-
公开(公告)号：US5252579A
公开(公告)日：1993-10-12
申请号：US17586
申请日：1993-02-16
IPC分类号： A61K31/435 , A61K31/52 , A61K31/57 , A61K31/675 , A61P37/06 , C07D498/18 , C07D491/16 , A61K31/345
CPC分类号： C07D498/18
摘要： This invention provides a compound of the structure ##STR1## wherein X is selected from the group consisting of --NR.sup.1 CR.sup.2 R.sup.3 (CR.sup.4 R.sup.5).sub.m S--, --NR.sup.1 CR.sup.2 R.sup.3 (CR.sup.4 R.sup.5).sub.m O--, --OCR.sup.2 R.sup.3 (CR.sup.4 R.sup.5).sub.m O--, --NR.sup.1 CR.sup.2 R.sup.3 (CR.sup.4 R.sup.5).sub.p --, --OCR.sup.2 R.sup.3 (CR.sup.4 R.sup.5).sub.p --, --NR.sup.1 CR.sup.2 R.sup.3 (CR.sup.4 R.sup.5).sub.m NR.sup.6 --, --OCR.sup.2 R.sup.3 (CR.sup.4 R.sup.5).sub.m NR.sup.6 --, --SCR.sup.2 R.sup.3 (CR.sup.4 R.sup.5).sub.m NR.sup.6 --, --SCR.sup.2 R.sup.3 (CR.sup.4 R.sup.5).sub.m S--, --NOR.sup.1 --, and --NR.sup.1 --;R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, and R.sup.6 are each, independently, hydrogen, alkyl, fluorine, trifluoromethyl, aryl, arylalkyl, or any pair taken together to form a 3-6 membered ring;m=1-6; andp=0-6or a pharmaceutically acceptable salt thereof which is useful as an immunosuppressive, antiinflamatory, antifungal, antiproliferative, and antitumor agent. This invention also covers derivatives of I and the use of I in combination with other immunoregulatory agents.
摘要翻译： 本发明提供了其中X选自-NR 1 CR 2 R 3（CR 4 R 5）m S - ， - NR 1 CR 2 R 3（CR 4 R 5）m O - ， - OCR 2 R 3（CR 4 R 5）m O - ， - NR 1 CR 2 R 3（CR 4 R 5） 对 - ，-OCR 2 R 3（CR 4 R 5）p - ，-NR 1 CR 2 R 3（CR 4 R 5）m NR 6 - ， - OCR 2 R 3（CR 4 R 5）m NR 6 - ，-SCR 2 R 3（CR 4 R 5）m NR 6 - ，-SCR 2 R 3（CR 4 R 5）m -S-，-NOR 1 - 和-NR 1 - ; R 1，R 2，R 3，R 4，R 5和R 6各自独立地为氢，烷基，氟，三氟甲基，芳基，芳基烷基或任何一对一起形成3-6元环; m = 1-6; 和p = 0-6或其药学上可接受的盐，其可用作免疫抑制，抗炎，抗真菌，抗增殖和抗肿瘤剂。 本发明还包括I的衍生物和I与其它免疫调节剂组合的用途。
-
2.发明授权Substituted 1-aryl-3-heteroaryl-thioureas and substituted 1-aryl-3-heteroaryl-isothioureas as antiatherosclerotic agents 失效新型取代的1-芳基-3-杂芳基硫脲和取代的1-芳基-3-杂芳基 - 异硫脲作为抗动脉粥样硬化剂公开(公告)号：US06686476B2
公开(公告)日：2004-02-03
申请号：US10212888
申请日：2002-08-06
IPC分类号： C07D27728
CPC分类号： C07D275/03 , A61K31/415 , C07D231/40 , C07D263/48 , C07D277/48 , C07D277/82 , C07D277/84 , C07D285/135
摘要： Antiatherosclerotic agents are provided which are represented by Formulas I or II: wherein R is wherein R9, R10, R11, R12, R13, and R14 are each, independently, hydrogen or a lower alkyl of 1-6 carbon atoms; R6, and R7 are each, independently, hydrogen, lower alkyl of 1-6 carbon atoms, or CH2COOR8, where R8 is a lower alkyl of 1-6 carbon atoms; and X is O or S; R1 is hydrogen or a lower alkyl of 1-6 carbon atoms; R2, R3, and R4 are each, independently, hydrogen or halogen; and R5 is a lower alkyl of 1-6 carbon atoms; or a pharmaceutically acceptable salt thereof.
