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1. 发明授权

US4172949A 2,4-Disubstituted-5-oxo-5H-dibenzo[a,d]cycloheptenes 失效
标题翻译： 2,4-二取代-5-氧代-5H-二苯并{8α，d {9环庚烯
公开(公告)号：US4172949A
公开(公告)日：1979-10-30
申请号：US920047
申请日：1978-06-28
申请人： James P. Dunn , Peter H. Nelson , Karl G. Untch
发明人： James P. Dunn , Peter H. Nelson , Karl G. Untch
IPC分类号： C07C51/36 , C07C59/90 , C07C65/28 , C07C65/40 , C07C65/14 , C07C69/76
CPC分类号： C07C65/40 , C07C51/36 , C07C59/90 , C07C65/28 , Y10S514/825 , Y10S514/916
摘要： Compounds of the formula ##STR1## wherein R is hydrogen or methyl; R.sup.1 is hydrogen, C.sub.1 to C.sub.8 linear or branched alkyl or C.sub.1 to C.sub.8 linear or branched alkanoyl; X is oxygen or sulfur; R.sup.2 is selected from the group hydrogen, C.sub.1 to C.sub.18 linear or branched alkyl and the radicals --(CH.sub.2).sub.n --NR.sup.3 R.sup.4, --CH.sub.2 --CH(OH)--CH.sub.2 --OH or a ketal thereof formed from the aldehyde or ketone R.sup.5 R.sup.6 CO, wherein R.sup.3 and R.sup.4 are each independently C.sub.1 to C.sub.6 linear or branched alkyl or R.sup.3 and R.sup.4 taken together with the nitrogen atom of the first radical are attached to form a 5- or 6-membered heterocyclic ring, R.sup.5 and R.sup.6 are each independently hydrogen, C.sub.1 to C.sub.6 linear or branched alkyl, phenyl or benzyl or R.sup.5 and R.sup.6 taken together represent an alkylene bridge of from 4 to 6 carbon atoms; n is an integer of from 2 to 4; and the dotted line represents an optional double bond; and the pharmaceutically acceptable salts thereof. The compounds have anti-inflammatory, analgesic and anti-pyretic activities and, accordingly, are useful in the treatment of inflammation, pain and/or pyrexia.
摘要翻译：式（I）的化合物，其中R是氢或甲基; R1是氢，C1至C8直链或支链烷基或C1至C8直链或支链烷酰基; X是氧或硫; R2选自氢，C1至C18直链或支链烷基和由醛或酮R5R6CO形成的基团 - （CH2）n-NR3R4，-CH2-CH（OH）-CH2-OH或其缩酮，其中 R 3和R 4各自独立地为C 1至C 6直链或支链烷基或与第一基团的氮原子一起的R 3和R 4连接以形成5-或6-元杂环，R 5和R 6各自独立地为氢，C 1 C 6直链或支链烷基，苯基或苄基或R 5和R 6一起表示4至6个碳原子的亚烷基桥; n为2〜4的整数，虚线表示任选的双键; 及其药学上可接受的盐。这些化合物具有抗炎，止痛和抗热解活性，因此可用于治疗炎症，疼痛和/或发热。

2. 发明授权

US4054579A Intermediates in the process for the preparation of 2-(5H-dibenzo[a,d]cyclohepten-5-on-2-yl)acetic, propionic and butyric acids 失效
标题翻译：制备2-（5H-二苯并{8a，d {9环庚烯-5-基-2-基）乙酸，丙酸和丁酸的方法中的中间体
公开(公告)号：US4054579A
公开(公告)日：1977-10-18
申请号：US697910
申请日：1976-06-21
申请人： Peter H. Nelson , Karl G. Untch , James P. Dunn
发明人： Peter H. Nelson , Karl G. Untch , James P. Dunn
IPC分类号： C07C51/06 , C07C51/08 , C07C51/373 , C07C63/331 , C07C63/66 , C07D317/72 , C07D317/10
CPC分类号： C07D317/72 , C07C51/06 , C07C51/08 , C07C51/373 , C07C63/331 , C07C63/66
摘要： 2-(5H-dibenzo[a,d]cyclohepten-5-on-2-yl)acetic, propionic and butyric acids, and esters and salts thereof, are prepared by solvolysis of nitrile or amide intermediates, or of ketal-protected nitrile, amide, acid, ester or salt intermediates.
摘要翻译： 2-（5H-二苯并[a，d]环庚烯-5-基-2-基）乙酸，丙酸和丁酸及其酯和盐通过溶剂分解腈或酰胺中间体或缩酮保护的腈制备，酰胺，酸，酯或盐的中间体。

