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31. 发明授权

US4994464A Piperazinylpyrimidines as .beta.-adrenergic receptor blockers 失效
标题翻译：哌嗪基嘧啶作为β-肾上腺素能受体阻断剂
公开(公告)号：US4994464A
公开(公告)日：1991-02-19
申请号：US417535
申请日：1989-10-05
申请人： Richard L. Tolman , John J. Baldwin , Arthur F. Wagner , Adolph Pietruszkiewicz
发明人： Richard L. Tolman , John J. Baldwin , Arthur F. Wagner , Adolph Pietruszkiewicz
IPC分类号： C07D495/04
CPC分类号： C07D495/04
摘要： Certain piperazinylpyrimidines have pronounced .beta.-adrenergic blocking properties and some of the compounds are particularly useful in the treatment of elevated intraocular pressure and glaucoma.
摘要翻译：某些哌嗪基嘧啶具有显着的β-肾上腺素能阻断性质，并且一些化合物特别可用于治疗眼内压升高和青光眼。

32. 发明授权

US4897479A Arylsulfonyloxy purine intermediates 失效
标题翻译：芳基磺酰氧基嘌呤中间体
公开(公告)号：US4897479A
公开(公告)日：1990-01-30
申请号：US165360
申请日：1988-02-29
申请人： Richard L. Tolman , Wallace Ashton , Malcolm Maccoss
发明人： Richard L. Tolman , Wallace Ashton , Malcolm Maccoss
IPC分类号： C07D473/00 , C07F9/6561
CPC分类号： C07D473/00 , C07F9/65616
摘要： Compounds of the formula ##STR1## and the pharmaceutically acceptable salts thereof are disclosed. In these compounds, R.sup.1 is halogen, --SR.sup.4 wherein R.sup.4 is H or alkyl of 1 to 4 carbon atoms, --OCH.sub.3, --OSO.sub.2 Ar wherein Ar is phenyl or alkyl substituted phenyl wherein the alkyl group has 1 to 6 carbon atoms, --NR.sup.4 R.sup.5 wherein R.sup.4 is as defined above and R.sup.5 is H, alkyl of 1 to 4 carbon atoms, amino, alkanoyl of 1 to 8 carbon atoms, benzoyl, methoxy or hydroxy or R.sup.1 is --N(CH.sub.3).sub.3.sup.+ X.sup.-whereinX is halogen or --OSO.sub.2 Ar wherein Ar is phenyl or alkyl substituted phenyl wherein the alkyl group has 1 to 6 carbon atoms;R.sup.2 is H, alkanoyl of 1 to 8 carbon atoms or benzoyl;R.sup.3 is A or B whereinA is ##STR2## and B is ##STR3## wherein R.sup.6 and R.sup.7 are independently selected from H and ##STR4## wherein R.sup.8 and R.sup.9 are independently selected from pharmaceutically acceptable cations and H, or R.sup.6 and R.sup.7 taken together are ##STR5## wherein R.sup.10 is selected from pharmaceutically acceptable cations and H; with the proviso that R.sup.4 is not H when: R.sup.5 is H, R.sup.3 is A, and R.sup.6 and R.sup.7 are H. The compounds have anti-viral activity.
摘要翻译：公开了式“IMAGE”的化合物及其药学上可接受的盐。在这些化合物中，R 1是卤素，-SR 4，其中R 4是H或1-4个碳原子的烷基，-OCH 3，-OSO 2 Ar，其中Ar是苯基或烷基取代的苯基，其中烷基具有1-6个碳原子，-NR4R5其中 R 4如上所定义，R 5为H，具有1至4个碳原子的烷基，氨基，1至8个碳原子的烷酰基，苯甲酰基，甲氧基或羟基或R 1为-N（CH 3）3 + X-，其中X为卤素或 -OSO 2 Ar，其中Ar是苯基或烷基取代的苯基，其中烷基具有1至6个碳原子; R2是H，1-8个碳原子的烷酰基或苯甲酰基; R3是A或B，其中A是，B是，其中R6和R7独立地选自H和IMA，其中R8和R9独立地选自药学上可接受的阳离子，H或R6和R7一起其中R 10选自药学上可接受的阳离子和H; 条件是当R 5为H，R 3为A且R 6和R 7为H时，R 4不为H。化合物具有抗病毒活性。

