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公开(公告)号：US07241791B2
公开(公告)日：2007-07-10
申请号：US10670646
申请日：2003-09-24
IPC分类号： A61K31/416 , C07D231/56
CPC分类号： C07D231/56 , C07D409/04
摘要： This invention provides compound of formulae I or II having the structure wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, and R10 are as defined in the specification or a pharmaceutically acceptable salt thereof which are useful for the treatment of the inflammatory component of diseases and are particularly useful in treating atherosclerosis, myocardial infarction, congestive heart failure, inflammatory bowel disease, arthritis, type II diabetes, and autoimmune diseases such as multiple sclerosis and rheumatiod arthritis.
摘要翻译： 本发明提供具有以下结构的式I或II的化合物，其中R 1，R 2，R 3，R 4， R 5，R 6，R 7，R 8，R 9， SUB＆gt;和R 10＆gt;如说明书中所定义或其药学上可接受的盐，其可用于治疗疾病的炎性成分，并且特别可用于治疗动脉粥样硬化，心肌梗塞，充血性心脏 失败，炎症性肠病，关节炎，II型糖尿病和自身免疫疾病如多发性硬化和风湿性关节炎。
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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。
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3.发明授权
公开(公告)号：US5298392A
公开(公告)日：1994-03-29
申请号：US883815
申请日：1992-05-13
CPC分类号： C12Q1/689 , Y10T436/25375
摘要： Processes and kits therefor for detection of water-borne pathogens and indicator organisms in water samples by recovering cells of the pathogens or indicator organisms from a water sample, lysing the cells to recover undegraded DNA, amplifying a target gene sequence of a target gene present in cells of the pathogens or indicator organisms by polymerase chain reaction amplification and detecting the presence of amplified target gene sequence to determine the presence or absence of pathogens or indicator organism in the test sample.
摘要翻译： 用于通过从水样中回收病原体或指示生物的细胞，裂解细胞以回收未降解的DNA，扩增存在于靶标基因中的靶基因的靶基因序列，从而检测水样中水性病原体和指示生物体的方法和试剂盒 通过聚合酶链反应扩增，检测病原体或指示生物的细胞，并检测扩增的靶基因序列的存在，以确定测试样品中病原体或指示生物的存在或不存在。
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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-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。
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5.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。
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6.发明授权Substituted tetrahydro-1,3,5-triazin-2[1H]-thiones as anti-atherosclerotic agents 失效取代的四氢-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：US6160114A
公开(公告)日：2000-12-12
申请号：US960832
申请日：1997-10-30
IPC分类号： A61P3/06 , A61P9/10 , C07D251/08 , C07D239/40
CPC分类号： C07D251/08
摘要： This invention provides compounds of formula 1 having the structure ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, and R.sup.5 are each independently, hydrogen, halogen, alkyl, cycloalkyl, alkenyl, alkynyl, phenylalkyl, alkoxy, aryloxy, fluoroalkoxy, trifluoromethyl, alkylthio, alkylsulfony, --SCF.sub.3, nitro, alkylamino, or dialkylamino;R.sup.6 is hydrogen, alkyl, cycloalkyl, or arylalkyl; andR.sup.7 is alkyl, cycloalkyl, or arylalkylor 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; R6是氢，烷基，环烷基或芳基烷基; 并且R 7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。
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公开(公告)号：US5373014A
公开(公告)日：1994-12-13
申请号：US134237
申请日：1993-10-08
IPC分类号： C07D498/18 , A61K31/395 , C07D491/16
CPC分类号： C07D498/18
摘要： A compound of the structure ##STR1## wherein R.sup.1 is ##STR2## R.sup.2 is hydrogen, alkyl, alkenyl, alkynyl, trifluoromethyl, arylalkyl, or Ar;R.sup.3 is hydrogen, alkyl, alkenyl, alkynyl, trifluoromethyl, arylalkyl, or --CO.sub.2 R.sup.8 ;R.sup.4 is alkyl, alkenyl, alkynyl, trifluoromethyl, arylalkyl, Ar, aminoalkyl, thioalkyl, alkylthioalkyl, hydroxyalkyl, or --CO.sub.2 R.sup.8 ;R.sup.5 is hydrogen, alkyl, alkenyl, alkynyl, trifluoromethyl, arylalkyl, At, or --CO.sub.2 R.sup.8 ;R.sup.6 is hydrogen, alkyl, alkenyl, alkynyl, trifluoromethyl, arylalkyl, or Ar;R.sup.7 is alkyl, alkenyl, alkynyl, trifluoromethyl, arylalkyl, or Ar;R.sup.8 is hydrogen, alkyl, alkenyl, alkynyl, trifluoromethyl, arylalkyl, fluorenylmethyl, orAr;Y is O or S;X is .dbd.N--O--(CH.sub.2).sub.f --Z or .dbd.N--O--Ar;Z is hydrogen, alkenyl, alkynyl, alkoxy, cyano, fluoro, trifluoromethyl, --NR.sup.5 R.sup.6, aryloxy, or Ar;Ar is aryl which may be optionally mono-, di-, or tri- substituted;a=0-4;b=0-1;c=0-4;d=0-6;e=0-6; andf=0-6;or a pharmaceutically acceptable salt thereof, with the proviso that when f is 0, Z is hydrogen and further provided that when R.sup.3 or R.sup.5 is --CO.sub.2 R.sup.8, R.sup.8 is not hydrogen which is useful as an immunosuppressive, antiinflammatory, antifungal, antiproliferative, and antitumor agent.
