naphthyl)acetic acid esters used for treating inflammation, pain or pyrexia 失效
标题翻译：含有用于治疗炎症，疼痛或发热的2-（6 {40-取代-2 {40-萘基）乙酸酯的组合物
公开(公告)号：US4048330A
公开(公告)日：1977-09-13
申请号：US605477
申请日：1975-08-18
申请人： John H. Fried , Ian T. Harrison
发明人： John H. Fried , Ian T. Harrison
IPC分类号： C07C45/28 , C07C45/46 , C07C49/697 , C07C49/755 , C07C57/42 , C07C57/60 , C07D307/20 , A61K31/235
CPC分类号： C07C45/46 , C07C45/28 , C07C57/42 , C07C57/60 , C07D307/20
摘要： Compositions containing 2-(6'-substituted-2'-naphthyl)acetic acid derivatives substituted at the 2-position of the acetic acid moiety with methyl, ethyl, difluoromethyl, or methylene, and the salts and esters thereof, having anti-inflammatory, analgesic and anti-pyretic activities, and methods for the use thereof in the treatment of inflammation, pain and pyrexia.
摘要翻译：含有在乙酸部分的2-位被甲基，乙基，二氟甲基或亚甲基取代的2-（6'-取代-2'-萘基）乙酸衍生物的组合物及其盐和酯，具有抗炎作用，镇痛和抗热解活性，以及用于治疗炎症，疼痛和发热的方法。

29. 发明授权

US4001301A 6-Substituted 2-naphthyl acetic acid derivatives 失效
标题翻译： 6-取代的2-萘基乙酸衍生物
公开(公告)号：US4001301A
公开(公告)日：1977-01-04
申请号：US558874
申请日：1975-03-17
申请人： John H. Fried , Ian T. Harrison
发明人： John H. Fried , Ian T. Harrison
IPC分类号： C07C45/46 , C07C49/697 , C07C49/755 , C07C57/58 , C07C59/13 , C07C59/64 , C07C59/72 , C07C69/616 , C07C233/00 , C07C69/76
CPC分类号： C07C323/00 , C07C45/28 , C07C45/46 , C07C57/58 , C07C59/64 , C07C59/72 , Y10S514/916
摘要： 2-Naphthyl acetic acid derivatives and the corresponding amides, esters, hydroxamic acids and addition salts thereof, optionally substituted at the .alpha.-position on the acetic acid moiety and/or at position 6 and/or at positions 1, 4, 7 or 8 on the naphthyl ring and optionally saturated at positions 3 and 4, are anti-inflammatory, analgesic, antipyretic and anti-pruritic agents. A pharmaceutical method of effecting treatment of inflammation, pain, pyrexia and pruritus by the administration of naphthyl acetic acid derivatives. A pharmaceutical composition for use in the treatment of the above maladies comprising a naphthyl acetic acid derivative.

30. 发明授权

US3985791A 16-Phenoxy and 16-substituted phenoxy-prostatrienoic acid derivatives 失效
标题翻译： 16-苯氧基和16-取代的苯氧基 - 前列腺烯酸衍生物
公开(公告)号：US3985791A
公开(公告)日：1976-10-12
申请号：US643219
申请日：1975-12-22
申请人： Joseph M. Muchowski , John H. Fried
发明人： Joseph M. Muchowski , John H. Fried
IPC分类号： C07C405/00 , C07D307/935 , C07D309/12 , C07F9/40 , C07C69/76
CPC分类号： C07D307/935 , C07C405/00 , C07D309/12 , C07F9/4006
摘要： Novel racemic and 8R-antimeric 16-phenoxy- and 16-(o, m or p)-substituted phenoxy derivatives of 9.alpha., 11.alpha.,15-trihydroxy-17,18,19,20-tetranorprosta-4,5,13-trans-trienoic acids, which may be further substituted at C-15 by a methyl or ethyl group, the pharmaceutically acceptable, non-toxic lower alkyl esters and salts thereof and processes for the production of such compounds. dl 9.alpha.,11.alpha.,15.alpha.-trihydroxy-16-m-trifluoromethylphenoxy-17,18,19,20-tetranorprosta-4,5,13-trans-trienoic acid and dl 9.alpha.,11.alpha.,15 -trihydroxy-15 -methyl-16-m-trifluoromethylphenoxy-17,18,19,20-tetranorprosta-4,5,13-trans-trienoic acid are representative compounds of the class. These compounds possess prostaglandin-like activities and thus are useful in the treatment of mammals where prostaglandins are indicated. They are particularly useful as luteolytic agents in female mammals.
摘要翻译： 9α，11α，15-三羟基-17,18,19,20-四前列腺素-4,5,13的新外消旋和8R-抗体的16-苯氧基和16-（o，m或p）取代的苯氧基衍生物可以在C-15被甲基或乙基基团进一步取代的反式三烯酸，其药学上可接受的无毒低级烷基酯及其盐及其制备方法。 dl9α，11α，15α-三羟基-16-间三氟甲基苯氧基-17,18,19,20-四前列腺素-4,5,13-反式三烯酸和dl9α，11α，15-三羟基 - 15-甲基-16-m-三氟甲基苯氧基-17,18,19,20-四前驱体-4,5,13-反式三烯酸是该类的代表性化合物。这些化合物具有前列腺素样活性，因此可用于治疗表达前列腺素的哺乳动物。它们在雌性哺乳动物中特别有用作为溶解性成分。

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