33. 发明授权

US4816469A 5-Amino or substituted amino 1,2,3-triazoles 失效
标题翻译： 5-氨基或取代的氨基-1,2,3-三唑
公开(公告)号：US4816469A
公开(公告)日：1989-03-28
申请号：US117773
申请日：1987-11-06
申请人： Richard J. Bochis , Richard L. Tolman , Elbert Harris
发明人： Richard J. Bochis , Richard L. Tolman , Elbert Harris
IPC分类号： C07D249/04 , C07D249/06
CPC分类号： C07C255/00 , C07D249/04
摘要： Novel 5-amino or substituted amino 1,2,3-triazoles are disclosed as having anticoccidial activity. The compounds are useful for controlling coccidiosis when administered in minor quantities to animals, in particular to poultry, usually in admixture with animal sustenance.
摘要翻译：公开了新的5-氨基或取代的氨基-1,2,3-三唑具有抗球虫活性。当以少量施用于动物，特别是家禽，通常与动物饲养物混合时，这些化合物可用于控制球虫病。

34. 发明授权

US4816447A Anti-viral guanine compounds 失效
标题翻译：抗病毒鸟嘌呤化合物
公开(公告)号：US4816447A
公开(公告)日：1989-03-28
申请号：US617868
申请日：1984-06-06
申请人： Wallace T. Ashton , Arthur K. Field , John D. Karkas , Richard L. Tolman
发明人： Wallace T. Ashton , Arthur K. Field , John D. Karkas , Richard L. Tolman
IPC分类号： C07D473/18 , A61K31/52 , A61K31/522 , A61P31/12 , C07D473/00 , C07F9/6561
CPC分类号： C07D473/00 , C07F9/65616
摘要： 9-(1,3-Dihydroxy-2-propoxymethyl)guanine and 9-(2,3-dihydroxy-1-propoxymethyl)guanine have been found to have potent anti-viral activity against herpes viruses. These compounds, their acyl derivatives, their phosphate derivatives and their pharmaceutically acceptable salts, pharmaceutical formulations containing these compounds, the treatment of DNA viral or herpes viral infections with these compounds, method of preparing these compounds, and novel intermediates useful in their preparation are all disclosed.The compounds may be prepared by reaction of the appropriate acetoxymethyl ether with diacetylguanine, followed by deprotection. The acetoxymethyl ethers may be obtained by reaction of glycerol formal with acetic anhydride in the presence of a catalyst.
摘要翻译：已经发现9-（1,3-二羟基-2-丙氧基甲基）鸟嘌呤和9-（2,3-二羟基-1-丙氧基甲基）鸟嘌呤对疱疹病毒具有有效的抗病毒活性。这些化合物，其酰基衍生物，其磷酸酯衍生物及其药学上可接受的盐，含有这些化合物的药物制剂，用这些化合物治疗DNA病毒或疱疹病毒感染，制备这些化合物的方法和用于制备这些化合物的新型中间体都是披露化合物可以通过合适的乙酰氧基甲基醚与二乙酰基鸟嘌呤的反应制备，然后脱保护。乙酰氧基甲基醚可以通过甘油缩甲醛与乙酸酐在催化剂存在下反应获得。

35. 发明授权

US4721791A 5-amino or substituted amino 1,2,3-triazoles 失效
公开(公告)号：US4721791A
公开(公告)日：1988-01-26
申请号：US864651
申请日：1986-05-19
申请人： Richard J. Bochis , Elbert Harris , Richard L. Tolman
发明人： Richard J. Bochis , Elbert Harris , Richard L. Tolman
IPC分类号： C07D249/04 , C07D249/06 , A61K31/41
CPC分类号： C07C255/00 , C07D249/04
摘要： Novel 5-amino or substituted amino 1,2,3-triazoles are disclosed as having anticoccidial activity. The compounds are useful for controlling coccidiosis when administered in minor quantities to animals, in particular to poultry, usually in admixture with animal sustenance.