摘要翻译： 提供由式I或II表示的抗动脉粥样硬化剂：其中R在其中R 9，R 10，R 11，R 12，R 13和R 14各自独立地为氢或1-6个碳原子的低级烷基; R 6和R 7各自为 独立地是氢，1-6个碳原子的低级烷基或CH2COOR8，其中R8是1-6个碳原子的低级烷基; 且X为O或S; R 1为氢或1-6个碳原子的低级烷基; R 2，R 3和R 4各自独立地为氢或卤素; 和R 5是1-6个碳原子的低级烷基;或其药学上可接受的盐。
-
3.发明授权Rapamycin 42-sulfonates and 42-(N-Carboalkoxy)Sulfamates Useful as Immunosuppressive Agents 失效雷帕霉素42-磺酸盐和42-（N-羧基烷氧基）磺酸盐可用作免疫抑制剂
公开(公告)号：US5260299A
公开(公告)日：1993-11-09
申请号：US917555
申请日：1992-07-21
IPC分类号： C07D498/18 , A61K31/395
CPC分类号： C07D498/18
摘要： A derivative of rapamycin of general formula (I) ##STR1## where R.sup.1 is alkyl, alkenyl, or alkynyl containing 1 to 6 carbon atoms; or an aromatic moiety selected from the group consisting of phenyl and naphthyl or a heterocyclic moiety selected from the group consisting of thiophenyl and quinolinyl or NHCO.sub.2 R.sup.2 wherein R.sup.2 is lower alkyl containing 1 to 6 carbon atoms or a pharmaceutically acceptable salt thereof, which by virtue of its immunosuppressive activity is useful in treating transplantation rejection, host versus graft disease, autoimmune diseases, and diseases of inflammation.
摘要翻译： 通式（I）的雷帕霉素的衍生物其中R 1是含有1至6个碳原子的烷基，烯基或炔基; 或选自苯基和萘基的芳族部分或选自噻吩基和喹啉基或NHCO 2 R 2的杂环部分，其中R 2是含有1至6个碳原子的低级烷基或其药学上可接受的盐，其由于 其免疫抑制活性可用于治疗移植排斥反应，宿主与移植物疾病，自身免疫疾病和炎症疾病。
-
4.发明授权Rapamycin 42-sulfonates and 42-(N-carboalkoxy) sulfamates useful as immunosuppressive agents 失效雷帕霉素42-磺酸盐和42-（N-烷氧羰基）氨基磺酸盐可用作免疫抑制剂
公开(公告)号：US5177203A
公开(公告)日：1993-01-05
申请号：US846637
申请日：1992-03-05
IPC分类号： C07D498/18
CPC分类号： C07D498/18
摘要： A derivative of rapamycin of general formula (I) ##STR1## where R.sup.1 is alkyl, alkenyl, or alkynyl containing 1 to 6 carbon atoms; or an aromatic moiety selected from the group consisting of phenyl and naphthyl or a heterocyclic moiety selected from the group consisting of thiophenyl and quinolinyl or NHCO.sub.2 R.sup.2 wherein R.sup.2 is lower alkyl containing 1 to 6 carbon atoms or a pharmaceutically acceptable salt thereof, which by virtue of its immunosuppressive activity is useful in treating transplantation rejection, host versus graft disease, autoimmune diseases, and diseases of inflammation.
