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公开(公告)号：US4348516A
公开(公告)日：1982-09-07
申请号：US158850
申请日：1980-06-12
CPC分类号： C12R1/29 , C12P19/485
摘要： The microorganisms Micromonospora inyoensis 1550F-1G and M. purpurea strain 1124 each microbiologically convert tobramycin, kanamycin A, kanamycin B and dibekacin to their respective 3"-N-methyl and 3"-N-methyl-4"-C-methyl derivatives. The derivatives exhibit significant activity against representative gram positive and gram negative bacteria and may also be converted to other derivatives which have significant antibacterial activity.
摘要翻译： 微生物Micromonospora inyoensis 1550F-1G和M.peppurea菌株1124每个微生物转化妥布霉素，卡那霉素A，卡那霉素B和二卡西汀至其相应的3' - N-甲基和3“ - N-甲基-4'-C- 甲基衍生物。 该衍生物对代表性的革兰氏阳性细菌和革兰氏阴性细菌表现出显着的活性，并且还可以转化为具有显着抗菌活性的其它衍生物。
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公开(公告)号：US4234685A
公开(公告)日：1980-11-18
申请号：US51790
申请日：1979-06-25
IPC分类号： C12P19/48
CPC分类号： C12R1/29 , C12P19/485 , Y10S435/862 , Y10S435/867
摘要： The microorganisms Micromonospora inyoensis 1550F-1G and M. purpurea strain 1124 each microbiologically convert tobramycin, kanamycin A, kanamycin B and dibekacin to their respective 3"-N-methyl and 3"-N-methyl-4"-C-methyl derivatives. The derivatives exhibit significant activity against representative gram positive and gram negative bacteria and may also be converted to other derivatives which have significant antibacterial activity.
摘要翻译： 微生物Micromonospora inyoensis 1550F-1G和M.peppurea菌株1124每个微生物转化妥布霉素，卡那霉素A，卡那霉素B和二卡西汀至其相应的3' - N-甲基和3“ - N-甲基-4'-C- 甲基衍生物。 该衍生物对代表性的革兰氏阳性细菌和革兰氏阴性细菌表现出显着的活性，并且还可以转化为具有显着抗菌活性的其它衍生物。
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公开(公告)号：US6159984A
公开(公告)日：2000-12-12
申请号：US94707
申请日：1998-06-15
申请人： Timothy J. Guzi , Dinanath F. Rane
发明人： Timothy J. Guzi , Dinanath F. Rane
IPC分类号： A61P35/00 , C07D401/04 , C07D401/14 , A61K31/4545
CPC分类号： C07D401/04 , C07D401/14
摘要： Novel compounds of the formula: ##STR1## wherein a represents N or NO, R.sup.1 and R.sup.3 are halo, R.sup.2 and R.sup.4 are independently H or halo provided that at least one is H, X is C, CH or N, and T represents ##STR2## wherein R.sub.5 is H (C.sub.1 -C.sub.6)alkyl or a bond; b and c are independently 0 to 3 and Y is a three, four, five or six membered cycloalkyl ring, pyridyl, pyrazinyl or phenyl are disclosed. Pharmaceutical Compositions containing such compounds, methods of inhibiting farnesyl protein transferase and methods for treating tumor cells using such compounds or compositions are also disclosed.
摘要翻译： 新的下式化合物：其中a表示N或NO，R 1和R 3是卤素，R 2和R 4独立地是H或卤素，条件是至少一个是H，X是C，CH或N，T表示其中R 5是H （C 1 -C 6）烷基或键; b和c独立地为0至3，Y为三，四，五或六元环烷基环，吡啶基，吡嗪基或苯基。 还公开了含有这种化合物的药物组合物，抑制法呢基蛋白转移酶的方法和使用这些化合物或组合物治疗肿瘤细胞的方法。
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4.发明授权
公开(公告)号：US5958940A
公开(公告)日：1999-09-28
申请号：US927728
申请日：1997-09-11
申请人： Dinanath F. Rane , Alan B. Cooper , Alan K. Mallams , Ronald J. Doll , F. George Njoroge , Arthur G. Taveras
发明人： Dinanath F. Rane , Alan B. Cooper , Alan K. Mallams , Ronald J. Doll , F. George Njoroge , Arthur G. Taveras
IPC分类号： C07D401/14 , A61K31/44
CPC分类号： C07D401/14
摘要： Novel tricyclic compounds and pharmaceutical compositions are disclosed which are inhibitors of the enzyme, farnesyl protein transferase. Also disclosed is a method of inhibiting Ras function and therefore inhibiting the abnormal growth of cells. The method comprises administering the novel tricyclic compound to a biological system. In particular, the method inhibits the abnormal growth of cells in a mammals such as a human.