36. 发明授权

US4695624A Covalently-modified polyanionic bacterial polysaccharides, stable covalent conjugates of such polysaccharides and immunogenic proteins with bigeneric spacers, and methods of preparing such polysaccharides and conjugates and of confirming covalency 失效
标题翻译：共价修饰的聚阴离子细菌多糖，这种多糖的稳定共价缀合物和具有更重隔离物的免疫原性蛋白质，以及制备这种多糖和缀合物以及确认共价的方法
公开(公告)号：US4695624A
公开(公告)日：1987-09-22
申请号：US719678
申请日：1985-04-04
申请人： Stephen Marburg , Richard L. Tolman , Peter J. Kniskern
发明人： Stephen Marburg , Richard L. Tolman , Peter J. Kniskern
IPC分类号： A61K39/02 , A61K39/09 , A61K39/095 , A61K39/102 , A61K39/108 , A61K39/385 , A61K39/39 , A61K47/48 , C07K14/22 , C07K17/06 , C07K17/10 , C08B37/00 , C08L99/00 , C12P21/00 , G01N33/531 , G01N33/569 , C07K15/04 , A61K37/02
CPC分类号： G01N33/569 , A61K39/385 , A61K39/39 , A61K47/4823 , A61K47/48338 , C07K17/06 , C07K17/10 , G01N33/531 , A61K2039/55516 , A61K2039/55583 , A61K2039/6031 , A61K2039/627 , Y10S424/831
摘要： Covalently modified bacterial polysaccharides and proteins; covalent conjugates of such polysaccharides linked by a bigeneric spacer, which permits proof of covalency and facilitates purification of conjugated materials, with immunogenic bacterial membrane or other proteins, which conjugates are useful components of bacterial vaccines; and methods of preparing such polysaccharides, proteins and conjugates and of confirming the covalency of the linkage between polysaccharides and proteins.
摘要翻译：共价修饰细菌多糖和蛋白质; 这种多糖的共价缀合物通过增加的间隔基连接，其允许证实共价性并有利于共轭物质的纯化，其具有免疫原性细菌膜或其它蛋白质，所述缀合物是细菌疫苗的有用组分; 以及制备这种多糖，蛋白质和缀合物并确认多糖和蛋白质之间的连接的共价性的方法。

37. 发明授权

US4488991A Bacterial toxoids and gram-negative immune globulin therefrom 失效
标题翻译：细菌类毒素和革兰氏阴性免疫球蛋白
公开(公告)号：US4488991A
公开(公告)日：1984-12-18
申请号：US545565
申请日：1983-10-26
申请人： Richard L. Tolman , Stephen Marburg , Lynn T. Callahan, III
发明人： Richard L. Tolman , Stephen Marburg , Lynn T. Callahan, III
IPC分类号： A61K38/00 , A61K39/104 , C07K16/12 , C07G7/00
CPC分类号： C07K16/12 , A61K39/104 , A61K38/00 , Y10S530/806 , Y10S530/807 , Y10S530/825
摘要： ADP-Ribosylating toxins are rendered enzymatically inactive by reactions with photolabile affinity reagents. The toxoids retain the antigenic and immunogenic properties of the original toxins. These bacterial toxoids can be used as immunogens to protect against the specific disease that the precursor toxins cause or, in the case of P. aeruginosa, the toxoid can be used in combination with E. coli J-5 vaccine to protect against gram-negative bacteremia in general.
摘要翻译： ADP-核糖核酸毒素通过与光不稳定亲和试剂的反应使其酶促无活性。类毒素保留原始毒素的抗原性和免疫原性。这些细菌类毒素可用作免疫原，以防止前体毒素引起的特定疾病，或在铜绿假单胞菌的情况下，类毒素可与大肠杆菌J-5疫苗组合使用，以防止革兰氏阴性菌血症一般。

