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51. 发明授权

US6147230A Amino acid dysiherbaine 失效
标题翻译：氨基酸dysiherbaine
公开(公告)号：US6147230A
公开(公告)日：2000-11-14
申请号：US77371
申请日：1999-05-26
申请人： Keiko Shimamoto , Ryuichi Sakai , Hisao Kamiya , Michio Murata
发明人： Keiko Shimamoto , Ryuichi Sakai , Hisao Kamiya , Michio Murata
IPC分类号： A61K31/35 , A61K35/56 , A61P25/00 , A61P43/00 , C07D493/04 , C07D311/00
CPC分类号： C07D493/04
摘要： The present invention provides a novel amino acid dysiherbaine which is a non-NMDA type glutamate receptor agonist as well as salts and biological precursors thereof, which are useful as experimental materials for elucidating neuronal death or the functions of signal transduction of the central nervous system associated with glutamate receptors and which provide a possibility for the development of a glutamate receptor blocker.A novel amino acid dysiherbaine represented by the formula (1): ##STR1## is obtained by purifying an aqueous extract of a sponge such as D. herbacea on the basis of toxicity to mice by liquid chromatography using Sephadex LH20 or the like and HPLC using a C18 column, and optionally converting it into a biological precursor thereof.
摘要翻译： PCT No.PCT / JP97 / 03047 Sec。 371日期：1998年5月26日 102（e）日期1998年5月26日PCT 1997年9月1日提交PCT本发明提供了一种新型氨基酸异丁啡碱，其是非NMDA型谷氨酸受体激动剂及其盐和生物前体，其可用作实验材料阐明神经元死亡或与谷氨酸受体相关的中枢神经系统的信号转导的功能，并且其提供谷氨酸受体阻断剂发展的可能性。通过使用Sephadex LH20等进行液相色谱纯化基于对小鼠的毒性的海绵的含水提取物的纯化得到的式（1）所示的新型氨基酸异冰贴肉碱，使用C18柱，并且任选地将其转化为其生物前体。

52. 发明授权

US6114568A Process for alkylating hindered sulfonamides useful in the production of matrix metalloproteinase inhibitors 失效
标题翻译：用于生产基质金属蛋白酶抑制剂的受阻磺酰胺的烷基化方法
公开(公告)号：US6114568A
公开(公告)日：2000-09-05
申请号：US289454
申请日：1999-04-09
申请人： Brian Michael Andresen , Phillip Dietrich Hammen , Joel Michael Hawkins
发明人： Brian Michael Andresen , Phillip Dietrich Hammen , Joel Michael Hawkins
IPC分类号： A61K31/223 , A61K31/351 , A61P1/00 , A61P1/02 , A61P1/04 , A61P3/10 , A61P9/00 , A61P9/04 , A61P9/10 , A61P11/00 , A61P17/02 , A61P19/02 , A61P19/10 , A61P25/00 , A61P25/04 , A61P25/06 , A61P25/14 , A61P25/16 , A61P25/24 , A61P25/28 , A61P27/02 , A61P29/00 , A61P31/04 , A61P31/18 , A61P35/00 , A61P35/04 , A61P37/04 , A61P37/06 , A61P37/08 , A61P43/00 , B01J23/44 , C07B61/00 , C07C303/36 , C07C303/40 , C07C311/29 , C07C311/37 , C07D309/14 , C07D311/00 , C07D493/06 , C07D493/08
CPC分类号： C07D493/08 , C07C303/40 , C07C311/29 , C07D309/14 , Y02P20/55
摘要： The present invention relates to a process for alkylating hindered sulfonamides useful as intermediates in the preparation of matrix metalloproteinase inhibitors.
摘要翻译：本发明涉及在制备基质金属蛋白酶抑制剂中用作中间体的受阻磺酰胺的烷基化方法。