摘要翻译： 公开了新的三环化合物和药物组合物，其是酶的抑制剂，法呢基蛋白转移酶。 还公开了抑制Ras功能并因此抑制细胞异常生长的方法。 该方法包括将新型三环化合物施用于生物系统。 特别地，该方法抑制哺乳动物如人的细胞的异常生长。
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5.发明授权Tri- and tetra-substituted-oxetanes and tetrahydrofurans and intermediates thereof 失效三取代 - 氧杂环丁烷和四氢呋喃及其中间体
公开(公告)号：US5039676A
公开(公告)日：1991-08-13
申请号：US460342
申请日：1990-05-11
IPC分类号： C07C17/16 , C07C21/22 , C07C45/29 , C07D473/04 , C07D521/00
CPC分类号： C07D231/12 , C07C17/16 , C07C21/22 , C07C45/292 , C07D233/56 , C07D249/08 , C07D473/04
摘要： This invention relates to tri- and tetra-substituted-oxetanes, e.g. (.+-.)-cis- and (.+-.)-trans-2-[(4-(4-isopropylpiperazin-1-yl)phenoxy)methyl]-4-(2,4-dihalophenyl)-4-[1H-1,2,4-triazol-1-yl)-methyl]oxetane and tri- and tetra-substituted-tetrahydrofurans, e.g. (.+-.)-cis- and (.+-.)-trans-1-[4-[[2-(2,4-dihalophenyl)tetrahydro-2-[(1H-azol-1-yl)methyl]-5-furanylmethoxy]phenyl]-4-yl-1-substituted piperazine-3-one and related derivatives which exhibit antifungal and antiallergy activities, pharmaceutical composition thereof, methods of their use in treating or preventing susceptible fungal infections and allergic reactions in a host including warm-blooded animals such as humans.
摘要翻译： 本发明涉及三 - 和四 - 取代 - 氧杂环丁烷，例如 （+/-） - 顺式 - 和（+/-） - 反式-2 - [（4-（4-异丙基哌嗪-1-基）苯氧基）甲基] -4-（2,4-二卤代苯基） [1H-1,2,4-三唑-1-基] - 甲基]氧杂环丁烷和三取代 - 四氢呋喃，例如 （+/-） - 顺 - 和（+/-） - 反式-1- [4 - [[2-（2,4-二卤苯基）四氢-2 - [（1H-氮杂-1-基）甲基] -5-呋喃基甲氧基]苯基] -4-基-1-取代的哌嗪-3-酮及其相关衍生物，其具有抗真菌和抗过敏活性，其药物组合物，其用于治疗或预防易感性真菌感染和其中的过敏反应的方法 宿主包括温血动物如人类。
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公开(公告)号：US06372747B1
公开(公告)日：2002-04-16
申请号：US09465553
申请日：1999-12-16
申请人： Arthur G. Taveras , Ronald J. Doll , Alan B. Cooper , Johan A. Ferreira , Timothy Guzi , Dinanath F. Rane , Viyyoor M. Girijavallabhan , Cynthia J. Aki , Jianping Chao , Carmen Alvarez , Joseph M. Kelly , Tarik Lalwani , Jagdish A. Desai , James J-S Wang
发明人： Arthur G. Taveras , Ronald J. Doll , Alan B. Cooper , Johan A. Ferreira , Timothy Guzi , Dinanath F. Rane , Viyyoor M. Girijavallabhan , Cynthia J. Aki , Jianping Chao , Carmen Alvarez , Joseph M. Kelly , Tarik Lalwani , Jagdish A. Desai , James J-S Wang
IPC分类号： A61K31496
CPC分类号： C07D401/04 , C07D401/14
摘要： Disclosed are compounds of the formula: wherein R13 represents an imidazole ring; R14 represents a carbamate, urea, amide or sulfonamide group; R8 represents H when the alkyl chain between the amide group and the R13 imidazole group is substituted, or R8 represents a substituent such as arylalkyl, heteroarylalkyl or cycloalkyl; and the remaining substituents are as defined herein. Also disclosed are compounds wherein R8 is H, and the alkyl chain between the amide group and the R13 imidazole group is unsubstituted. Also disclosed is a method of treating cancer and a method of inhibiting farnesyl protein transferase using the disclosed compounds.
摘要翻译： 公开了下式的化合物：其中R 13表示咪唑环; R14表示氨基甲酸酯，脲，酰胺或磺酰胺基; 当酰胺基和R 13咪唑基之间的烷基链被取代时，R8表示H，或R8表示芳基烷基，杂芳基烷基或环烷基等取代基; 并且其余的取代基如本文所定义。 还公开了其中R 8为H，酰胺基和R 13咪唑基之间的烷基链未被取代的化合物。 还公开了使用所公开的化合物治疗癌症的方法和抑制法呢基蛋白转移酶的方法。
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7.发明授权Tricyclic compounds useful for inhibition of G-protein function and for treatment of proliferative diseases 失效可用于抑制G蛋白功能和治疗增殖性疾病的三环化合物
公开(公告)号：US5958890A
公开(公告)日：1999-09-28
申请号：US927727
申请日：1997-09-11
IPC分类号： C07D401/14 , C07D413/14 , A61K31/70 , A61K31/44 , C07D221/16 , C07M15/00
CPC分类号： C07D401/14 , C07D413/14
摘要： Compounds the formula ##STR1## their use as farnesyl transferase protein inhibitors and pharmaceutical compositions containing them are disclosed, especially compounds of the formula ##STR2## wherein R.sup.1, R.sup.2 and R.sup.3 are halo, A and B are each H.sub.2, and R is as defined in the specification.