3. 发明授权

US3979430A Solvolytic process for the preparation of 2-(5H-dibenzo[a,d]cyclohepten-5-on-2-yl)acetic, propionic and butyric acids 失效
标题翻译：用于制备2-（5H-二苯并{8a，d {9环庚烯-5-基-2-基）乙酸，丙酸和丁酸的溶剂分解方法
公开(公告)号：US3979430A
公开(公告)日：1976-09-07
申请号：US611057
申请日：1975-09-08
申请人： Peter H. Nelson , Karl G. Untch , James P. Dunn
发明人： Peter H. Nelson , Karl G. Untch , James P. Dunn
IPC分类号： C07C51/06 , C07C51/08 , C07C51/373 , C07C59/86 , C07C63/331 , C07C63/66 , C07D317/72 , C07C121/66
CPC分类号： C07D317/72 , C07C51/06 , C07C51/08 , C07C51/373 , C07C59/86 , C07C63/331 , C07C63/66
摘要： 2-(5H-dibenzo[a,d]cyclohepten-5-on-2-yl) acetic, propionic and butyric acids, and esters and salts thereof, are prepared by solvolysis of nitrile or amide intermediates, or of ketal-protected nitrile, amide, acid, ester or salt intermediates.
摘要翻译： 2-（5H-二苯并[a，d]环庚烯-5-基-2-基）乙酸，丙酸和丁酸及其酯和盐通过溶剂分解腈或酰胺中间体或缩酮保护的腈制备，酰胺，酸，酯或盐的中间体。

4. 发明授权

US3966820A 2-Substituted-5-oxo-5H-dibenzo-[A,D]cycloheptenes, the esters and ethers thereof, having pharmaceutical activity, and methods and compositions for the use thereof 失效
标题翻译： 2-取代的5-氧代-5H-二苯并 - {8 A，D 9环庚烯，其具有药物活性的酯和醚及其使用的方法和组合物
公开(公告)号：US3966820A
公开(公告)日：1976-06-29
申请号：US581501
申请日：1975-05-30
申请人： Peter H. Nelson , Karl G. Untch
发明人： Peter H. Nelson , Karl G. Untch
IPC分类号： C07C69/007 , A61K31/12 , C07C45/00 , C07C49/747 , C07C49/753 , C07C49/755 , C07C51/09 , C07C51/377 , C07C51/493 , C07C63/331 , C07C63/66 , C07C67/00 , C07C49/76
CPC分类号： C07C63/66 , C07C49/747 , C07C49/755 , C07C51/09 , C07C51/377 , C07C51/493 , C07C63/331 , Y10S514/916
摘要： 2-Substituted-5-oxo-5H-dibenzo [a,d]cycloheptenes represented by the following formula: ##SPC1##Where one of R.sup.2 and R.sup.3 is hydrogen, and the other is hydrogen, methyl, or ethyl, or together R.sup.2 and R.sup.3 are methylene; the dotted line represents an optional, additional bond between the carbon atoms at the 10- and 11-positions; and the pharmaceutically acceptable esters and ethers thereof. The compounds have anti-inflammatory, analgesic, and antipyretic activities and, accordingly, are useful in the treatment of inflammation, pain and pyrexia.
摘要翻译： 2-取代的5-氧代-5H-二苯并[a，d]环庚烯，由下式表示：