53. 发明授权

US6004971A Pentacyclic compounds, intermediates, processes, compositions, and methods 失效
标题翻译：五环化合物，中间体，方法，组合物和方法
公开(公告)号：US6004971A
公开(公告)日：1999-12-21
申请号：US878799
申请日：1997-06-19
申请人： Timothy Alan Grese
发明人： Timothy Alan Grese
IPC分类号： A61K31/00 , A61K31/35 , A61K31/352 , A61K31/38 , A61K31/381 , A61K31/47 , A61K31/473 , A61P3/00 , A61P3/06 , A61P5/30 , A61P5/32 , A61P19/00 , A61P19/10 , C07D221/04 , C07D221/18 , C07D311/00 , C07D311/78 , C07D493/04 , C07D495/04 , C07F7/18 , A61K31/44 , C07D471/22
CPC分类号： C07D493/04 , C07D221/04 , C07D221/18 , C07D311/00 , C07D311/78 , C07D495/04 , C07F7/1856 , C07F7/1892
摘要： The present invention provides compounds of formula I and II: ##STR1## wherein X is --O--, --S--, or --NR.sup.5 --;Y is --O--, --S--, --CH.sub.2 --, --Ch.sub.2 CH.sub.2 --, --CH.dbd.CH--, or --NR.sup.5 --;B is --CH.sup.2 -- or --CO--;R.sup.1, R.sup.2, and R.sup.3 are each independently --H, --OH, --O(C.sub.1 -C.sub.4 alkyl), --OCOC.sub.6 H.sub.5, --OCO(C.sub.1 -C.sub.6 alkyl), --OSO.sub.2 (C.sub.4 -C.sub.6 alkyl), --OSO.sub.2 CF.sub.3, Cl, or F;n is 1 or 2;W is CH.sub.2 or C.dbd.O;R.sup.4 is 1-piperidinyl, 2-oxo-1-piperidinyl, 1-pyrrolidinyl, methyl-1-pyrrolidinyl, dimethyl-1-pyrrolidinyl, 2-oxo-1-pyrrolidinyl, 4-morpholino, dimechylamino, diethylamino, or 1-hexamethyieneimino;R.sup.5 is C.sub.1 -C.sub.3 alkyl, --COC.sub.6 H.sub.5, --CO(C.sub.1 -C.sub.6 alkyl), --C(O)OC.sub.6 H.sub.5, --C(O)O(C.sub.1 -C.sub.6 alkyl), --SO.sub.2 (C.sub.1 -C.sub.6 alkyl), --SO.sub.2 C.sub.6 H.sub.5,or --SO.sub.2 CF.sub.3 ; or a pharmaceutically acceptable salt or solvate thereof.
摘要翻译：本发明提供式I和II的化合物：其中X是-O - ， - S - 或-NR 5 - ; Y是-O - ， - S - ， - CH 2 - ， - C 2 CH 2 - ， - CH = CH-或-NR 5 - ; B是-CH 2 - 或-CO-; R1，R2和R3各自独立地为-H，-OH，-O（C1-C4烷基），-OCOC6H5，-OCO（C1-C6烷基），-OSO2（C4-C6烷基），-OSO2CF3，或F; n为1或2; W是CH 2或C = O; R4是1-哌啶基，2-氧代-1-哌啶基，1-吡咯烷基，甲基-1-吡咯烷基，二甲基-1-吡咯烷基，2-氧代-1-吡咯烷基，4-吗啉代，二甲基氨基，二乙基氨基或1-六甲基亚氨基亚氨基 ; R5是C1-C3烷基，-COC6H5，-CO（C1-C6烷基），-C（O）OC6H5，-C（O）O（C1-C6烷基），-SO2（C1-C6烷基），-SO2C6H5 ，或-SO 2 CF 3; 或其药学上可接受的盐或溶剂合物。

54. 发明授权

US5597715A 7,42-Bis(O-demethyl)rapamycin 失效
标题翻译： 7,42-双（O-脱甲基）雷帕霉素
公开(公告)号：US5597715A
公开(公告)日：1997-01-28
申请号：US492129
申请日：1995-08-10
申请人： Brian D. Ford
发明人： Brian D. Ford
IPC分类号： A61K31/445 , A61P31/04 , A61P31/10 , A61P35/00 , A61P37/06 , C07D498/18 , C12N1/20 , C12P17/18 , C12R1/465 , A61K31/455 , C07D311/00
CPC分类号： C07D498/18 , C12P17/18
摘要： A compound of formula (I) is obtainable by the cultivation of a microorganism from the genus Streptomyces, such as Streptomyces NCIMB 40515. In the presence of rapamycin, and recovery thereof from the culture medium. The compound, and pharmaceutical compositions containing it, is useful as an immunomodulatory agent, as an anticancer agent, or in the treatment of microbial infections in animals including humans. ##STR1##
摘要翻译： PCT No.PCT / GB94 / 00269 Sec。 371日期：1995年8月10日 102（e）日期1995年8月10日PCT 1994年2月10日PCT PCT。 WO94 / 18208 PCT公开号日期1994年8月18日通过培养来自链霉菌属（Streptomyces）属的链霉菌属（Streptomyces）NCIMB 40515的微生物获得式（I）化合物。在雷帕霉素存在下，从培养基中回收。该化合物和含有它的药物组合物可用作免疫调节剂，作为抗癌剂，或用于治疗包括人在内的动物的微生物感染。（一）

