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31. 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。

32. 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。

33. 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：

34. 发明授权

US07432261B2 Anti-inflammatory phosphonate compounds 失效
标题翻译：抗炎膦酸盐化合物
公开(公告)号：US07432261B2
公开(公告)日：2008-10-07
申请号：US10833294
申请日：2004-04-26
申请人： Carina Cannizzaro , James Chen , Xiaowu Chen , Aesop Cho , Lee Chong , Maria Fardis , Craig Gibbs , Ralph F. Hirschmann , Thorsten Kirschberg , Christopher P. Lee , Kuei-Ying Lin , Richard L. Mackman , Peter H. Nelson , David A. Oare , Hyung-Jung Pyun , Adrian S. Ray , Rosemarie Sherlock , Sundaramoorthi Swaminathan , William J. Watkins , Jennifer R. Zhang
发明人： Carina Cannizzaro , James Chen , Xiaowu Chen , Aesop Cho , Lee Chong , Maria Fardis , Craig Gibbs , Ralph F. Hirschmann , Thorsten Kirschberg , Christopher P. Lee , Kuei-Ying Lin , Richard L. Mackman , Peter H. Nelson , David A. Oare , Hyung-Jung Pyun , Adrian S. Ray , Rosemarie Sherlock , Sundaramoorthi Swaminathan , William J. Watkins , Jennifer R. Zhang
IPC分类号： A61K31/60 , C07D237/00
CPC分类号： C07F9/65583 , A61K31/60 , A61K47/548 , C07F9/4006 , C07F9/4021 , C07F9/46 , C07F9/572 , C07F9/5728 , C07F9/65031 , C07F9/65038 , C07F9/650905 , C07F9/6524 , C07F9/653 , C07F9/65515 , C07F9/65517 , C07F9/65586 , C07F9/6561 , C07F9/65616
摘要： The invention is related to phosphorus substituted anti-inflammatory compounds, compositions containing such compounds, and therapeutic methods that include the administration of such compounds, as well as to processes and intermediates useful for preparing such compounds.
摘要翻译：本发明涉及磷取代的抗炎化合物，含有这些化合物的组合物，以及包括施用这些化合物的治疗方法以及可用于制备这些化合物的方法和中间体。

35. 发明授权

US5512568A Method of using 4-amino derivatives of 5-substituted mycophenolic acid 失效
标题翻译：使用5-取代霉酚酸的4-氨基衍生物的方法
公开(公告)号：US5512568A
公开(公告)日：1996-04-30
申请号：US198732
申请日：1994-02-18
申请人： David Morgans, Jr. , Eric B. Sjogren , David B. Smith , Francisco X. Talamas , Dean R. Artis , Alicia Cervantes , Todd R. Elworthy , Mario Fernandez , Fidencio Franco , Ronald C. Hawley , Teresa Lara , David G. Loughhead , Peter H. Nelson , John W. Patterson , Alejandra Trejo , Ann M. Waltos , Robert J. Weikert
发明人： David Morgans, Jr. , Eric B. Sjogren , David B. Smith , Francisco X. Talamas , Dean R. Artis , Alicia Cervantes , Todd R. Elworthy , Mario Fernandez , Fidencio Franco , Ronald C. Hawley , Teresa Lara , David G. Loughhead , Peter H. Nelson , John W. Patterson , Alejandra Trejo , Ann M. Waltos , Robert J. Weikert
IPC分类号： A61K31/34 , A61K31/365 , A61K31/38 , A61K31/40 , A61K31/4025 , A61P17/00 , A61P29/00 , A61P37/06 , C07D307/88 , C07D405/06 , C07D407/06 , C07D409/06 , A61K31/535
CPC分类号： C07D405/06 , C07D307/88 , C07D407/06 , C07D409/06
摘要： The disclosed derivatives of mycophenolic acid are therapeutic agents advantageous in the treatment of disease states indicated for mycophenolic acid and/or mycophenolate mofetil and other immunosuppressant agents.
摘要翻译：公开的霉酚酸衍生物是治疗针对霉酚酸和/或霉酚酸酯和其它免疫抑制剂的疾病状态的治疗剂。

36. 发明授权

US4727069A Heterocyclic aminoalkyl esters of mycophenolic acid, derivatives thereof and pharmaceutical compositions 失效
标题翻译：霉酚酸的杂环氨基烷基酯，其衍生物和药物组合物
公开(公告)号：US4727069A
公开(公告)日：1988-02-23
申请号：US8909
申请日：1987-01-30
申请人： Peter H. Nelson , Chee-Liang L. Gu , Anthony C. Allison , Elsie M. Eugui , William A. Lee
发明人： Peter H. Nelson , Chee-Liang L. Gu , Anthony C. Allison , Elsie M. Eugui , William A. Lee
IPC分类号： C07D307/88 , A61K31/535 , A61K31/55 , C07D295/14
CPC分类号： C07D307/88
摘要： Heterocyclic aminoalkyl esters of mycophenolic acid, and the derivatives and pharmaceutically acceptable salts thereof, are useful as immunosuppressive agents, anti-inflammatory agents, anti-tumor agents, anti-viral agents, and anti-psoriatic agents.
摘要翻译：霉酚酸的杂环氨基烷基酯及其衍生物和药学上可接受的盐可用作免疫抑制剂，抗炎剂，抗肿瘤剂，抗病毒剂和抗牛皮癣剂。