5. 发明授权

US4112114A Esters of 2-substituted-5-oxo-5H-dibenzo[a,d]cycloheptenes having pharmaceutical activity, and methods and compositions for the use thereof 失效
标题翻译：具有药物活性的2-取代-5-氧代-5H-二苯并[8α，d {9环庚烯的酯，及其用途的方法和组合物
公开(公告)号：US4112114A
公开(公告)日：1978-09-05
申请号：US830264
申请日：1977-09-02
申请人： Peter H. Nelson , Karl G. Untch
发明人： Peter H. Nelson , Karl G. Untch
IPC分类号： C07C51/09 , C07C51/36 , C07C63/66 , C07D303/16 , C07D317/24 , C07D317/32 , C07D317/36
CPC分类号： C07D317/36 , C07C51/09 , C07C51/36 , C07C63/66 , C07D303/16 , C07D317/24 , C07D317/32
摘要： Esters of 2-substituted-5-oxo-5H-dibenzo[a,d]cycloheptenes represented by the following formula: ##STR1## where R' is --CH.sub.2 --CH.dbd.CH.sub.2, --CH.sub.2 --CH(OH)--CH.sub.2 OH, ##STR2## where Y is either O or S, or ##STR3## where R.sup.4 and R.sup.5 are independently hydrogen, alkyl having 1 to 6 carbon atoms, phenyl, or benzyl, or together R.sup.4 and R.sup.5 form an alkylene bridge having 4, 5 or 6 carbon atoms; one of R.sup.2 and R.sup.3 is hydrogen and the other is hydrogen, methyl, or ethyl, or together R.sup.2 and R.sup.3 are methylene. The compounds have anti-inflammatory, analgesic, and antipyretic activities and, accordingly, are useful in the treatment of inflammation, pain and/or pyrexia.
摘要翻译：由下式表示的2-取代-5-氧代-5H-二苯并[a，d]环庚烯的酯：其中R'是-CH 2 -CH = CH 2，-CH 2 -CH（OH）-CH 2 OH，其中Y是O或S，或者其中R4和R5独立地是氢，具有1-6个碳原子的烷基，苯基或苄基，或者一起R4和R5形成具有4,5或6个亚烷基的桥碳原子 R2和R3中的一个是氢，另一个是氢，甲基或乙基，或者一起R2和R3是亚甲基。该化合物具有抗炎，镇痛和解热活性，因此可用于治疗炎症，疼痛和/或发热。

6. 发明授权

US3975540A 2-Substituted-5-oxo-5H-dibenzo(a,d)cycloheptenes, and derivatives thereof, and methods and compositions for the use thereof 失效
标题翻译： 2-取代的5-氧代-5H-二苯并（a，d）环庚烯及其衍生物及其用途的方法和组合物
公开(公告)号：US3975540A
公开(公告)日：1976-08-17
申请号：US572477
申请日：1975-04-28
申请人： Peter H. Nelson , Karl G. Untch
发明人： Peter H. Nelson , Karl G. Untch
IPC分类号： C07C51/09 , C07C51/487 , C07C51/493 , C07C63/331 , C07C63/66 , C07C65/36 , C07C65/38 , A61K31/185
CPC分类号： C07C65/38 , C07C51/09 , C07C51/487 , C07C51/493 , C07C63/331 , C07C63/66 , C07C65/36 , Y10S514/887 , Y10S514/916
摘要： 2-Substituted-5-oxo-5H-dibenzo[a,d]cycloheptenes represented by the following formula: ##SPC1##Where one of R.sup.2 and R.sup.3 is hydrogen, and the other is hydrogen, methyl, or ethyl, or together R.sup.2 and R.sup.3 are methylene; and R' and R.sup.4 are alkoxy, or together R' and R.sup.4 are =O, =NOH, =NNHCONH.sub.2, or alkylenedioxy of the formula --O--CH.sub.2 --(CR.sup.5.sub.2).sub.n --CH.sub.2 --O-- where n.sub.5 is O--2, R.sup.5 is hydrogen or methyl when n is 1, and R.sup.5 is hydrogen when n is 2, or one of R' and R.sup.4 is --OH and the other is (SO.sub.3 Y) where Y is sodium or potassium. The compounds have anti-inflammatory, analgesic and anti-pyretic activities and, accordingly, are useful in the treatment of inflammation, pain and pyrexia.
摘要翻译： 2-取代的5-氧代-5H-二苯并[a，d]环庚烯，由下式表示：

7. 发明授权

US4011243A Intermediate in the oxidative process for the preparation of 2-(5H-dibenzo[a,d]cyclohepten-5-on-2-yl)acetic, propionic and butyric acids 失效
标题翻译：用于制备2-（5H-二苯并（A，D）环己-5-烯-2-基）乙酸，丙酸和丁酸的氧化方法中的中间体
公开(公告)号：US4011243A
公开(公告)日：1977-03-08
申请号：US611054
申请日：1975-09-08
申请人： Peter H. Nelson , Karl G. Untch
发明人： Peter H. Nelson , Karl G. Untch
IPC分类号： C07C51/16 , C07C63/331 , C07C63/66 , C07D317/72 , C07F9/54
CPC分类号： C07D317/72 , C07C51/16 , C07C63/331 , C07C63/66 , C07F9/5456
摘要： 2-(5H-Dibenzo[a,d]cyclohepten-5-on-2-yl)acetic, propionic and butyric acids are prepared by oxidation of the corresponding 5-oxo- or ketal-protected oxoalcohols and aldehydes. The acid products exhibit anti-inflammatory, analgesic and anti-pyretic activity.

