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1. 发明申请

WO1991016894A1 QUINOLIZINONE TYPE COMPOUNDS 审中-公开
标题翻译：喹诺酮类化合物
公开(公告)号：WO1991016894A1
公开(公告)日：1991-11-14
申请号：PCT/US1991002998
申请日：1991-05-01
申请人： ABBOTT LABORATORIES , CHU, Daniel, T. , LEE, Cheuk, M. , LI, Qun , COOPER, Curt, S. , PLATTNER, Jacob, J.
发明人： ABBOTT LABORATORIES
IPC分类号： A61K31/54
CPC分类号： C07D471/04 , A61K38/00 , C07D213/68 , C07D455/02 , C07K5/06026
摘要： Novel compounds are disclosed having formula (I) as well as pharmaceutically acceptable salts, esters and amides thereof, wherein R is selected from (a) loweralkyl, (b) loweralkenyl, (c) halo(loweralkyl), (d) loweralkoxy, (e) cycloalkyl of from 3 to 8 carbons, (f) phenyl, (g) halo, (h) cyano, (i) nitro, (j) bicycloalkyl, (k) loweralkynyl, (l) alkoxycarbonyl, (m) nitrogen-containing aromatic heterocycle and (n) a group of the formula -NR R ; R is selected from the group consisting of halogen, loweralkoxy, carbocyclic aryloxy or carbocyclic aryl(loweralkyl)oxy, loweralkyl, loweralkenyl, cycloalkyl of from 3 to 8 carbons, cycloalkenyl of from 4 to 8 carbons, carbocyclic aryl(loweralkyl), cycloalkyl(loweralkyl), phenyl, amino, (loweralkyl)amino, carbocyclic aryl(loweralkyl)amino, hydroxy-substituted (loweralkyl)amino, nitrogen-containing aromatic heterocycle, bicyclic nitrogen-containing heterocycle and nitrogen-containing heterocycle having formula (II), wherein x is 0 to 3; R is selected from (a)-(CH2)m-, wherein m is 1, 2 or 3, and (b) -(CH2)nR (CH2)p-, wherein R is selected from S, O and N, n is 1 or 2, and p is 1 or 2; and Y is a non-hydrogen substituent independently selected from loweralkyl, halo(loweralkyl), loweralkoxy, hydroxy-substituted loweralkyl, hydroxy, amino(loweralkyl), halogen and a group having the formula -NR R ; R is hydrogen, halogen or loweralkoxy; R is selected from the group consisting of hydrogen, loweralkyl, a pharmaceutically acceptable cation and a prodrug ester group; R is selected from the group consisting of hydrogen, halogen, hydroxy, loweralkyl, halo(loweralkyl), loweralkoxy and a group having the formula -NR R ; and A is N or CR , wherein R is selected from hydrogen, halogen, loweralkyl, halo(loweralkyl), hydroxy-substituted loweralkyl, loweralkoxy(loweralkyl), loweralkoxy and amino(loweralkyl) or, alternatively, R and R , taken together with the atoms to which they are attached, form a 6-membered saturated ring which may contain an oxygen or a sulfur atom and which may be substituted with loweralkyl; with the proviso that when R is hydrogen and A is CH then either (a) R is NR R , or (b) R is a group having formula (III), wherein x is 1-3 and R and Y are as defined above.
摘要翻译：公开了具有式（I）化合物及其药学上可接受的盐，酯和酰胺的新型化合物，其中R 1选自（a）低级烷基，（b）低级链烯基，（c）卤代（低级烷基），（d）（f）苯基，（g）卤素，（h）氰基，（i）硝基，（j）双环烷基，（k）低级炔基，（I）烷氧基羰基，（m））含氮芳族杂环和（n）式-NR 7 R 8的基团; R 2选自卤素，低级烷氧基，碳环芳氧基或碳环芳基（低级烷基）氧基，低级烷基，低级烯基，3至8个碳的环烷基，4至8个碳的环烯基，碳环芳基（低级烷基），环烷基（低级烷基），苯基，氨基，（低级烷基）氨基，碳环芳基（低级烷基）氨基，羟基取代的（低级烷基）氨基，含氮芳族杂环，双环含氮杂环和含有式），其中x为0至3; R 9选自（a） - （CH 2）m - ，其中m为1,2或3，和（b） - （CH 2）n R 10（CH 2）p - ，其中R 10为选自S，O和N，n为1或2，p为1或2; 并且Y是独立地选自低级烷基，卤代（低级烷基），低级烷氧基，羟基取代的低级烷基，羟基，氨基（低级烷基），卤素和具有式-NR 11 R 12的基团的非氢取代基。 R 3是氢，卤素或低级烷氧基; R 4选自氢，低级烷基，药学上可接受的阳离子和前药酯基; R 5选自氢，卤素，羟基，低级烷基，卤代（低级烷基），低级烷氧基和具有式-NR 13 R 14的基团。并且A是N或CR 6，其中R 6选自氢，卤素，低级烷基，卤代（低级烷基），羟基取代的低级烷基，低级烷氧基（低级烷基），低级烷氧基和氨基（低级烷基），或者，R 1和R 6与它们所连接的原子一起形成可含有氧或硫原子并且可以被低级烷基取代的6元饱和环; 条件是当R 5为氢且A为CH时，则（a）R 1为NR 7 R 8，或（b）R 2为具有式（III）的基团，，其中x为1-3且R 9和Y如上所定义。