摘要翻译： 其中R1是氢，烷基，烯基，炔基，三氟甲基，芳烷基或Ar的结构化合物
R3是氢，烷基，烯基，炔基，三氟甲基，芳烷基或-CO2R8; R4是烷基，烯基，炔基，三氟甲基，芳基烷基，Ar，氨基烷基，硫代烷基，烷硫基烷基，羟基烷基或-CO 2 R 8; R5是氢，烷基，烯基，炔基，三氟甲基，芳烷基，At或-CO2R8; R6是氢，烷基，烯基，炔基，三氟甲基，芳烷基或Ar; R7是烷基，烯基，炔基，三氟甲基，芳烷基或Ar; R8是氢，烷基，烯基，炔基，三氟甲基，芳基烷基，芴基甲基或Ar; Y为O或S; X = N-O-（CH 2）f-Z或= N-O-Ar; Z是氢，烯基，炔基，烷氧基，氰基，氟，三氟甲基，-NR5R6，芳氧基或Ar; Ar是可任选被单，二或三取代的芳基; a = 0-4; b = 0-1; c = 0-4; d = 0-6; e = 0-6; 和f = 0-6; 或其药学上可接受的盐，条件是当f为0时，Z为氢，并且还提供当R3或R5为-CO2R8时，R8不为氢，可用作免疫抑制，抗炎，抗真菌，抗增殖和抗肿瘤 代理商 -
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。
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公开(公告)号：US5162333A
公开(公告)日：1992-11-10
申请号：US757858
申请日：1991-09-11
IPC分类号： C07D498/18 , C07D519/00
CPC分类号： C07D498/18 , C07D519/00
摘要： A compound of the structure ##STR1## wherein R.sup.1 is ##STR2## R.sup.3 is hydrogen, alkyl, arylalkyl, (CH.sub.2).sub.s NR.sup.4 R.sup.5, aminoalkyl, hydroxyalkyl, guanylalkyl, mercaptoalkyl, alkylthioalkyl, indolylmethyl, hydroxyphenylmethyl, imidazolylmethyl or phenyl which is optionally mono-, di-, or tri-substituted;R.sup.4 is hydrogen, alkyl, or aralkyl;R.sup.2 and R.sup.5 are each independently hydrogen, formyl, alkanoyl, arylalkanoyl, aryloyl, or CO.sub.2 R.sup.6 ;R.sup.6 is alkyl, arylalkyl, allyl, fluorenylmethyl, or phenyl which is optionally mono-, di-, or tri-substituted;m is 0-4; n is 0-4; p is 0-1; q is 0-4; r is 0-4; and s is 0-4; 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.
摘要翻译： 其中R 1是R 3是氢，烷基，芳基烷基，（CH 2）n NR 4 R 5，氨基烷基，羟基烷基，脒基烷基，巯基烷基，烷基硫代烷基，吲哚基甲基，羟苯基甲基，咪唑基甲基或苯基的结构化合物， 二取代或三取代; R4是氢，烷基或芳烷基; R2和R5各自独立地为氢，甲酰基，烷酰基，芳基烷酰基，芳氧基或CO 2 R 6; R6是烷基，芳基烷基，烯丙基，芴基甲基或任选被一或二或三取代的苯基; m为0-4; n为0-4; p为0-1; q为0-4; r为0-4; s为0-4; 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，自身免疫性疾病和炎症疾病，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。
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公开(公告)号：US5120726A
公开(公告)日：1992-06-09
申请号：US667684
申请日：1991-03-08
IPC分类号： C07D498/18
CPC分类号： C07D498/18
摘要： A compound of the structure ##STR1## wherein R.sup.1 is hydrogen, alkyl or aralkyl; R.sup.2 is hydrogen, alkyl, cycloalkyl, aralkyl, --COR.sup.3, --CO.sub.2 R.sup.3, --SO.sub.2 R.sup.3, --CONR.sup.4 R.sup.5, --CSNR.sup.4 R.sup.5, --COCONR.sup.4 R.sup.5, or Ar; R.sup.3 is alkyl, aralkyl, or Ar; R.sup.4 and R.sup.5 are each, independently, hydrogen, alkyl, cycloalkyl, allyl, aralkyl, or Ar;Ar is ##STR2## R.sup.6, R.sup.7, R.sup.8 are each, independently, hydrogen, alkyl, alkoxy, hydroxy, cyano, halo, nitro, carbalkoxy, trifluoromethyl, trifluoromethoxy, amino, or a carboxylic acid; X is CH or N; Y is NH, O, or S; 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 antitumor activity is useful in treating solid tumors; and by virtue of its antifungal activity is useful in treating fungal infections.
摘要翻译： 结构
的化合物，其中R 1是氢，烷基或芳烷基; R 2是氢，烷基，环烷基，芳烷基，-COR 3，-CO 2 R 3，-SO 2 R 3，-CONR 4 R 5，-CSNR 4 R 5，-COCONR 4 R 5或Ar; R3是烷基，芳烷基或Ar; R 4和R 5各自独立地为氢，烷基，环烷基，烯丙基，芳烷基或Ar; R 6，R 7，R 8各自独立地为氢，烷基，烷氧基，羟基，氰基，卤素，硝基，烷氧基，三氟甲基，三氟甲氧基，氨基或羧酸。 X是CH或N; Y是NH，O或S; 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; 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。
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