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11. 发明授权

US5120727A Rapamycin dimers 失效
标题翻译：雷帕霉素二聚体
公开(公告)号：US5120727A
公开(公告)日：1992-06-09
申请号：US706821
申请日：1991-05-29
申请人： Wenling Kao , Robert L. Vogel , John H. Musser
发明人： Wenling Kao , Robert L. Vogel , John H. Musser
IPC分类号： A61K31/445 , A61K31/395 , A61K31/435 , A61P29/00 , A61P31/04 , A61P31/10 , A61P35/00 , A61P37/06 , C07D498/12 , C07D498/18 , C07D519/00
CPC分类号： C07D498/18 , C07D519/00
摘要： A rapamycin dimer of general formula (1) ##STR1## wherein A is --(CH.sub.2).sub.n --, --(CH.sub.2)n--(CH.dbd.CH)--(CH.sub.2).sub.m --, --(CH.sub.2)n--(--C.tbd.C--)--(CH.sub.2).sub.m --, ##STR2## substituted alkyl, substituted alkenyl, substituted alkynyl, and substituted aromatic; n=1-10, m=1-10 and n=m or n .noteq.mor a pharmaceutically acceptable salt thereof, which is by virtue of its immunosuppressive activity is useful in treating transplantation rejection host vs. graft disease, autoimmune diseases, and diseases of inflammation.
摘要翻译：其中A为 - （CH 2）n - ， - （CH 2）n - （CH = CH） - （CH 2）m - ， - （CH 2）取代的烷基，被取代的烯基，被取代的炔基和被取代的芳族; n - （ - C 3 O） - （CH 2）m - ， - n = 1-10，m = 1-10，n = m或n由于其免疫抑制活性而引起的或其药学上可接受的盐可用于治疗移植排斥宿主与移植物疾病，自身免疫疾病和炎症疾病

12. 发明授权

US4769461A Quinolinyl benzene hydroxamic acids as anti-inflammatory/antiallergic agents 失效
标题翻译：喹啉基苯异羟肟酸作为抗炎/抗过敏剂
公开(公告)号：US4769461A
公开(公告)日：1988-09-06
申请号：US907933
申请日：1986-09-16
申请人： John H. Musser , Dennis M. Kubrak
发明人： John H. Musser , Dennis M. Kubrak
IPC分类号： C07D215/20 , C07D235/26 , C07D277/68 , C07D215/04 , C07D215/22 , C07D215/36 , C07D215/38
CPC分类号： C07D277/68 , C07D215/20 , C07D235/26
摘要： There are disclosed compounds of the formula ##STR1## wherein W represents a covalent bond or ##STR2## X is N or CR.sup.2 ; Y is O, S, NR.sup.2 or C(R.sup.2).sub.2 when n=0, or N or CR.sup.2 when n=1Z is ##STR3## R.sup.1 is hydrogen, lower alkyl, trifluoromethyl, nitro, hydroxy, lower alkoxy, mercapto, loweralkylthio or halo;R.sup.2 is hydrogen or lower alkyl;n is 0-1;m is 1-6 with the proviso that m is 0-5 when W represents a covalent bond;and the pharmaceutically acceptable salts thereof, and their use in the treatment of leukotriene-mediated naso-bronchial obstructive airpassageway conditions, such as allergic rhinitis, allergic bronchial asthma and the like, in psoriasis, ulcerative colitis, rheumatoid arthritis as well as in other immediate hypersensitivity reactions.
摘要翻译：公开了下式的化合物：其中W代表共价键，或者X是N或CR 2; 当n = 0时，Y为O，S，NR2或C（R2）2，当n = 1时为N或CR2，Z为氢，低级烷基，三氟甲基，硝基，羟基，低级烷氧基，巯基，低级烷硫基或卤素; R2是氢或低级烷基; n为0-1; m为1-6，条件是当W表示共价键时，m为0-5; 及其药学上可接受的盐，以及它们在治疗银屑病，溃疡性结肠炎，类风湿性关节炎以及其他立即治疗白三烯介导的鼻支气管阻塞性空气通道病症如过敏性鼻炎，过敏性支气管哮喘等中的用途超敏反应。