摘要翻译： 通式（I）的雷帕霉素的衍生物其中R 1是含有1至6个碳原子的烷基，烯基或炔基; 或选自苯基和萘基的芳族部分或选自噻吩基和喹啉基或NHCO 2 R 2的杂环部分，其中R 2是含有1至6个碳原子的低级烷基或其药学上可接受的盐，其由于 其免疫抑制活性可用于治疗移植排斥反应，宿主与移植物疾病，自身免疫疾病和炎症疾病。
-
![Substitued tetrahydro-1,3,5-triazin-2[1H]-thiones as anti-atherosclerotic agents](/abs-image/US/2001/07/31/US06268364B1/abs.jpg.150x150.jpg)
5.发明授权Substitued tetrahydro-1,3,5-triazin-2[1H]-thiones as anti-atherosclerotic agents 失效将取代的四氢-1,3,5-三嗪-2 [1H] - 噻二唑作为抗动脉粥样硬化剂公开(公告)号：US06268364B1
公开(公告)日：2001-07-31
申请号：US09483711
申请日：2000-01-14
IPC分类号： A61K3153
CPC分类号： C07D251/08
摘要： This invention provides compounds of formula 1 having the structure wherein R1, R2, R3, R4, and R5 are each independently, hydrogen, halogen, alkyl, cycloalkyl, alkenyl, alkynyl, phenylalkyl, alkoxy, aryloxy, fluoroalkoxy, trifluoromethyl, alkylthio, alkylsulfony, —SCF3, nitro, alkylamino, or dialkylamino; R6 is hydrogen, alkyl, cycloalkyl, or arylalkyl; and R7 is alkyl, cycloalkyl, or arylalkyl or a pharmaceutically acceptable salt thereof which are useful as antiatherosclerotic agents.
摘要翻译： 本发明提供具有其中R 1，R 2，R 3，R 4和R 5各自独立地为氢，卤素，烷基，环烷基，烯基，炔基，苯基烷基，烷氧基，芳氧基，氟烷氧基，三氟甲基，烷硫基，烷基磺酰基， SCF 3，硝基，烷基氨基或二烷基氨基; R 6是氢，烷基，环烷基或芳基烷基; 和R7是可用作抗动脉粥样硬化剂的烷基，环烷基或芳烷基或其药学上可接受的盐。
-
公开(公告)号：US5164399A
公开(公告)日：1992-11-17
申请号：US793765
申请日：1991-11-18
IPC分类号： C07D498/22
CPC分类号： C07D498/22
摘要： A compound of the structure ##STR1## wherein Z is ##STR2## and R.sup.1 is hydrogen, alkyl, or arylalkyl, provided that when R.sup.2 is present, R.sup.1 is absent;R.sup.2 is hydrogen, alkyl, or arylalkyl, provided that when R.sup.1 is present, R.sup.2 is absent;the dotted lines in the pyrazole ring represent double bonds between the 31- and 32-positions and between the 33- and 53-positions when R.sup.1 is present and double bonds between the 31- and 52-positions and between the 32- and 33-positions when R.sup.2 is present;or a pharmaceutically acceptable salt thereof which by virtue of its immunosuppressive activity is useful in treating transplantation rejection, host vs. graft disease, autoimmune diseases, and diseases of inflammation, by virtue of its antifungal activity is useful in treating fungal infections; and by virtue of its antitumor activity is useful in treating tumors. Intermediates possessing a 31,33-.beta.-dicarbonyl moiety that are useful for the same purposes are also described.