55. 发明授权

US5164503A Preparation of aminocyclopentane acids 失效
标题翻译：氨基环戊酸的制备
公开(公告)号：US5164503A
公开(公告)日：1992-11-17
申请号：US698895
申请日：1991-05-13
申请人： Ian Waterhouse , David R. Marshall , Eric W. Collington , Christopher J. Wallis , Peter Hallett
发明人： Ian Waterhouse , David R. Marshall , Eric W. Collington , Christopher J. Wallis , Peter Hallett
IPC分类号： C07D295/08 , A61K31/44 , A61K31/535 , A61K31/5375 , A61P7/02 , A61P11/00 , C07D295/096 , C07D295/112 , C07D295/116 , C07D295/155 , C07D309/12 , C07D311/00 , C07D333/16 , C07D333/26
CPC分类号： C07D295/096 , C07D295/112 , C07D295/116 , C07D295/155 , C07D311/00
摘要： A process is described for the preparation of compounds of the formula ##STR1## in which W is C.sub.1-7 alkyleneX is cis or trans --CH.dbd.CH-- or --CH.sub.2 Ch.sub.2 --Y is a saturated heterocyclic amino group, andR.sup.2 is substituted or unsubstituted phenyl-, thienyl- or naphthyl-alkyl, or cinnamyl,and their salts and solvates.The process comprises hydrolysing a corresponding ester, amide, nitrile or ortho-ester. The starting materials are preferably prepared by reducing the corresponding cyclopentanone and hydrolysis can take place simultaneously with reduction.
摘要翻译：描述了制备式“IMAGE”的化合物的方法，其中W为C 1-7亚烷基X为顺式或反式-CH = CH-或-CH 2 CH 2 - Y为饱和杂环氨基，R 2为取代或未取代的苯基 - ，噻吩基或萘基 - 烷基或肉桂基，及其盐和溶剂合物。该方法包括水解相应的酯，酰胺，腈或原酸酯。原料优选通过还原相应的环戊酮制备，水解可以同时还原而进行。

56. 发明授权

US5081262A Substituted cyclopentenyl oxabicyclooctanes, cyclopentenylformylcyclohexenes and cyclopentenylhydroxymethyl cyclohexenes, processes for preparing same and organoleptic uses thereof 失效
标题翻译：取代的环戊烯基氧杂双环辛烷，环戊烯基甲酰基环己烯和环戊烯基羟甲基环己烯，其制备方法及其感官用途
公开(公告)号：US5081262A
公开(公告)日：1992-01-14
申请号：US588825
申请日：1990-09-27
申请人： Anubhav P. S. Narula , John J. De Virgilio , Carlos Benaim , Anton Van Ouwerkerk , Olivier Gillotin
发明人： Anubhav P. S. Narula , John J. De Virgilio , Carlos Benaim , Anton Van Ouwerkerk , Olivier Gillotin
IPC分类号： C07C13/20 , C07C29/14 , C07C33/14 , C07C45/69 , C07C45/75 , C07C47/225 , C07C47/44 , C07D311/00 , C07D493/08 , C11B9/00 , C11D3/50
CPC分类号： C11D3/50 , C07C29/14 , C07C33/14 , C07C45/69 , C07C45/75 , C07C47/225 , C07C47/44 , C07D493/08 , C11B9/003 , C11B9/0034 , C11B9/0076 , C12C11/02 , C07C2101/16
摘要： Described are cyclopentenyl-oxabicyclooctanes, cyclopentenyl-formylcyclohexenes and cyclopentyl-hydroxymethyl cyclohexenes having the generic structures: ##STR1## wherein R.sub.1, R.sub.2, R.sub.3 ', and R.sub.3 " each represents hydrogen or methyl with the provisos:(i) one or two of R.sub.1, R.sub.2, R.sub.3 ' and R.sub.3 " represents methyl;(ii) R.sub.1 and/or R.sub.2 are methyl;(iii) at least one of R.sub.3 ' and R.sub.3 " is hydrogen; and(iv) when R.sub.1 and R.sub.2 is methyl then each of R.sub.3 ' and R.sub.3 " is hydrogenwherein R.sub.4 ' is hydrogen or C.sub.1 -C.sub.5 alkyl, processes for preparing same and uses thereof in augmenting or enhancing the aroma of perfume compositions, colognes and perfumed articles, e.g., solid or liquid, anionic, cationic, nonionic or zwitterionic detergents, cosmetic preparations, fabric softener compositions, fabric softener articles, hair preparations and perfumed polymers.
摘要翻译：描述了具有以下通用结构的环戊烯基 - 氧杂双环辛烷，环戊烯基 - 甲酰基环己烯和环戊基 - 羟甲基环己烯：其中R 1，R 2，R 3'和R 3“各自表示氢或甲基与条件是：（i）R1，R2，R3'和R3“中的一个或两个表示甲基; （ii）R 1和/或R 2为甲基; （iii）R 3'和R 3“中的至少一个是氢; 和（iv）当R 1和R 2为甲基时，R 3'和R 3“中的每一个为氢，其中R 4'为氢或C 1 -C 5烷基，其制备方法及其用于增强或增强香料组合物香气，古龙香和香料制品，例如固体或液体阴离子，阳离子，非离子或两性离子洗涤剂，化妆品制剂，织物柔软剂组合物，织物柔软剂制品，毛发制品和加香聚合物。