摘要翻译： 公开了将其用作法呢基转移酶蛋白抑制剂和含有它们的药物组合物的化合物，特别是下式的化合物其中R 1，R 2和R 3是卤素，A和B各自为H 2，R如说明书中所定义。
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8.发明授权Tricyclic compounds useful for inhibition of G-protein function and for treatment of proliferative diseases 失效可用于抑制G蛋白功能和治疗增殖性疾病的三环化合物
公开(公告)号：US5712280A
公开(公告)日：1998-01-27
申请号：US418973
申请日：1995-04-07
申请人： Ronald J. Doll , Alan K. Mallams , Adriano Afonso , Dinanath F. Rane , Randall R. Rossman , F. George Njoroge
发明人： Ronald J. Doll , Alan K. Mallams , Adriano Afonso , Dinanath F. Rane , Randall R. Rossman , F. George Njoroge
IPC分类号： A61K31/44 , A61K31/4427 , A61K31/4433 , A61K31/445 , A61K31/47 , A61K31/473 , A61K31/495 , A61P35/00 , A61P43/00 , C07D211/32 , C07D213/28 , C07D221/16 , C07D401/06 , C07D401/12 , C07D401/14 , C07D409/12 , C07D491/04 , C07D491/044
CPC分类号： C07D401/12 , C07D211/32 , C07D221/16 , C07D401/14 , C07D409/12 , C07D491/04
摘要： Novel compounds of Formula ##STR1## are disclosed. Also disclosed is a method of inhibiting Ras function and therefore inhibiting the abnormal growth of cells. The method comprises administering a compound of the Formula 1.0 to a biological system. In particular, the method inhibits the abnormal growth of cells in a mammal such as a human being.
摘要翻译： 公开了新颖的式（IMAGE）化合物。 还公开了抑制Ras功能并因此抑制细胞异常生长的方法。 该方法包括向生物系统施用式1.0的化合物。 特别地，该方法抑制哺乳动物例如人的细胞的异常生长。
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9.发明授权Tricyclic compounds useful for inhibition of G-protein function and for treatment of proliferative diseases 失效可用于抑制G蛋白功能和治疗增殖性疾病的三环化合物
公开(公告)号：US5672611A
公开(公告)日：1997-09-30
申请号：US446265
申请日：1995-05-22
申请人： Ronald J. Doll , Alan K. Mallams , Adriano Afonso , Dinanath F. Rane , Randall R. Rossman , F. George Njoroge
发明人： Ronald J. Doll , Alan K. Mallams , Adriano Afonso , Dinanath F. Rane , Randall R. Rossman , F. George Njoroge
IPC分类号： A61K31/44 , A61K31/4427 , A61K31/4433 , A61K31/445 , A61K31/47 , A61K31/473 , A61K31/495 , A61P35/00 , A61P43/00 , C07D211/32 , C07D213/28 , C07D221/16 , C07D401/06 , C07D401/12 , C07D401/14 , C07D409/12 , C07D491/04 , C07D491/044 , C07D211/06
CPC分类号： C07D401/12 , C07D211/32 , C07D221/16 , C07D401/14 , C07D409/12 , C07D491/04
摘要： Novel compounds of Formula ##STR1## are disclosed. Also disclosed is a method of inhibiting Ras function and therefore inhibiting the abnormal growth of cells. The method comprises administering a compound of the Formula 1.0 to a biological system. In particular, the method inhibits the abnormal growth of cells in a mammal such as a human being.
摘要翻译： 公开了新颖的式（IMAGE）化合物。 还公开了抑制Ras功能并因此抑制细胞异常生长的方法。 该方法包括向生物系统施用式1.0的化合物。 特别地，该方法抑制哺乳动物例如人的细胞的异常生长。
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10.发明授权公开(公告)号：US07585864B2
公开(公告)日：2009-09-08
申请号：US11301308
申请日：2005-12-12
申请人： Dinanath F. Rane
发明人： Dinanath F. Rane
IPC分类号： A61K31/497 , C07D241/04 , C07D295/00
CPC分类号： C07D491/04
摘要： Disclosed are compounds of the formula: wherein R8 represents a cyclic and acyclic moiety to which is bound an imidazolylalkyl group; R9 represents a carbamate, urea, amide or sulfonamide group; and the remaining substituents are as defined herein. Also disclosed is a method of treating cancer and a method of inhibiting farnesyl protein transferase using the disclosed compounds.
摘要翻译： 公开了下式的化合物：其中R8表示与咪唑基烷基结合的环状和非环状部分; R9表示氨基甲酸酯，脲，酰胺或磺酰胺基团; 并且其余的取代基如本文所定义。 还公开了使用所公开的化合物治疗癌症的方法和抑制法呢基蛋白转移酶的方法。
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