37. 发明授权

US4725622A Mycophenolic acid derivatives in the treatment of rheumatoid arthritis 失效
标题翻译：霉酚酸衍生物治疗类风湿关节炎
公开(公告)号：US4725622A
公开(公告)日：1988-02-16
申请号：US821633
申请日：1986-01-23
申请人： Peter H. Nelson , Anthony C. Allison , Elsie M. Eugui , Joseph M. Muchowski
发明人： Peter H. Nelson , Anthony C. Allison , Elsie M. Eugui , Joseph M. Muchowski
IPC分类号： C07D307/88 , A61K31/44
CPC分类号： C07D307/88
摘要： A method of treating rheumatoid arthritis which method comprises administering to a mammal in need of such treatment a therapeutically effective amount of a compound of the formula: ##STR1## and the pharmaceutically acceptable salts thereof, wherein:A is oxygen or sulfur;R.sup.1 is selected from the group consisting of H, ##STR2## in which Y is oxygen or sulfur:R.sup.2 is alkyl, haloalkyl or --NR.sup.4 R.sup.5, where R.sup.4 and R.sup.5 are independently H, alkyl, haloalkyl, cycloalkyl, phenyl optionally monosubstituted with halogen, hydroxy, carboxy, chlorocarbonyl, sulfonylamino, nitro, cyano, phenyl, alkyl, acyl, alkoxycarbonyl, acylamino, dialkylamino or dialkylaminoethoxycarbonyl, phenyl optionally disubstituted with hydroxy, carboxy, nitro or alkyl, or benzyl optionally substituted with dialkylamino;n is an integer from 0-6;R.sup.3 is H alkyl or a pharmaceutically acceptable cation;Q and R are independently H or --CO.sub.2 R.sup.3 ; andZ is selected from the group consisting of ##STR3## in which X is oxygen or sulfur,R.sup.7 is H, alkyl, alkenyl, cycloalkyl, optionally substituted phenyl, optionally substituted benzyl or a pharmaceutically acceptable cation; andR.sup.8 and R.sup.9 are independently H, alkyl or cycloalkyl, or R.sup.8 and R.sup.9 taken together are --(CH.sub.2).sub.4 --, --(CH.sub.2).sub.5 -- or --(CH.sub.2).sub.2 O(CH.sub.2).sub.2 --;with the proviso that R.sup.1 and R.sup.7 cannot both be H if X and A are oxygen.
摘要翻译：治疗类风湿性关节炎的方法，该方法包括向需要这种治疗的哺乳动物施用治疗有效量的下式化合物及其药学上可接受的盐，其中：A为氧或硫; 其中Y是氧或硫：R 2是烷基，卤代烷基或-NR 4 R 5，其中R 4和R 5独立地是H，烷基，卤代烷基，环烷基，任选被卤素单取代的苯基，羟基，羧基，氯代羰基，磺酰基氨基，硝基，氰基，苯基，烷基，酰基，烷氧基羰基，酰氨基，二烷基氨基或二烷基氨基乙氧基羰基，任选被羟基，羧基，硝基或烷基二取代的苯基或任选被二烷基氨基取代的苄基; n是0-6的整数; R3是H烷基或药学上可接受的阳离子; Q和R独立地是H或-CO 2 R 3; Z选自CH 2 OH，CHO，CN，1H-四唑基，其中X是氧或硫，R 7是H，烷基，烯基，环烷基，任选取代的苯基，任选取代的苄基或药学上可接受的阳离子并且R 8和R 9独立地为H，烷基或环烷基，或者R 8和R 9一起为 - （CH 2）4 - ， - （CH 2）5 - 或 - （CH 2）2 O（CH 2）2 - 条件是如果X和A是氧，则R1和R7不能都是H。