57. 发明授权

US5055582A Process for preparing thromboxane A.sub.2 antagonists 失效
标题翻译：制备血栓素A2拮抗剂的方法
公开(公告)号：US5055582A
公开(公告)日：1991-10-08
申请号：US283639
申请日：1988-12-13
申请人： Robert B. Garland , Masateru Miyano
发明人： Robert B. Garland , Masateru Miyano
IPC分类号： C07C49/453 , C07C59/46 , C07C327/42 , C07D311/00
CPC分类号： C07D311/00 , C07C327/42 , C07C49/453 , C07C59/46 , C07C2103/68
摘要： This invention relates to a process for preparing useful thromboxane A.sub.2 inhibiting (.+-.)7-[3.alpha.-[1-[[(phenylamino)thioxomethyl]hydrazono]ethyl]-1.alpha.,4.alpha.-bicyclo[2.2.1]hept-2.beta.-yl]-heptenoic acids and useful derivatives thereof from (.+-.)octahydro-1.alpha.-methyl-3a.alpha.,7a.alpha.-4.alpha.,7.alpha.-methano-2H-inden-2-ones.
摘要翻译：本发明涉及一种制备有用的血栓素A2抑制（+/-）7- [3α-[1 - [[（苯基氨基）硫代甲基]亚肼基]乙基]-1α，4α-双环[2.2.1] （+/-）八氢-1α-甲基-3αα，7aα-4α，7α-甲基-2H-茚-2-酮的有用衍生物。

58. 发明授权

US5023262A Hydrogenated rapamycin derivatives 失效
标题翻译：氢化雷帕霉素衍生物
公开(公告)号：US5023262A
公开(公告)日：1991-06-11
申请号：US567858
申请日：1990-08-14
申请人： Craig E. Caufield , John H. Musser , James M. Rinker
发明人： Craig E. Caufield , John H. Musser , James M. Rinker
IPC分类号： A61K31/435 , A61K31/395 , A61P31/04 , A61P31/10 , C07D311/00 , C07D498/18 , C07H19/01
CPC分类号： C07D498/18 , C07H19/01
摘要： A derivative of rapamycin where one, two, or three of the double bonds at the 1-,3-, or 5-positions of rapamycin have been reduced to the corresponding alkane, or a pharmaceutically acceptable salt thereof, which by virtue of its antifungal activity is useful in treating fungal infections. ##STR1##
摘要翻译：雷帕霉素的衍生物，其中雷帕霉素的1-，3-或5-位上的一个，两个或三个双键已被还原成相应的烷烃或其药学上可接受的盐，由于其抗真菌活性可用于治疗真菌感染。

59. 发明授权

US4956480A 7-amino-4-methyl-coumarin-3-carboxyalkyl derivates and fluorescent conjugates thereof 失效
标题翻译： 7-氨基-4-甲基 - 香豆素-3-羧基烷基衍生物及其荧光共轭物
公开(公告)号：US4956480A
公开(公告)日：1990-09-11
申请号：US203453
申请日：1988-06-17
申请人： Don Robinson
发明人： Don Robinson
IPC分类号： G01N21/78 , C07D311/00 , C07D311/16 , C12Q1/00 , C12Q1/37 , G01N33/533
CPC分类号： G01N33/533 , C07D311/16 , C12Q1/37 , C12Q2337/22
摘要： A novel compound having the formula (I): ##STR1## or a reactive derivative or functional equivalent thereof, wherein m is an integer from 1 to 4, and R.sub.1 and R.sub.2 are same or different and selected from hydrogen and 1-4C alkyl; a fluorescent conjugate having the formula (III): ##STR2## wherein m R.sub.1 and R.sub.2 have the meaning given in claim 1, and R.sub.4 is a substituent attached to the keto group of formula (III) by a covalen bond. The new compounds and conjugates are usefual as fluorescent labelling agents.
摘要翻译： PCT No.PCT / SE86 / 00550 Sec。 371日期：1988年6月17日 102（e）日期1988年6月17日PCT Filted 1986年12月2日PCT公布。出版物WO87 / 03589 1987年6月18日，具有式（I）的新型化合物：其中m为1〜4的整数，R1和R2相同或不同。并选自氢和1-4C烷基; 具有式（III）的荧光共轭物：其中m R1和R2具有权利要求1中给出的含义，R4是通过共价键与式（III）的酮基连接的取代基。新化合物和缀合物作为荧光标记试剂是有用的。