2. 发明申请

WO1992003136A1 QUINOBENZOXAZINE, QUINOBENZOTHIAZINE, AND PYRIDO-ACRIDINE ANTINEOPLASTIC AGENTS 审中-公开
标题翻译：喹诺酮类，喹诺酮类和吡虫啉类抗生素
公开(公告)号：WO1992003136A1
公开(公告)日：1992-03-05
申请号：PCT/US1991006040
申请日：1991-08-23
申请人： ABBOTT LABORATORIES , CHU, Daniel, T. , PLATTNER, Jacob, J. , HALLAS, Robert
发明人： ABBOTT LABORATORIES
IPC分类号： A61K31/44
CPC分类号： C07D455/00 , C07D513/06 , Y02P20/55
摘要： Quinobenzoxazine, quinobenzothiazines, and pyrido-acridine derivatives of formula (I), as well as the pharmaceutically acceptable salts, esters, amides and prodrugs thereof are disclosed, wherein R is hydrogen or a carboxy-protecting group, R and R are substituents, A is oxygen, sulfur, or carbon, Z is a halogen or a nitrogen-containing group, X is hydrogen, halogen or alkyl, and W is hydrogen, alkyl, amino or halogen. The compounds have potent antineoplastic activity.
摘要翻译：公开了式（I）的喹苯并恶嗪，醌苯并噻嗪和吡啶并吖啶衍生物，以及其药学上可接受的盐，酯，酰胺和前药，其中R 1是氢或羧基保护基，R 2，和R 3是取代基，A是氧，硫或碳，Z是卤素或含氮基团，X是氢，卤素或烷基，W是氢，烷基，氨基或卤素。这些化合物具有有效的抗肿瘤活性。

