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11. 发明申请

US20020040002A1 Hydroxamic acids substituted by heterocycles useful for inhibition of tumor necrosis factor 审中-公开
标题翻译：被用于抑制肿瘤坏死因子的杂环取代的羟氨酸
公开(公告)号：US20020040002A1
公开(公告)日：2002-04-04
申请号：US09814119
申请日：2001-03-22
申请人： ZENECA LIMITED
发明人： Thomas Geoffrey Colerick Bird
IPC分类号： A61K038/05 , C07D239/72 , C07D235/04 , C07D217/06 , C07D215/38
CPC分类号： C07D215/227 , C07D209/38 , C07D215/14 , C07D239/90 , C07D241/42 , C07D263/56 , C07D265/36 , C07D277/64
摘要： 1 Compounds of formula (I), wherein: n is 1 to 6; Het is a nitrogen containing ring fused to the benzene ring on two adjacent carbon atoms to form a bicyclic ring system which ring system may be optionally substituted; R1 is hydrogen, C1-8alkyl, C2-6alkenyl, C2-6alkynyl, C3-8cycloalkyl, aryl, heteroaryl, heterocyclyl, arylC1-6alkyl, heteroarylC1-6alkyl, heterocyclylC1-6alkyl or C3-8cycloalkylC1-6alkyl; R2 is C1-6alkyl, C2-6alkenyl, arylC1-6alkyl, heteroarylC1-6alkyl or the side-chain of a naturally occurring amino acid; R3 is hydrogen, C1-6alkyl, C3-8cycloalkyl, C4-8cycloalkenyl, arylC1-6alkyl, heteroarylC1-6alkyl or heterocyclylC1-6alkyl; R4 is hydrogen or C1-6alkyl; or R3 and R4 together with the nitrogen atom to which they are joined form a heterocyclic ring; wherein any group or ring, in R1-R4, is optionally substituted; and pharmceutically acceptable salts and in vivo hydrolysable esters thereof, are described as inhibitors of the production of Tumour Necrosis Factor and/or one or more matrix metalloproteinase enzymes. Compositions containing them and their preparation are also described.
摘要翻译：式（I）化合物，其中n为1至6; Het是与两个相邻碳原子上的苯环稠合的含氮环，形成环系统可以任选取代的双环体系; R 1是氢，C 1-8烷基，C 2-6烯基，C 2-6炔基，C 3-8环烷基，芳基，杂芳基，杂环基，芳基C 1-6烷基，杂芳基C 1-6烷基，杂环基C 1-6烷基或C 3-8环烷基C 1-6烷基; R 2是C 1-6烷基，C 2-6烯基，芳基C 1-6烷基，杂芳基C 1-6烷基或天然存在的氨基酸的侧链; R 3是氢，C 1-6烷基，C 3-8环烷基，C 4-8环烯基，芳基C 1-6烷基，杂芳基C 1-6烷基或杂环基C 1-6烷基; R4是氢或C1-6烷基; 或R 3和R 4与它们所连接的氮原子一起形成杂环; 其中R 1 -R 4中的任何基团或环任选被取代; 和药学上可接受的盐和其体内可水解的酯被描述为产生肿瘤坏死因子和/或一种或多种基质金属蛋白酶的抑制剂。还描述了含有它们的组合物及其制备方法

12. 发明授权

US6165777A Process for the resolution of cis 1,2-indane diols using Pseudomonas putida 失效
标题翻译：使用恶臭假单胞菌解决顺式1,2-二氢化茚二醇的方法
公开(公告)号：US6165777A
公开(公告)日：2000-12-26
申请号：US93875
申请日：1998-06-09
申请人： Christopher Curtis Royston Allen , Derek Raymond Boyd , Howard Dalton
发明人： Christopher Curtis Royston Allen , Derek Raymond Boyd , Howard Dalton
IPC分类号： C12P41/00 , C12R1/40 , C07C00/00
CPC分类号： C12P41/002 , Y02P20/582 , Y10S435/877
摘要： A process for resolution of a mixture of dihydroxydihydroindene enantiomers comprising treating the mixture of enantiomers with a Pseudomonas putida species microorganism.Resolved dihydroxydihydroindenes are valuable intermediates for the synthesis of biologically active compounds such as pharmaceuticals and agrochemicals.
摘要翻译：一种解决二羟基二氢茚对映异构体混合物的方法，包括用恶臭假单胞菌种微生物处理对映异构体混合物。分解的二羟基二氢茚是用于合成生物活性化合物如药物和农药的有价值的中间体。