13. 发明授权

US4754043A Oxazole and thiazole naphthalenes as antiallergic agents 失效
标题翻译：恶唑和噻唑萘作为抗过敏剂
公开(公告)号：US4754043A
公开(公告)日：1988-06-28
申请号：US915444
申请日：1986-10-06
申请人： Anthony F. Kreft, III , John H. Musser , Thomas W. Pattison , John P. Yardley
发明人： Anthony F. Kreft, III , John H. Musser , Thomas W. Pattison , John P. Yardley
IPC分类号： C07D213/30 , C07D215/14 , C07D277/24 , C07D277/64 , C07D277/62 , C07D263/30 , C07D263/54 , C07D277/20
CPC分类号： C07D213/30 , C07D215/14 , C07D277/64
摘要： There are disclosed compounds of the formula ##STR1## wherein X is --CH.sub.2 CH.sub.2 --, --CH.dbd.CH--, ##STR2## Z is CR or N, where n=1; or Z is O,S, or NR, when n=0; R is hydrogen or loweralkyl;n is 0 or 1;R.sup.1 is hydroxy, amino, loweralkyl sulfonamido, perfluoro loweralkyl sulfonamido or OR;R.sup.2 is hydrogen or loweralkyl;R.sup.3 is hydrogen or loweralkyl; orR.sup.2 and R.sup.3 taken together form a benzene ring; andthe dotted line represents an optional double bond;and the pharmaceutically acceptable salts thereof, and their use in the treatment of leukotriene-mediated naso-bronchial obstructive airpassageway conditions, such as allergic rhinitis, allergic bronchial asthma and the like.
摘要翻译：公开了下式的化合物，其中X是-CH 2 CH 2 - ， - CH = CH-，Z是CR或N，其中n = 1; 或当N = 0时，Z为O，S或NR; R是氢或低级烷基; n为0或1; R1是羟基，氨基，低级烷基亚磺酰氨基，全氟低级烷基亚磺酰氨基或OR; R2是氢或低级烷基; R3是氢或低级烷基; 或R 2和R 3一起形成苯环; 虚线表示任选的双键; 及其药学上可接受的盐，以及它们在治疗白三烯介导的鼻支气管阻塞性空气通道病症如过敏性鼻炎，过敏性支气管哮喘等中的用途。

14. 发明授权

US4719308A Imidazolylmethoxy naphthalene compounds as antiallergic agents 失效
标题翻译：咪唑甲氧基萘化合物作为抗过敏剂
公开(公告)号：US4719308A
公开(公告)日：1988-01-12
申请号：US915443
申请日：1986-10-06
申请人： Anthony F. Kreft, III , John H. Musser , Thomas W. Pattison , John P. Yardley
发明人： Anthony F. Kreft, III , John H. Musser , Thomas W. Pattison , John P. Yardley
IPC分类号： C07D213/30 , C07D215/14 , C07D233/64 , C07D277/64
CPC分类号： C07D213/30 , C07D215/14 , C07D277/64
摘要： There are disclosed compounds of the formula ##STR1## wherein X is --CH.sub.2 CH.sub.2 --, --CH.dbd.CH--, ##STR2## Z is CR or N, when n=1; or Z is O, S, or NR, when n=0, R is hydrogen or loweralkyl;n is 0 or 1;R.sup.1 is hydroxy, amino, loweralkyl sulfonamido, perfluoro loweralkyl sulfonamido or OR;R.sup.2 is hydrogen or loweralkyl;R.sup.3 is hydrogen or loweralkyl; orR.sup.2 and R.sup.3 taken together form a benzene ring; andthe dotted line represents an optional double bond;and the pharmaceutically acceptable salts thereof, and their use in the treatment of leukotriene-mediated naso-bronchial obstructive airpassageway conditions, such as allergic rhinitis, allergic bronchial asthma and the like.
摘要翻译：公开了下式的化合物，其中当n = 1时，X是-CH 2 CH 2 - ， - CH = CH-，Z是CR或N; 或Z为O，S或NR，当n = 0时，R为氢或低级烷基; n为0或1; R1是羟基，氨基，低级烷基亚磺酰氨基，全氟低级烷基亚磺酰氨基或OR; R2是氢或低级烷基; R3是氢或低级烷基; 或R 2和R 3一起形成苯环; 虚线表示任选的双键; 及其药学上可接受的盐，以及它们在治疗白三烯介导的鼻支气管阻塞性空气通道病症如过敏性鼻炎，过敏性支气管哮喘等中的用途。