3. 发明申请

WO1990003971A1 NON-PEPTIDE RENIN INHIBITORS 审中-公开
标题翻译：非肽RENIN抑制剂
公开(公告)号：WO1990003971A1
公开(公告)日：1990-04-19
申请号：PCT/US1989004385
申请日：1989-10-03
申请人： ABBOTT LABORATORIES , FUNG, Anthony, K., L. , BAKER, William, R. , ARMIGER, Yoek-Lin , ROSENBERG, Saul, H. , DE, Biswanath , PLATTNER, Jacob, J. , BOYD, Steven, A. , KEMPF, Dale, J. , SHAM, Hing, Leung , KLEINERT, Hollis, D. , MANTEI, Robert, A.
发明人： ABBOTT LABORATORIES
IPC分类号： C07D233/56
CPC分类号： C07D233/64 , C07C237/08 , C07C317/28 , C07C323/58 , C07C2601/14 , C07D203/18 , C07D211/44 , C07D211/62 , C07D211/96 , C07D295/185 , C07D401/12 , C07D407/12 , C07D413/12
摘要： A renin inhibiting compound of formula (I), wherein A is a substituent; R1 is hydrogen, loweralkyl, substituted loweralkyl or loweralkenyl; X is CH2, CHOH, C(O), O, S, S(O), SO2, NH, N(O) or -P(O)O-; R3 is loweralkyl, loweralkenyl or substituted loweralkyl; and T is mimic of the Leu-Val cleavage site of angiotensinogen; or a pharmaceutically acceptable salt, ester or prodrug thereof.

4. 发明申请

WO1989010752A1 RETROVIRAL PROTEASE INHIBITORS 审中-公开
标题翻译：替代蛋白酶抑制剂
公开(公告)号：WO1989010752A1
公开(公告)日：1989-11-16
申请号：PCT/US1989002055
申请日：1989-05-12
申请人： ABBOTT LABORATORIES , KEMPF, Dale, J. , PLATTNER, Jacob, J. , NORBECK, Daniel, W. , BOYD, Steven, A. , BAKER, William, R. , ERICKSON, John, W. , FUNG, Anthony, K., L. , CROWLEY, Steven, R.
发明人： ABBOTT LABORATORIES
IPC分类号： A61K37/02
CPC分类号： C07D239/10 , A61K38/00 , C07C271/22 , C07C317/44 , C07C323/60 , C07C2601/06 , C07C2601/14 , C07D233/32 , C07D263/06 , C07D263/20 , C07D263/22 , C07D263/24 , C07D263/26 , C07D265/06 , C07D273/00 , C07D295/205 , C07D295/215 , C07D307/58 , C07D307/68 , C07D317/36 , C07D333/38 , C07D413/06 , C07K5/06026 , C07K5/06043 , C07K5/06078 , C07K5/101 , C07K5/1016 , C07K7/02
摘要： A retroviral protease inhibiting compound of formula (I) or a pharmaceutically acceptable salt, prodrug or ester thereof.

5. 发明申请

WO1989010751A1 FUNCTIONALIZED PEPTIDYL AMINODIOLS AND -TRIOLS 审中-公开
标题翻译：功能性肽肽氨基酸
公开(公告)号：WO1989010751A1
公开(公告)日：1989-11-16
申请号：PCT/US1989001931
申请日：1989-05-05
申请人： ABBOTT LABORATORIES , ROSENBERG, Saul, H. , DELLARIA, Joseph, F. , PLATTNER, Jacob, J. , BAKER, William, R.
发明人： ABBOTT LABORATORIES
IPC分类号： A61K37/02
CPC分类号： C07K5/06191 , A61K38/00 , C07K5/0227 , C07K5/06078
摘要： A renin inhibiting compound of formula (I) or a pharmaceutically acceptable salt, ester or prodrug thereof.