8. 发明授权

US4011241A An intermediate in the preparation of 2-(5H-dibenzo[a,d]cyclophepten-5-on-2-yl)acetic, propionic and butyric acids 失效
标题翻译：在2-（5H-二苯并（A，D）环己基-5-戊-2-烯基）乙酸，丙酸和丁酸的制备中的中间体
公开(公告)号：US4011241A
公开(公告)日：1977-03-08
申请号：US611053
申请日：1975-09-08
申请人： Peter H. Nelson , Karl G. Untch
发明人： Peter H. Nelson , Karl G. Untch
IPC分类号： C07C49/675 , C07C49/757 , C07C51/06 , C07C51/08 , C07C51/09 , C07C51/373 , C07C51/377 , C07C63/331 , C07C63/66 , C07D303/02 , C07D303/48
CPC分类号： C07D303/48 , C07C49/675 , C07C49/757 , C07C51/06 , C07C51/08 , C07C51/09 , C07C51/373 , C07C51/377 , C07C63/331 , C07C63/66 , C07D303/02
摘要： 2-(5H-Dibenzo[a,d]cyclohepten-5-on-2-yl)acetic, propionic and butyric acids, are prepared from glycidonitrile intermediates. The acid products exhibit anti-inflamatory, analgesic and anti-pyretic activity.
摘要翻译：由缩水甘油腈中间体制备2-（5H-二苯并[a，d]环庚烯-5-酮-2-基）乙酸，丙酸和丁酸。

9. 发明授权

US4100174A Process for the preparation of 2-(5H-dibenzo[a,d]cyclohepten-5-on-2-yl)acetic, propionic and butyric acids and intermediates 失效
标题翻译：制备2-（5H-二苯并{8a，d {9环庚烯-5-基-2-基）乙酸，丙酸和丁酸及其中间体的方法
公开(公告)号：US4100174A
公开(公告)日：1978-07-11
申请号：US748083
申请日：1976-12-06
申请人： Peter H. Nelson , Karl G. Untch
发明人： Peter H. Nelson , Karl G. Untch
IPC分类号： C07C49/675 , C07C49/757 , C07C51/06 , C07C51/08 , C07C51/09 , C07C51/373 , C07C51/377 , C07C63/331 , C07C63/66 , C07D303/02 , C07D303/48 , C07D317/72
CPC分类号： C07D303/48 , C07C49/675 , C07C49/757 , C07C51/06 , C07C51/08 , C07C51/09 , C07C51/373 , C07C51/377 , C07C63/331 , C07C63/66 , C07D303/02
摘要： 2-(5H-Dibenzo[a,d]cyclohepten-5-on-2-yl) acetic, propionic and butyric acids, are prepared from glycidonitrile intermediates.

10. 发明授权

US4051260A 2-Substituted-5-oxo-5H-dibenzo[a,d]cycloheptenes, and derivatives thereof, and methods and compositions for the use thereof 失效
标题翻译： 2-取代的-5-氧代-5H-二苯并（A，D）环己烯酮及其衍生物及其用途的方法和组合物
公开(公告)号：US4051260A
公开(公告)日：1977-09-27
申请号：US675095
申请日：1976-04-08
申请人： Peter H. Nelson , Karl G. Untch
发明人： Peter H. Nelson , Karl G. Untch
IPC分类号： C07C51/09 , C07C51/487 , C07C51/493 , C07C57/74 , C07C63/331 , C07C63/66 , C07C65/36 , C07C65/38 , C07C49/76 , A01N9/24
CPC分类号： C07C65/38 , C07C51/09 , C07C51/487 , C07C51/493 , C07C57/74 , C07C63/331 , C07C63/66 , C07C65/36 , Y10S514/889
摘要： 2-Substituted-5-oxo-5H-dibenzo[a,d]cycloheptenes represented by the following formula: ##STR1## where one of R.sup.2 and R.sup.3 is hydrogen, and the other is hydrogen, methyl, or ethyl, or together R.sup.2 and R.sup.3 are methylene; and R' and R.sup.4 are alkoxy, or together R' and R.sup.4 are .dbd.O, .dbd.NOH, .dbd.NNHCONH.sub.2, or alkylenedioxy of the formula --O--CH.sub.2 --(CR.sup.5.sub.2).sub.n --CH.sub.2 --O-- where n.sub.5 is O-2, R.sup.5 is hydrogen or methyl when n is 1, and R.sup.5 is hydrogen when n is 2, or one of R' and R.sup.4 is --OH and the other is (SO.sub.3 Y) where Y is sodium or potassium. The compounds have anti-inflammatory, analgesic and anti-pyretic activities and, accordingly, are useful in the treatment of inflammation, pain and pyrexia.

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