15. 发明授权

US4681940A 5-[3-[[2-quinolyl]methoxy]phenyl]-1,3-oxazoles 失效
标题翻译： 5- [3 - [[2-喹啉基]甲氧基]苯基] -1,3-恶唑
公开(公告)号：US4681940A
公开(公告)日：1987-07-21
申请号：US799673
申请日：1985-11-19
申请人： John H. Musser , Reinhold H. W. Bender
发明人： John H. Musser , Reinhold H. W. Bender
IPC分类号： C12N9/99 , A61K31/42 , A61K31/425 , A61K31/47 , A61P11/08 , A61P29/00 , A61P43/00 , C07D263/14 , C07D263/24 , C07D333/00 , C07D413/04 , C07D413/12 , C07D413/14 , C07D417/12
CPC分类号： C07D417/12 , C07D263/14 , C07D263/24 , C07D413/04 , C07D413/12 , C07D413/14
摘要： There are disclosed compounds of the formula ##STR1## wherein X is N or CR.sup.2Y is O, S, NR.sup.2, CHR.sup.2 or C(R.sup.2).sub.2 when n=0, or N or CR.sup.2 when n=1;p is 0-3;R.sup.1 is ##STR2## R.sup.2 is hydrogen or lower alkyl; R.sup.3 is hydrogen, lower alkyl, phenyl, thienyl, furyl, pyridyl, ##STR3## --C(R.sup.4).sub.3 or --(CH.sub.2).sub.p COOR.sup.2 ; R.sup.4 is halo;Z is O or S;and the pharmaceutically acceptable salts thereof, and their use in the treatment of luekotriene-mediated naso-bronchial obstructive airpassageway conditions, such as allergic rhinitis, allergic bronchial asthma and the like, in psoriasis, ulcerative colitis, rheumatoid arthritis as well as in other immediate hypersensitivity reactions.
摘要翻译：当n = 0时，公开了下式的化合物，其中当n = 0时，X是N或CR 2 Y是O，S，NR 2，CHR 2或C（R 2）2，或当n = 1时，N或CR 2; p为0-3; R1是氢或低级烷基; R3是氢，低级烷基，苯基，噻吩基，呋喃基，吡啶基，-C（R4）3或 - （CH2）pCOOR2; R4是卤素; Z是O或S; 及其药学上可接受的盐，以及它们在治疗牛皮癣，溃疡性结肠炎，类风湿性关节炎以及其他立即治疗氯代三烯介导的鼻支气管阻塞性空气通道病症如过敏性鼻炎，过敏性支气管哮喘等中的用途超敏反应。

16. 发明授权

US4594425A Heterocyclic compounds as antiallergic agents 失效
标题翻译：杂环化合物作为抗过敏剂
公开(公告)号：US4594425A
公开(公告)日：1986-06-10
申请号：US578444
申请日：1984-02-09
申请人： John H. Musser , Dennis M. Kubrak
发明人： John H. Musser , Dennis M. Kubrak
IPC分类号： C07D277/64 , C07D277/68 , C07D307/80 , C07D277/82 , A61K31/42 , A61K31/425 , C07D263/58
CPC分类号： C07D277/68 , C07D277/64 , C07D307/80
摘要： There are disclosed compounds of the formula ##STR1## n is 0-6; A is O or S;B is OR.sup.2, SR.sup.2 or N(R.sup.2).sub.2 ;R.sup.1 is hydrogen, loweralkyl, loweralkoxy or halo;R.sup.2 is hydrogen or loweralkyl;and the pharmaceutically acceptable salts thereof, and their use in the treatment of leukotriene-mediated naso-bronchial obstructive airpassageway conditions, such as allergic rhinitis, allergic bronchial asthma and the like.
摘要翻译：公开了下式的化合物：其中 + TR n为0-6; A是O或S; B为OR2，SR2或N（R2）2; R1是氢，低级烷基，低级烷氧基或卤素; R2是氢或低级烷基; 及其药学上可接受的盐，以及它们在治疗白三烯介导的鼻支气管阻塞性空气通道病症如过敏性鼻炎，过敏性支气管哮喘等中的用途。