13. 发明授权

US6156904A Process 失效
标题翻译：处理
公开(公告)号：US6156904A
公开(公告)日：2000-12-05
申请号：US469822
申请日：1999-12-22
申请人： Martin Charles Bowden , Stephen Martin Brown
发明人： Martin Charles Bowden , Stephen Martin Brown
IPC分类号： C07D277/20 , C07D277/36
CPC分类号： C07D277/36
摘要： 5-Chloro-2-(4,4-difluorobutylthio)thiazole is prepared from 2-mercaptotriazole by a multistep process involving S-alkylation, chlorination and dehydrochlorination and is converted by oxidation to the corresponding sulfone which is useful as an agricultural nematicide.
摘要翻译：通过涉及S-烷基化，氯化和脱氯化氢的多步法由2-巯基三唑制备5-氯-2-（4,4-二氟丁基硫代）噻唑，并通过氧化转化成可用作农业杀线虫剂的相应的砜。

14. 发明授权

US6149843A Microcapsules containing suspensions of biologically active compounds and ultraviolet protectant 失效
公开(公告)号：US6149843A
公开(公告)日：2000-11-21
申请号：US120965
申请日：1998-07-22
申请人： Herbert B. Scher , Jin Ling Chen
发明人： Herbert B. Scher , Jin Ling Chen
IPC分类号： A01N25/04 , A01N25/22 , A01N25/28 , A01N25/30 , A01N37/38 , A01N41/10 , A01N43/70 , A01N53/00 , B01J13/02 , B01J13/04 , B01J13/18 , A01N25/34
CPC分类号： B01J13/18 , A01N25/04 , A01N25/22 , A01N25/28 , A01N37/38 , A01N41/10 , A01N43/70 , A01N53/00 , B01J13/02 , B01J13/04
摘要： Microcapsules containing a biologically active material which is sensitive to ultraviolet light are prepared which contain an ultraviolet light protectant selected from titanium dioxide, zinc oxide and mixtures thereof, suspended and thoroughly dispersed in a liquid.

15. 发明授权

US06147083A Azospiro compounds as NK1 or NK2 antagonists 失效
标题翻译： Azospiro化合物作为NK1或NK2拮抗剂
公开(公告)号：US06147083A
公开(公告)日：2000-11-14
申请号：US384444
申请日：1999-08-27
申请人： Keith Russell
发明人： Keith Russell
IPC分类号： C07D211/14 , C07D211/52 , C07D295/13 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12 , C07D417/12 , C07D491/04 , C07D491/10 , C07D495/04 , C07D521/00 , A61K31/44
CPC分类号： C07D295/13 , C07D211/14 , C07D211/52 , C07D231/12 , C07D233/56 , C07D249/08 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12 , C07D417/12 , C07D491/04 , C07D491/10 , C07D495/04
摘要： Compounds of formula I: ##STR1## wherein Q.sup.1, Q.sup.2, Q.sup.3, Q.sup.4, and Q.sup.5 have any of the meanings given in the specification, their N-oxides, and their pharmaceutically acceptable salts are nonpeptide antagonists of SP and NKA are useful for the treatment of asthma, etc. Also disclosed are pharmaceutical compositions, processes for preparing the compounds of formula I and intermediates.
摘要翻译：式I化合物：其中Q1，Q2，Q3，Q4和Q5具有本说明书中给出的任何含义，其N-氧化物及其药学上可接受的盐是SP和NKA的非肽拮抗剂，可用于治疗哮喘等等。还公开了药物组合物，制备式I化合物的方法和中间体。