摘要翻译： 结构
的化合物，其中Z为 ，R 1为氢，烷基或芳烷基，条件是当存在R 2时，R 1不存在; R2是氢，烷基或芳基烷基，条件是当R 1存在时，R 2不存在; 吡唑环中的虚线代表31位和32位之间的双键，当R1存在时，33位和53位之间的双键，31位和52位之间以及32位和33位之间的双键， R2存在时的位置; 或其药学上可接受的盐，由于其免疫抑制活性可用于治疗移植排斥反应，宿主与移植物疾病，自身免疫疾病和炎症疾病，由于其抗真菌活性可用于治疗真菌感染; 并且由于其抗肿瘤活性可用于治疗肿瘤。 还描述了具有用于相同目的的31,33-β-二羰基部分的中间体。 -
公开(公告)号：US5120842A
公开(公告)日：1992-06-09
申请号：US678380
申请日：1991-04-01
CPC分类号： C07F7/1856
摘要： A compound of the structure ##STR1## wherein R.sup.1 is --SiR.sup.3 R.sup.4 R.sup.5 ;R.sup.2 is hydrogen or --SiR.sup.3 R.sup.4 R.sup.5 ; andR.sup.3, R.sup.4, and R.sup.5 are each, independently, alkyl, alkenyl, aralkyl, triphenylmethyl, or phenyl which by virtue of its immunosuppressive activity is useful in treating transplantation rejection, host vs. graft disease, autoimmune diseases and diseases of inflammation; by virtue of its antitumor activity is useful in treating solid tumors; and by virtue of its antifungal activity is useful in treating fungal infections. This invention also provides a method of using rapamycin 42-[O-[(1,1-dimethylethyl)-dimethylsilyl] ether for the preparation of 31-substituted rapamycin derivatives.
摘要翻译： 结构
的化合物，其中R 1是-SiR 3 R 4 R 5; R2是氢或-SiR3R4R5; 并且R3，R4和R5各自独立地为烷基，烯基，芳烷基，三苯基甲基或苯基，由于其免疫抑制活性可用于治疗移植排斥反应，宿主与移植物疾病，自身免疫疾病和炎症疾病; 由于其抗肿瘤活性可用于治疗实体瘤; 并且由于其抗真菌活性可用于治疗真菌感染。 本发明还提供了使用雷帕霉素42- [O - [（1,1-二甲基乙基） - 二甲基甲硅烷基]醚来制备31-取代的雷帕霉素衍生物的方法。 -
8.发明授权Substituted 1-aryl-3-heteroaryl-thioureas (or isothioureas) as antiatherosclerotic agents 失效取代的1-芳基-3-杂芳基硫脲（或异硫脲）作为抗动脉粥样硬化剂公开(公告)号：US06455566B1
公开(公告)日：2002-09-24
申请号：US09145909
申请日：1998-09-02
IPC分类号： A61K31415
CPC分类号： C07D275/03 , A61K31/415 , C07D231/40 , C07D263/48 , C07D277/48 , C07D277/82 , C07D277/84 , C07D285/135
摘要： Antiatherosclerotic agents are provided which are represented by Formulas I or II: wherein R is wherein R9, R10, R11, R12, R13, and R14 are each, independently, hydrogen or a lower alkyl of 1-6 carbon atoms; R6, and R7 are each, independently, hydrogen, lower alkyl of 1-6 carbon atoms, or CH2COOR8, where R8 is a lower alkyl of 1-6 carbon atoms; and X is O or S; R1 is hydrogen or a lower alkyl of 1-6 carbon atoms; R2, R3, and R4 are each, independently, hydrogen or halogen; and R5 is a lower alkyl of 1-6 carbon atoms; or a pharmaceutically acceptable salt thereof.