6. 发明申请

WO1999045389A2 LIGAND SCREENING AND DESIGN BY X-RAY CRYSTALLOGRAPHY 审中-公开
标题翻译：通过X射线晶体学的配镜筛选和设计
公开(公告)号：WO1999045389A2
公开(公告)日：1999-09-10
申请号：PCT/US1999004518
申请日：1999-03-01
申请人： ABBOTT LABORATORIES
发明人： ABBOTT LABORATORIES , NIENABER, Vicki, L. , GREER, Jonathan , ABAD-ZAPATERO, Celerino , NORBECK, Daniel, W.
IPC分类号： G01N33/50
CPC分类号： G01N33/6845 , C07K2299/00 , C30B7/00 , G01N23/20 , G01N33/68 , G01N33/6803 , G01N33/6842 , G01N2333/9723 , G01N2500/00
摘要： X-ray crystallography can be used to screen compounds that are not known ligands of a target biomolecule for their ability to bind the target biomolecule. The method includes obtaining a crystal of a target biomolecule; exposing the target biomolecule crystal to one or more test samples; and obtaining an X-ray crystal diffraction pattern to determine whether a ligand/receptor complex is formed. The target is exposed to the test samples by either co-crystallizing a biomolecule in the presence of one or more test samples or soaking the biomolecule crystal in a solution of one or more test samples. In another embodiment, structural information from ligand/receptor complexes are used to design ligands that bind tighter, that bind more specifically, that have better biological activity or that have better safety profile. A further embodiment of the invention comprises identifying or designing biologically-active moieties by the instant process. In a further embodiment, a biomolecule crystal having an easily accessible active site is formed by co-crystallizing the biomolecule with a degradable ligand and degrading the ligand.
摘要翻译：可以使用X射线晶体学来筛选目标生物分子的未知配体的化合物，以获得其结合目标生物分子的能力。该方法包括获得目标生物分子的晶体; 将目标生物分子晶体暴露于一个或多个测试样品; 并获得X射线晶体衍射图，以确定是否形成配体/受体复合物。通过在一个或多个测试样品的存在下共生结晶生物分子或将生物分子晶体浸泡在一个或多个测试样品的溶液中，将靶标暴露于测试样品。在另一个实施方案中，来自配体/受体复合物的结构信息用于设计更紧密结合的配体，其更具体地结合，具有更好的生物活性或具有更好的安全性。本发明的另一个实施方案包括通过本方法识别或设计生物活性部分。在另一个实施方案中，通过使生物分子与可降解配体共结晶并使配体降解而形成具有易于接近的活性位点的生物分子晶体。

7. 发明申请

WO1998031699A1 CRYSTAL FORM 0 OF CLARITHROMYCIN 审中-公开
标题翻译：克拉霉素的晶体形式0
公开(公告)号：WO1998031699A1
公开(公告)日：1998-07-23
申请号：PCT/US1997023607
申请日：1997-12-19
申请人： ABBOTT LABORATORIES
发明人： ABBOTT LABORATORIES , SPANTON, Stephen, G. , HENRY, Rodger, F. , RILEY, David, A. , LIU, Jih-Hua
IPC分类号： C07H17/08
CPC分类号： C07H17/08
摘要： The present invention concerns the novel antibiotic 6-O-methylerythromycin A form 0 solvate of formula (I), a process for its preparation, pharmaceutical compositions comprising this compound and a method of use as a therapeutic agent.
摘要翻译：本发明涉及式（I）的新型抗生素6-O-甲基红霉素A型0溶剂合物，其制备方法，包含该化合物的药物组合物和用作治疗剂的方法。

8. 发明申请

WO1998031698A1 PROCESS FOR PREPARATION OF 4-DEOXYERYTHROMYCINS A AND B 审中-公开
标题翻译：制备4-去氧肉桂素A和B的方法
公开(公告)号：WO1998031698A1
公开(公告)日：1998-07-23
申请号：PCT/US1997023356
申请日：1997-12-18
申请人： ABBOTT LABORATORIES
发明人： ABBOTT LABORATORIES , PAREKH, Shyamal, I. , GRAHAM, Alexandra, E. , DiPIERRO, Michael, J. , THOMAS, Albert, V. , RILEY, David, A.
IPC分类号： C07H17/08
CPC分类号： C07H17/08
摘要： A process for the preparation of 4''-deoxyerythromycins, having formula (I), wherein R is H or OH, Rp is H or acetyl, and R is H or loweralkyl; by treatment of the 2'-O-acetyl-4''-imidazolylthionocarbonyl-erythromycin starting material with the radical initiator 4,4'-azobis-(4-cyanovaleric acid), H3PO2 and an organic base in a water-miscible solvent other than an alcohol, and optionally eliminating the 2'-O-acetyl group. In a preferred embodiment, the water-miscible solvent is an alcohol and the deoxygenation and deacetylation is carried out in one step.
摘要翻译：制备具有式（I）的4“ - 脱氧红霉素的方法，其中R为H或OH，Rp为H或乙酰基，R 1为H或低级烷基; 通过用自由基引发剂4,4'-偶氮双（4-氰基戊酸），H 3 PO 2和有机碱在水混溶性溶剂中处理2'-O-乙酰基-4“ - 咪唑基硫羰基 - 红霉素原料并且任选地除去2'-O-乙酰基。在优选的实施方案中，水混溶性溶剂是醇，脱氧和脱乙酰化在一个步骤中进行。