16. 发明授权

US6103721A Heteroaryl-substituted pyridazino quinoline compounds 失效
标题翻译：杂芳基取代的哒嗪喹啉化合物
公开(公告)号：US6103721A
公开(公告)日：2000-08-15
申请号：US455096
申请日：1999-12-06
申请人： Thomas Michael Bare , Timothy Wayne Davenport , James Roy Empfield , Jeffrey Alan McKinney , Richard Bruce Sparks
发明人： Thomas Michael Bare , Timothy Wayne Davenport , James Roy Empfield , Jeffrey Alan McKinney , Richard Bruce Sparks
IPC分类号： A61K31/50 , A61K31/5025 , A61P3/08 , A61P3/10 , A61P9/10 , A61P25/00 , A61P25/08 , A61P25/28 , A61P43/00 , C07D215/56 , C07D221/00 , C07D221/04 , C07D237/00 , C07D471/04 , C07D471/14 , C07D495/14
CPC分类号： C07D471/04 , C07D215/56
摘要： The present invention concerns compounds according to the following formula, ##STR1## wherein: R.sup.1 is (CH.sub.2).sub.n,L where n is an integer in the range 0 to 6, and L is a carbon-linked five-membered heteroaryl ring having an oxygen or sulfur heteroatom, R.sup.4 is hydrogen, halo or NO.sub.2, and pharmaceutical compositions and methods of using thereof in the treatment and/or prevention of neurological diseases or conditions.
摘要翻译：本发明涉及根据下式的化合物，其中：R1是（CH2）n，L，其中n是0-6的整数，L是具有氧或硫的碳连接的五元杂芳基环杂原子，R4是氢，卤素或NO2，以及其用于治疗和/或预防神经疾病或病症的药物组合物和方法。

17. 发明授权

US6100258A Aromatic amine compounds that antagonize the pain enhancing effects of prostaglandins 失效
标题翻译：拮抗前列腺素疼痛增强作用的芳香胺化合物
公开(公告)号：US6100258A
公开(公告)日：2000-08-08
申请号：US973915
申请日：1997-12-16
申请人： Gloria Anne Breault
发明人： Gloria Anne Breault
IPC分类号： A61K31/44 , A61K31/4427 , A61K31/455 , A61K31/465 , A61K31/50 , A61P25/04 , A61P29/00 , C07D213/80 , C07D213/82 , C07D237/18 , C07D237/24 , C07D401/04 , C07D403/04 , C07D413/04 , C07D413/12 , C07D417/12 , A61K31/5377
CPC分类号： C07D213/80 , C07D213/82 , C07D237/18 , C07D237/24 , C07D401/04 , C07D403/04 , C07D413/04 , C07D413/12 , C07D417/12
摘要： Compounds antagonistic of the pain enhancing effects of prostaglandins are disclosed. The compounds comprise an optionally-substituted A ring with a --CH(R.sup.3)N(R.sup.2)B--R.sup.1 and --OD groups positioned in a 1,2 relationship to one another on ring carbon atoms. The 3-position ring-atom is not substituted. B is also an optionally-substituted ring and the group R.sup.1 is positioned on B in a 1,3 or 1,4 relationship with the --CH(R.sup.3)N(R.sup.2)-- linking group. R.sup.1, R.sup.2 and R.sup.3 and D can be a number of different organic or halogen moieties. N-oxides of --NR.sup.2 and S-oxides of sulphur containing rings are disclosed as are processes for the preparation of the compounds, intermediates in their preparation, pharmaceutical compositions containing them, and their use as therapeutic agents.
摘要翻译： PCT No.PCT / GB96 / 01443 Sec。 371日期：1997年12月16日 102（e）日期1997年12月16日PCT Filed 1996年6月17日PCT公布。公开号WO97 / 00864 日期1997年1月9日公开了对前列腺素疼痛增强作用的拮抗作用。这些化合物包括在环碳原子上具有-CH 2（R 3）N（R 2）B-R 1和-OD基团彼此相关的任意取代的A环。 3位环原子不被取代。 B也是任选取代的环，并且基团R 1与-CH（R 3）N（R 2） - 连接基以1,3或1,4个关系位于B上。 R1，R2和R3和D可以是许多不同的有机或卤素部分。公开了NR2的N-氧化物和含硫环的S-氧化物，作为制备化合物的方法，其制备中的中间体，含有它们的药物组合物及其作为治疗剂的用途。