60. 发明授权

US4939278A Herbicidal pyrones 失效
公开(公告)号：US4939278A
公开(公告)日：1990-07-03
申请号：US188800
申请日：1988-04-13
申请人： Janet E. Anderson-McKay , Andris J. Liepa
发明人： Janet E. Anderson-McKay , Andris J. Liepa
IPC分类号： A01N43/16 , A01N43/24 , C07D309/00 , C07D309/32 , C07D309/36 , C07D311/00 , C07D311/96 , C07D409/00 , C07D409/04 , C07D495/00 , C07D495/10
CPC分类号： C07D495/10 , A01N43/16 , A01N43/24 , C07D309/32 , C07D311/96
摘要： Compounds of the general formula (2) and isomeric and/or tautomeric forms thereof ##STR1## characterized in that R.sup.1 is selected from the group consisting of: hydrogen; alkyl; alkenyl; alkynyl; cycloalkyl; cycloalkenyl; substituted alkyl or substituted cycloalkyl wherein the alkyl or cycloalkyl group is substituted with a substituent selected from the group consisting of alkoxy, alkylthio, optionally substituted phenyl, optionally substituted heterocycle; optionally substituted phenyl; optionally substituted heterocycle, alkyl sulfonyl; optionally substituted benzene sulfonyl; an acyl group; and an inorganic or organic cation;R.sup.2 is selected from the group consisting of: alkyl; alkenyl; cycloalkyl; cycloalkenyl; haloalkenyl; alkynyl; haloalkynyl; substituted alkyl or substituted cycloalkyl wherein the alkyl or cycloalkyl group is substituted with a substituent selected from the group consisting of halogen, alkoxy, alkylthio, optionally substituted phenyl, and optionally substituted heterocycle; optionally substituted phenyl; and optionally substituted heterocycle;R.sup.3 is selected from the group consisting of: alkyl; haloalkyl; alkenyl; cycloalkyl; cycloalkenyl; alkynyl; and optionally substituted phenyl;R.sup.4 is selected from the group consisting of: alkynyl; haloalkyl; haloalkenyl; cycloalkyl; cycloalkenyl; substituted alkyl or substituted cycloalkyl wherein the alkyl or cycloalkyl group is substituted with a substituent selected from the group consisting of alkoxy, alkylthio, oxo, acyl, alkoxycarbonyl, (alkoxyimino) alkyl, ketal, carboxylic acid optionally substituted phenyl, and optionally substituted heterocycle; and optionally substituted heterocycle;R.sup.5 is selected from the group consisting of: alkyl; alkanyl; alkynyl; haloalkyl; haloalkenyl; cycloalkyl; cycloalkenyl; substituted alkyl or substituted cycloalkyl wherein the alkyl or cycloalkyl group is substituted with a substituent selected from the group consisting of alkoxy, alkylthio, oxo, acyl, alkoxycarbonyl, (alkoxyimino) alkyl, betal, carboxylic acid optionally substituted phenyl, and optionally substituted heterocycle; and optionally substituted heterocycle;orR.sup.4 and R.sup.5 together with the carbon to which they are attached form a substituted or unsubstituted saturated or partially saturated heterocyclic or carbocyclic ring containing 3 or more ring atoms, which ring may be bridged or fused and may contain substituents selected from the group consisting of hydrogen; alkyl; alkenyl; alkynyl; substituted alkyl wherein the alkyl group is substituted with a substituent selected from the group consisting of alkoxy, alkylthio, optionally substituted phenyl, and optionally substituted heterocycle; optionally substituted phenyl; and optionally substituted heterocycle; oxo; acyl; alkoxy; alkylthio; alkoxycarbonyl; (alkoxyimino) alkyl; ketal; and carboxylic acid.The compounds of formula (2) have herbicidal and plant growth regulating properties.

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