9. 发明申请

WO1998028979A1 A PROCESS FOR INHIBITING STEM ELONGATION IN BULBOUS PLANTS 审中-公开
标题翻译：一种阻止植物生长发育的过程
公开(公告)号：WO1998028979A1
公开(公告)日：1998-07-09
申请号：PCT/US1997022919
申请日：1997-12-12
申请人： ABBOTT LABORATORIES
发明人： ABBOTT LABORATORIES , VENBURG, Gregory, D. , HANSEN, James, R. , WOOLARD, Derek, D. , SHAFER, Warren, E. , BLACK-SCHAEFER, Candace
IPC分类号： A01N37/44
CPC分类号： A01N37/36 , A01N37/44
摘要： A process of inhibiting stem elongation in ornamental bulbous plants or to cut flowers from such plants, involving treating such plants or flowers with an effective amount of ACC synthase inhibitor, such as aminoethoxyvinylglycine and aminooxyacetic acid to inhibit stem elongation, by administration of a solid, semi-solid or a solution of such ACC synthase inhibitor.
摘要翻译：一种抑制装饰性球茎植物茎茎伸长或从这些植物切花的方法，涉及用有效量的ACC合成酶抑制剂如氨基乙氧基乙烯基甘氨酸和氨基氧乙酸处理这样的植物或花，以抑制茎伸长，通过施用固体，半固体或这种ACC合酶抑制剂的溶液。

10. 发明申请

WO1998025665A1 ANESTHETIC VAPORIZER DRAINING SYSTEM 审中-公开
标题翻译： ANESTHETIC VAPORIZER排水系统
公开(公告)号：WO1998025665A1
公开(公告)日：1998-06-18
申请号：PCT/US1997022462
申请日：1997-12-09
申请人： ABBOTT LABORATORIES
发明人： ABBOTT LABORATORIES , GRABENKORT, Richard, W.
IPC分类号： A61M16/18
CPC分类号： A61M16/183 , A61M2205/6045
摘要： A system is provided for draining an anesthetic agent from a reservoir of an anesthetic vaporizer. The system includes an anesthetic agent container having an inlet into which the agent can drain. The vaporizer has a draining station that defines an outlet and that defines a drain passage between the vaporizer reservoir and the outlet. A valve is operable to open and close the drain passage. A connector is provided with a receiving end for connecting to the draining station at the outlet. The connector has a discharge end for connecting to the container inlet. The connector holds the container below the draining station outlet and defines a transfer passage between the receiving end and the discharge end for draining the agent from the draining station into the container. Structural key configurations, uniquely associated with a specific anesthetic, are preferably provided at the connection of the container and connector and at the connection of the draining station and connector.
摘要翻译：提供一种用于从麻醉蒸发器的储存器排出麻醉剂的系统。该系统包括具有入口的麻醉剂容器，药剂可以排出入口。蒸发器具有限定出口并且在蒸发器储存器和出口之间限定排放通道的排水站。阀可操作以打开和关闭排水通道。连接器设置有用于连接到出口处的排水站的接收端。连接器具有用于连接到容器入口的排放端。连接器将容器保持在排水站出口下方，并且在接收端和排放端之间限定了一个传送通道，用于将试剂从排水站排出到容器中。优选地，在容器和连接器的连接处以及在排水站和连接器的连接处提供与特定麻醉剂唯一相关联的结构关键构造。

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