18. 发明授权

US6090813A Use of oxido-squalene cyclase inhibitors to lower blood cholesterol 失效
标题翻译：使用氧化 - 角鲨烯环化酶抑制剂降低血液胆固醇
公开(公告)号：US6090813A
公开(公告)日：2000-07-18
申请号：US11718
申请日：1998-02-13
申请人： David Waterson , Elaine Sophie Elizabeth Stokes , George Robert Brown , Robin Wood
发明人： David Waterson , Elaine Sophie Elizabeth Stokes , George Robert Brown , Robin Wood
IPC分类号： C07D239/42 , A61K31/00 , A61K31/4427 , A61K31/4433 , A61K31/445 , A61K31/4465 , A61K31/4523 , A61K31/4545 , A61K31/495 , A61K31/496 , A61K31/505 , A61K31/506 , A61K31/55 , A61K31/551 , A61K31/5513 , A61P9/00 , A61P31/00 , A61P31/10 , A61P43/00 , C07D213/74 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/04 , C07D409/14 , C07D413/14 , A01N43/60
CPC分类号： C07D401/04 , A61K31/496 , A61K31/506 , C07D401/14 , C07D409/14 , C07D413/14
摘要： A compound of formula (I), or a pharmaceutically acceptable salt thereof, wherein G, T.sup.1, T.sup.2 and T.sup.3 are selected from CH and N; provided that T.sup.2 and T.sup.3 are not both CH; A is selected from a direct bond and (1-4C)alkylene; X is selected from oxy, thio, sulphinyl, sulphonyl, carbonyl, carbonylamino, N-di-(1-6C)alkylcarbonylamino, sulphonamido, methylene, (1-4C)alkylmethylene and di-(1-6C)alkylmethylene, and when T.sup.2 is CH, X may also be selected from aminosulphonyl and oxycarbonyl; and Q is selected from (5-7C)cycloalkyl, a heterocyclic moiety containing up to 4 heteroatoms selected from nitrogen, oxygen and sulphur, phenyl, naphthyl, phenyl(1-4C)alkyl and phenyl(2-6C)alkenyl; for the manufacture of a medicament for treating diseases or medical conditions in which an inhibition of oxido-squalene cyclase is desirable. ##STR1##
摘要翻译： PCT No.PCT / GB96 / 01985 Sec。 371日期1998年2月13日 102（e）1998年2月13日PCT PCT 1996年8月14日PCT公布。公开号WO97 / 06802 日期：1997年2月27日一种式（I）化合物或其药学上可接受的盐，其中G，T1，T2和T3选自CH和N; 只要T2和T3都不是CH; A选自直接键和（1-4C）亚烷基; X选自氧基，硫基，亚磺酰基，磺酰基，羰基，羰基氨基，N-二 - （1-6C）烷基羰基氨基，磺酰氨基，亚甲基，（1-4C）烷基亚甲基和二 - （1-6C）烷基亚甲基，当T2 是CH，X也可以选自氨基磺酰基和氧羰基; 且选自（5-7C）环烷基，含有至多4个选自氮，氧和硫的杂原子的杂环部分，苯基，萘基，苯基（1-4C）烷基和苯基（2-6C）烯基; 用于制备治疗需要抑制氧化 - 角鲨烯环化酶的疾病或医学病症的药物。

19. 发明授权

US6084103A One pot synthesis of 2-oxazolidinone derivatives 失效
标题翻译：一锅合成2-恶唑烷酮衍生物
公开(公告)号：US6084103A
公开(公告)日：2000-07-04
申请号：US11045
申请日：1998-05-13
申请人： Rajnikant Patel
发明人： Rajnikant Patel
IPC分类号： A61K31/00 , A61K31/42 , A61K31/421 , A61K31/422 , A61P25/00 , A61P25/06 , C07B61/00 , C07C20060101 , C07C215/06 , C07C219/06 , C07C219/32 , C07C269/04 , C07C269/06 , C07C271/16 , C07C271/20 , C07C271/22 , C07D20060101 , C07D209/14 , C07D263/20 , C07D413/06 , C07D263/04 , C07D263/16
CPC分类号： C07D263/20 , C07C271/20 , C07C271/22 , C07D413/06
摘要： The present invention provides an improved process for preparing (S)-4-{[3-[2-(dimethylamino)ethyl]-1H-indol-5-yl]methyl}-2-oxazolidinone which comprises: a) forming a carbamate of formula (III), from methyl 4-nitro-(L)-phenylalaninate hydrochloride; b) reducing the compound of formula (III) to give the compound of formula (IV); c) reducing the methyl ester grouping in the compound of formula (IV) to give the compound of formula (V); d) ring closure of the compound of formula (V) to give the compound of formula (VI); e) diazonium salt formation from the compound of formula (VI) followed by reduction to give the compound of formula (VII); f) Fischer reaction of the compound of formula (VII) to give (S)-4-{[3-[2-(dimethylamino)ethyl]-1H-indol-5-yl]methyl}-2-oxazolidinone.
摘要翻译： PCT No.PCT / GB96 / 01885 Sec。 371日期1998年5月13日 102（e）日期1998年5月13日PCT提交1996年8月2日PCT公布。出版物WO97 / 06162 日期：1997年2月20日本发明提供了制备（S）-4 - {[3- [2-（二甲基氨基）乙基] -1H-吲哚-5-基]甲基} -2-恶唑烷酮的改进方法，其包括： a）由4-硝基 - （L） - 苯丙氨酸甲酯盐酸盐形成式（III）的氨基甲酸酯; b）还原式（III）化合物以得到式（Ⅳ）化合物; c）还原式（IV）化合物中的甲酯基团，得到式（Ⅴ）化合物; d）式（Ⅴ）化合物闭环，得到式（Ⅵ）化合物; e）由式（VI）化合物形成重氮盐，然后还原，得到式（Ⅶ）化合物; f）式（VII）化合物与（S）-4 - {[3- [2-（二甲基氨基）乙基] -1H-吲哚-5-基]甲基} -2-恶唑烷酮的费休反应。