17. 发明授权

US4581457A Heterocyclic sulfonamides 失效
标题翻译：杂环磺酰胺
公开(公告)号：US4581457A
公开(公告)日：1986-04-08
申请号：US653733
申请日：1984-09-21
申请人： John H. Musser , Dennis M. Kubrak
发明人： John H. Musser , Dennis M. Kubrak
IPC分类号： C07D235/12 , C07D277/64
CPC分类号： C07D235/12 , C07D277/64
摘要： There are disclosed compounds of the formula ##STR1## wherein X is ##STR2## W is ##STR3## Y is ##STR4## n is 0-8; R.sup.1 is hydrogen, loweralkyl, loweralkoxy, lower alkanoyl, halo, trifluoromethyl, cyano or nitro;R.sup.2 is hydrogen or loweralkyl;and the pharmaceutically acceptable salts thereof, and their use in the treatment of leukotriene-mediated naso-bronchial obstructive airpassageway conditions, such as allergic rhinitis, allergic bronchial asthma and the like, and in antithrombotic therapy.
摘要翻译：公开了下式的化合物：其中X是，Y是 + TR n是0-8; R 1是氢，低级烷基，低级烷氧基，低级烷酰基，卤素，三氟甲基，氰基或硝基; R2是氢或低级烷基; 及其药学上可接受的盐及其在治疗白三烯介导的鼻支气管阻塞性空气通道病症如过敏性鼻炎，过敏性支气管哮喘等以及抗血栓治疗中的用途。

18. 发明授权

US4563463A 2-Oxo-1,3-oxazolo[4,5-h] quinolines useful as anti-allergy agents 失效
标题翻译：可用作抗过敏剂的2-氧代-1,3-恶唑并[4,5-h]喹啉
公开(公告)号：US4563463A
公开(公告)日：1986-01-07
申请号：US667667
申请日：1984-11-02
申请人： John H. Musser , Richard E. Brown
发明人： John H. Musser , Richard E. Brown
IPC分类号： C07D215/28 , C07D498/04 , A61K31/47
CPC分类号： C07D215/28
摘要： New quinoline compound, and the corresponding 1,2-; 1,3-; and 1,4-benzodiazines, the quinoline compounds being of the formulae: ##STR1## and salts thereof, wherein R is hydrogen, acyl, carboethoxy,(3-methoxyphen)acetyl,(2-phenyl)propionyl, dimethylcarbamoyl or methyl,R.sub.1 and R.sub.2 are independently hydrogen, lower alkyl, halo, trifluoromethyl, amino, lower alkyl amino, lower acylamino, cyano, aryl, aryl/lower alkylene, nitro, lower alkynyl, lower alkenyl, lower alkyl sulfinyl, lower alkyl sulfonyl, lower alkoxycarbonyl, carboxyl, lower alkoxy, lower alkanoyl, or lower alkenoyl,Y is oxygen, sulfur, nitrogen or R.sub.3 N wherein R.sub.3 is hydrogen, lower alkyl, alkenyl, alkynyl, aryl, aralkyl, acyl, aminoalkyl, or carboxyalkyl,Z is oxygen, sulfur or nitrogen,X is cyano, carbalkoxy, carboxyl, formyloximino, tetrazolyl, carbalkoxyalkyl or carboxyalkyl, andm is 0 or 1, are useful as medicinals, especially for treatment of asthma, and/or as intermediates in the preparation of compounds useful for treating asthma.
摘要翻译：新喹啉化合物及相应的1,2-; 1,3- 其中R为氢，酰基，乙酰乙氧基，（3-甲氧基苯基）乙酰基，（2-苯基）丙酰基，二甲基氨基甲酰基或甲基，R 1，R 2，氰基，芳基，芳基/低级亚烷基，硝基，低级炔基，低级烯基，低级烷基亚磺酰基，低级烷基磺酰基，低级烷氧基羰基，低级烷基氨基，低级烷基氨基，羧基，低级烷氧基，低级烷酰基或低级烯酰基，Y是氧，硫，氮或R3N，其中R3是氢，低级烷基，烯基，炔基，芳基，芳烷基，酰基，氨基烷基或羧基烷基，Z是氧，硫或氮，X为氰基，烷氧羰基，羧基，甲酰肟基，四唑基，碳烷氧基烷基或羧基烷基，m为0或1，可用作药物，特别是用于治疗哮喘，和/或作为制备用于治疗哮喘的化合物的中间体。