38. 发明授权

US4512990A Benzthiazine analogs as antiinflammatory agents 失效
标题翻译：苯并噻嗪类似物作为抗炎剂
公开(公告)号：US4512990A
公开(公告)日：1985-04-23
申请号：US349738
申请日：1982-02-18
申请人： Peter H. Nelson , Howard J. Ringold , Stefan H. Unger , Thomas R. Thieme
发明人： Peter H. Nelson , Howard J. Ringold , Stefan H. Unger , Thomas R. Thieme
IPC分类号： C07D215/06 , C07D215/08 , C07D279/16 , A61K31/54
CPC分类号： C07D279/16 , C07D215/06 , C07D215/08
摘要： Compounds of the formula: ##STR1## and the pharmaceutically acceptable acid addition salts thereof, wherein: Z is S;Y is halo, alkoxy, alkyl, or dialkylamino;a is 0, 1 or 2;b is an integer from 2-12 with the proviso that if b is 2 or 3, a cannot be 0, and with the further proviso that if X is OH, b cannot be 2-5 and with the further proviso that if X is --NH.sub.2, b cannot be 2-5; andX is selected from the group consisting of: --OH, OR.sup.1, --NH.sub.2, --NHR.sup.1, NR1/2, ##STR2## and --NHCONHR.sup.2 in which each R.sup.1 is independently alkyl or cycloalkyl or, in --NR1/2, both R.sup.1 s together are alkylene or form a piperazine ring optionally substituted at the ring N by alkyl or --CH.sub.2 CH.sub.2 OH; andR.sup.2 is alkyl, cycloalkyl, or optionally substituted phenyl;have antiinflammatory properties and are useful in the treatment of conditions characterized by inflammation and swelling.
摘要翻译：下式的化合物：其中：Z是S;和其药学上可接受的酸加成盐。 Y是卤素，烷氧基，烷基或二烷基氨基; a是0,1或2; b为2-12的整数，条件是如果b为2或3，则a不能为0，另外条件是如果X为OH，则b不能为2-5，进一步的条件是，如果X为 -NH2，b不能为2-5; 并且X选自：-OH，OR 1，-NH 2，-NHR 1，NR 1/2，＆lt; IMAGE＆gt;和-NHCONHR 2，其中每个R 1独立地为烷基或环烷基，或在-NR 1/2中，一起是亚烷基或形成在环N任选被烷基或-CH 2 CH 2 OH取代的哌嗪环; 并且R 2是烷基，环烷基或任选取代的苯基; 具有抗炎性质，可用于治疗以炎症和肿胀为特征的病症。

39. 发明授权

US4059611A Oxidative process for the preparation of 2-(5H-dibenzo[a,d]cyclohepten-5-on-2-yl)acetic, propionic and butyric acid 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，丙酸和丁酸的氧化方法
公开(公告)号：US4059611A
公开(公告)日：1977-11-22
申请号：US702651
申请日：1976-07-06
申请人： Peter H. Nelson , Karl G. Untch
发明人： Peter H. Nelson , Karl G. Untch
IPC分类号： C07C59/86 , C07C309/73 , C07C143/68 , C07C65/14 , C07C83/00
CPC分类号： C07C59/86 , C07C309/73
摘要： 2-(5H-Dibenzo[a,d]cyclohepten-5-on-2-yl) acetic, propionic and butyric acid, and esters and salts thereof, are prepared by oxidation of non-ketonic 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非酮中间体的氧化制备。

40. 发明授权

US4035509A Methods and compositions for the use of 2-carboxy-5-oxo-5H-dibenzo[a,d]cycloheptenes, salts and esters thereof 失效
标题翻译：使用2-羧基-5-氧代-5H-二苯并{8a，d {9环庚烯，其盐和酯的方法和组合物
公开(公告)号：US4035509A
公开(公告)日：1977-07-12
申请号：US564001
申请日：1975-03-31
申请人： Peter H. Nelson , Karl G. Untch
发明人： Peter H. Nelson , Karl G. Untch
IPC分类号： C07C51/00 , C07C51/41 , C07C63/331 , C07C63/66 , C07C65/36 , C07C65/38 , C07C67/00 , C07C69/76 , C07C213/00 , C07C219/14 , A61K31/19 , A61K31/205 , A61K31/235
CPC分类号： C07C65/38 , C07C51/412 , C07C63/331 , C07C63/66 , C07C65/36 , Y10S514/825 , Y10S514/826 , Y10S514/885
摘要： 2-Substituted-5-oxo-5H-dibenzo[a,d]cycloheptenes represented by the following formula: ##STR1## where R' is hydrogen, alkyl having 1 to 12 carbon atoms, or ##STR2## where n is an integer from 2 to 4, inclusive, and R.sup.4 and R.sup.5 are independently lower alkyl having 1 to 6 carbon atoms or together R.sup.4 and R.sup.5 and the nitrogen atom to which they are attached form a heterocyclic ring having 5 or 6 total ring atoms; and the pharmaceutically acceptable salts thereof. The compounds are useful in the treatment of auto-immune diseases and allergic reactions.
摘要翻译：由下式表示的2-取代的5-氧代-5H-二苯并[a，d]环庚烯：其中R'是氢，具有1至12个碳原子的烷基或其中n是从 R 4和R 5独立地为具有1至6个碳原子的低级烷基，或者与R 4和R 5一起，并且与它们相连的氮原子形成具有5或6个总环原子的杂环; 及其药学上可接受的盐。该化合物可用于治疗自身免疫疾病和过敏反应。

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