20. 发明授权

US6072080A Purification process 失效
标题翻译：净化过程
公开(公告)号：US6072080A
公开(公告)日：2000-06-06
申请号：US41858
申请日：1998-03-12
申请人： Louie Akos Nady , Seyed Mehdi Tavana , Thomas Gray , Stephen Martin Brown , Brian David Gott
发明人： Louie Akos Nady , Seyed Mehdi Tavana , Thomas Gray , Stephen Martin Brown , Brian David Gott
IPC分类号： C07C201/16 , C07C205/00
CPC分类号： C07C201/16 , C07C311/51
摘要： A process for the purification of a compound of general formula I: ##STR1## wherein R.sup.1 is hydrogen or C.sub.1 -C.sub.6 alkyl, C.sub.2 -C.sub.6 alkenyl or C.sub.2 -C.sub.6 alkynyl, any of which may optionally be substituted with one or more substituents selected from halogen and hydroxy; or COOR.sup.4, COR.sup.6, CONR.sup.4 R.sup.5 or CONHSO.sub.2 R.sup.4 ;R.sup.4 and R.sup.5 independently represent hydrogen or C.sub.1 -C.sub.4 alkyl optionally substituted with one or more halogen atoms;R.sup.6 is a halogen atom or a group R.sup.4 ;R.sup.2 is hydrogen or halo; andR.sup.3 is C.sub.1 -C.sub.4 alkyl, C.sub.2 -C.sub.4 alkenyl or C.sub.2 -C.sub.4 alkynyl, any of which may optionally be substituted with one or more halogen atoms; or halo;or, where appropriate, a salt thereof;from a mixture containing the compound of general formula I together with one or more isomers or di-nitrated analogues thereof; the process comprising dissolving the mixture in a suitable crystallisation solvent and recrystallising the product from the resulting crystallisation solution wherein the crystallisation solution contains not more than 25% loading of the compound of general formula I, loading being defined as: ##EQU1## and wherein the temperature to which the solution is cooled for crystallisation is not greater than about 30.degree. C.; wherein, after the addition of the crystallising solvent but before recrystallisation, the crystallisation solution is subjected to at least one wash with an aqueous solution having an acid pH followed by back extraction with fresh crystallising solvent. The process is particularly useful for purifying acifluorfen produced via a route starting with m-cresol.
摘要翻译：一种用于纯化通式I化合物的方法：其中R 1是氢或C 1 -C 6烷基，C 2 -C 6烯基或C 2 -C 6炔基，其中任何一个可任选被一个或多个选自卤素和羟基的取代基取代 ; 或COOR4，COR6，CONR4R5或CONHSO2R4; R4和R5独立地表示氢或任选被一个或多个卤素原子取代的C 1 -C 4烷基; R6是卤素原子或基团R4; R2是氢或卤素; 并且R 3是C 1 -C 4烷基，C 2 -C 4烯基或C 2 -C 4炔基，其中任何一个可任选地被一个或多个卤素原子取代; 或卤素; 或者在适当情况下为其盐; 从含有通式I化合物的混合物与一种或多种异构体或其二硝化类似物组合; 该方法包括将该混合物溶解在合适的结晶溶剂中，并从所得结晶溶液中重结晶该产物，其中该结晶溶液含有不超过25％的通式I化合物的负载量，其定义为：并且其中该溶液冷却结晶不大于约30℃; 其中，在加入结晶溶剂之后但在重结晶之前，将结晶溶液用具有酸性pH的水溶液进行至少一次洗涤，然后用新鲜的结晶溶剂反萃取。该方法特别可用于纯化通过以间甲酚开始的途径产生的三氟果霜。

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