38. 发明授权

US4156720A Carbohydrate derivatives of milbemycin and processes therefor 失效
公开(公告)号：US4156720A
公开(公告)日：1979-05-29
申请号：US852403
申请日：1977-11-17
申请人： Michael H. Fisher , Richard L. Tolman
发明人： Michael H. Fisher , Richard L. Tolman
IPC分类号： C07D493/20 , C07H17/08 , A61K31/70 , C07G11/00
CPC分类号： C07D493/20 , C07H17/08
摘要： Carbohydrate derivatives of the antibiotic substance milbemycin, also identified as B-41, and of 13-hydroxy milbemycin are prepared. The carbohydrate groups are attached to the available hydroxy groups of milbemycin and to the hydroxy group synthesized at the 13-position. The reactions may be made selectively such that more than one carbohydrate group may be attached to a single position, or that multiple carbohydrate groups may be attached at different positions on the molecule. The described carbohydrate derivatives have antiparasitic activity.

39. 发明授权

US07563618B2 Oligonucleotide conjugates 有权
标题翻译：寡核苷酸缀合物
公开(公告)号：US07563618B2
公开(公告)日：2009-07-21
申请号：US10255535
申请日：2002-09-25
申请人： Sergei Gryaznov , Krisztina Pongracz , Richard L. Tolman , Gregg B. Morin
发明人： Sergei Gryaznov , Krisztina Pongracz , Richard L. Tolman , Gregg B. Morin
IPC分类号： C12Q1/68 , C12N5/00 , A01N43/04 , C07H21/02 , C07H21/04
CPC分类号： A61K47/48092 , A61K47/549 , C07H21/00
摘要： Oligonucleotide conjugates, where an oligonucleotide is covalently attached to an aromatic system, are provided. In particular embodiments the oligonucleotide is complementary to the RNA component of human telomerase and is covalently attached to a nucleobase via an optional linker. The conjugates inhibit telomerase enzyme activity.
摘要翻译：提供寡核苷酸共轭物，其中寡核苷酸共价连接到芳族体系上。在具体实施方案中，寡核苷酸与人端粒酶的RNA组分互补，并通过任选的接头共价连接于核碱基。缀合物抑制端粒酶的活性。

40. 发明授权

US06452014B1 Telomerase inhibitors and methods of their use 失效
标题翻译：端粒酶抑制剂及其使用方法
公开(公告)号：US06452014B1
公开(公告)日：2002-09-17
申请号：US09748622
申请日：2000-12-22
申请人： Tsutomu Akama , Ryan Holcomb , Richard L. Tolman
发明人： Tsutomu Akama , Ryan Holcomb , Richard L. Tolman
IPC分类号： A01N4378
CPC分类号： C07D417/10 , C07D417/14
摘要： Thiazolidinedione compounds, compositions, and methods of inhibiting telomerase activity in vitro and treatment of telomerase mediated conditions or diseases ex vivo and in vivo are provided. The methods, compounds and compositions of the invention may be employed alone, or in combination with other pharmacologically active agents in the treatment of conditions or diseases mediated by telomerase activity, such as in the treatment of cancer. Also disclosed are methods for assaying or screening for inhibitors of telomerase activity.
摘要翻译：提供噻唑烷二酮化合物，组合物和在体外抑制端粒酶活性的方法以及离体和体内治疗端粒酶介导的病症或疾病。本发明的方法，化合物和组合物可以单独使用或与其它药理学活性剂组合用于治疗由端粒酶活性介导的病症或疾病，例如治疗癌症。还公开了用于测定或筛选端粒酶活性抑制剂的方法。

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