摘要翻译： 提供由式I或II表示的抗动脉粥样硬化剂：其中R是其中R 9，R 10，R 11，R 12，R 13和R 14各自独立地是氢或1-6个碳原子的低级烷基; R 6和R 7是 各自独立地为氢，1-6个碳原子的低级烷基或CH2COOR8，其中R8是1-6个碳原子的低级烷基; 且X为O或S; R 1为氢或1-6个碳原子的低级烷基; R 2，R 3和R 4各自独立地为氢或卤素; 和R 5是1-6个碳原子的低级烷基;或其药学上可接受的盐。
-
公开(公告)号：US06344451B1
公开(公告)日：2002-02-05
申请号：US09495506
申请日：2000-02-01
IPC分类号： A61K3155
CPC分类号： C07D487/14 , A61K31/551
摘要： The present invention provides compounds of the formula: wherein: X, Y and Z are independently selected from O, S, CH, CH2, N, or NR4; W is moiety selected from (CH2)n; n=1-2; R1, R2 are independently, hydrogen, straight chain alkyl (C1-C6), branched chain alkyl (C3-C7), cycloalkyl (C3-C7), alkoxyalkyl (C2-C7), halogen, straight or branched chain alkoxy (C1-C6), hydroxy, CF3, or perfluoroalkyl (C2-C6); R3 is hydrogen or a straight chain alkyl group (C1-C6), branched chain alkyl (C3-C7), cycloalkyl (C3-C7), alkoxyalkyl (C2-C7), or hydroxyalkyl (C1-C6); R4 is selected from hydrogen, or (lower alkyl (C1-C6); and R5 is selected from halogen or hydrogen; or a pharmaceutically acceptable salt thereof: as well as methods and pharmaceutical compositions utilizing these compounds for the treatment of disorder which may be remedied or alleviated by vasopressin agonist activity, including diabetes insipidus, nocturnal enuresis, nocturia, urinary incontinence, bleeding and coagulation disorders, or temporary delay of urination.
摘要翻译： 本发明提供下式的化合物：其中：X，Y和Z独立地选自O，S，CH，CH 2，N或NR 4; W是选自（CH 2）n; n = 1-2; R 1 ，R2独立地为氢，直链烷基（C1-C6），支链烷基（C3-C7），环烷基（C3-C7），烷氧基烷基（C2-C7），卤素，直链或支链烷氧基（C1-C6 ），羟基，CF 3或全氟烷基（C 2 -C 6）; R 3是氢或直链烷基（C 1 -C 6），支链烷基（C 3 -C 7），环烷基（C 3 -C 7） ）或羟基烷基（C 1 -C 6）; R 4选自氢或（低级烷基（C 1 -C 6））;和R 5选自卤素或氢;或其药学上可接受的盐：以及利用它们的方法和药物组合物 用于治疗可通过加压素激动剂活性治疗或减轻的疾病的化合物，包括尿崩症，夜间遗尿，夜尿症，尿失禁，出血和凝血障碍或暂时性 排尿迟缓。
-
10.发明授权Substituted indole-1-carbothioic acid amides as novel antiatherosclerotic agents 失效取代的吲哚-1-硫代硫酸酰胺作为新的抗动脉粥样硬化剂
公开(公告)号：US6011053A
公开(公告)日：2000-01-04
申请号：US145942
申请日：1998-09-02
IPC分类号： A61K31/404 , A61K31/4155 , C07D209/08 , C07D403/12 , A61K31/40 , A61K31/415
CPC分类号： C07D403/12 , A61K31/404 , A61K31/4155 , C07D209/08
摘要： Antiatherosclerotic agents are provided having the structure: ##STR1## wherein R is a lower alkyl of 1-6 carbon atoms, ##STR2## wherein R.sub.5, R.sub.6, and R.sub.7 are lower alkyl of 1-6 carbon atoms; and R.sub.8, R.sub.9 and R.sub.10 are each, independently, hydrogen or halogen;R.sub.1 and R.sub.2 are each, independently, hydrogen or a lower alkyl of 1-6 carbon atoms; andR.sub.3 and R.sub.4 are each, independently, hydrogen, a lower alkyl of 1-6 carbon atoms or halogen;or a pharmaceutically acceptable salt thereof.
摘要翻译： 提供具有以下结构的抗动脉粥样硬化剂：其中R是1-6个碳原子的低级烷基，其中R5，R6和R7是1-6个碳原子的低级烷基; 并且R 8，R 9和R 10各自独立地为氢或卤素; R1和R2各自独立地为氢或1-6个碳原子的低级烷基; 并且R 3和R 4各自独立地为氢，1-6个碳原子的低级烷基或卤素; 或其药学上可接受的盐。
-
-
-
-
-
-
-
-
-
搜索结果
67 条记录 (耗时 0.023 秒)