19. 发明授权

US4552876A Bisbenzoxazines and pharmaceutical use 失效
标题翻译：双苯并恶嗪和药物用途
公开(公告)号：US4552876A
公开(公告)日：1985-11-12
申请号：US629285
申请日：1984-07-09
申请人： Howard Jones , Ernest Magnien , John H. Musser , Mujahid L. Shaikh
发明人： Howard Jones , Ernest Magnien , John H. Musser , Mujahid L. Shaikh
IPC分类号： C07D263/62 , C07D265/36 , A61K31/535
CPC分类号： C07D263/62 , C07D265/36
摘要： Compounds of the formula: ##STR1## wherein, R is H, alkyl, cycloalkyl, aryl, or heteroaryl;R.sub.1 is H, alkyl, cycloalkyl, aryl, heteroaryl, substituted heteroaryl, aralkyl, substituted aryl, halo, OR.sup.2, SR.sup.2, NR.sub.2, CF.sub.3, NO.sub.2, CN, COOR.sup.2, CHO, SO.sub.3 H or SO.sub.2 NH.sub.2,whereinR.sup.2 is H, methyl, ethyl or propyl;Y is ##STR2## Z is O, S, NH or CH.sub.2 ; X is --CH.sub.2 --, ##STR3## or --(CH.sub.2).sub.n CHOH(CH.sub.2).sub.n --; whereinR.sup.2 is H, methyl, ethyl or propyl;n is 1-10, and pharmaceutically acceptable salts thereof have antiallergy and antiinflammatory activity.
摘要翻译：下式的化合物：其中R为H，烷基，环烷基，芳基或杂芳基; R1是H，烷基，环烷基，芳基，杂芳基，取代的杂芳基，芳烷基，取代的芳基，卤素，OR2，SR2，NR2，CF3，NO2，CN，COOR2，CHO，SO3H或SO2NH2，其中R2是H，甲基，乙基或丙基; Z是O，S，NH或CH2; Y是 + TR 或者 - （CH 2）n CHOH（CH 2）n - ; - 其中R2是H，甲基，乙基或丙基; n为1-10，其药学上可接受的盐具有抗炎和抗炎活性。

20. 发明申请

US20120277146A1 Compounds For Enzyme Inhibition 审中-公开
标题翻译：化合物用于酶抑制
公开(公告)号：US20120277146A1
公开(公告)日：2012-11-01
申请号：US13411044
申请日：2012-03-02
申请人： Mark S. Smyth , Guy J. Laidig , Ronald T. Borchardt , Barry A. Bunin , Craig M. Crews , John H. Musser
发明人： Mark S. Smyth , Guy J. Laidig , Ronald T. Borchardt , Barry A. Bunin , Craig M. Crews , John H. Musser
IPC分类号： A61K38/07 , A61P31/18 , A61P25/28 , A61P31/12 , A61P35/00 , A61P31/00 , A61P29/00 , A61P37/00 , C07K5/107 , A61P21/00
CPC分类号： C07K5/1016 , C07K5/0812 , C07K5/0827
摘要： Peptide-based compounds including heteroatom-containing, three-membered rings efficiently and selectively inhibit specific activities of N-terminal nucleophile (Ntn) hydrolases. The activities of those Ntn having multiple activities can be differentially inhibited by the compounds described. For example, the chymotrypsin-like activity of the 20S proteasome may be selectively inhibited with the inventive compounds. The peptide-based compounds include at least three peptide units, an epoxide or aziridine, and functionalization at the N-terminus. Among other therapeutic utilities, the peptide-based compounds are expected to display anti-inflammatory properties and inhibition of cell proliferation.
摘要翻译：包括含杂原子的三元环的基于肽的化合物有效地选择性地抑制N末端亲核试剂（Ntn）水解酶的比活性。具有多种活性的那些Ntn的活性可被所描述的化合物差别地抑制。例如，本发明化合物可以选择性地抑制20S蛋白酶体的胰凝乳蛋白酶样活性。基于肽的化合物包括至少三个肽单元，环氧化物或氮丙啶，并且在N-末端官能化。除了其他治疗用途之外，预期基于肽的化合物显示抗炎性质和抑制细胞增殖。

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