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41. 发明授权

US5747473A L-nucleoside analogues and pharmaceutical compositions 失效
标题翻译： L-核苷类似物和药物组合物
公开(公告)号：US5747473A
公开(公告)日：1998-05-05
申请号：US516551
申请日：1995-08-18
申请人： Bjorn Olof Classon , Bengt Bertil Samuelsson , Ingemar Sven-Anders Kvarnstrom , Lars Goran Svansson , Stefan Carl Tore Svensson
发明人： Bjorn Olof Classon , Bengt Bertil Samuelsson , Ingemar Sven-Anders Kvarnstrom , Lars Goran Svansson , Stefan Carl Tore Svensson
IPC分类号： A61K31/505 , A61K31/52 , A61K31/70 , A61K31/7042 , A61K31/7052 , A61K31/7064 , A61K31/7068 , A61K31/7072 , A61K31/7076 , A61K31/708 , A61P31/12 , A61P33/10 , C07D239/46 , C07D405/04 , C07D473/00 , C07D473/02 , C07F9/6512 , C07F9/6558 , C07F9/6561 , C07H19/04 , C07H19/06 , C07H19/10 , C07H19/16 , C07H19/20
CPC分类号： A61K31/70 , A61K31/505 , A61K31/52 , C07D405/04 , C07D473/00 , C07F9/65121 , C07F9/65586 , C07F9/65616 , C07H19/04 , C07H19/06 , C07H19/10 , C07H19/16 , C07H19/20
摘要： ##STR1## Novel antiviral compounds of formulae (1A) and (1B), wherein X and R
1 -R
4 are as stated in claim 1 in the form of an α- or β-anomer or a mixture thereof, and pharmaceutically acceptable salts thereof, are disclosed, as well as a new method for preparation thereof. Said compounds can be used for treatment of infections caused by viruses requiring reverse transcriptase for replication, such as HIV and hepatitis B virus.
摘要翻译：（1A）式（1A）和（1B）的新型抗病毒化合物，其中X和R 1 -R 4如权利要求1中所述，为α-或β-甘油基或其混合物及其药学上可接受的盐，以及其制备方法。所述化合物可用于治疗由需要逆转录酶复制的病毒引起的感染，例如HIV和乙型肝炎病毒。

42. 发明授权

US5473063A Synthesis of furanosyl compounds useful as intermediates in preparation of nucleoside analogues 失效
标题翻译：用作核苷类似物制备中间体的呋喃糖基化合物的合成
公开(公告)号：US5473063A
公开(公告)日：1995-12-05
申请号：US030168
申请日：1993-05-20
申请人： Bjorn O. Classon , Bengt B. Samuelsson , Imgemar S. Kvarnstrom , Lars G. Svansson , Stefan C. T. Svensson
发明人： Bjorn O. Classon , Bengt B. Samuelsson , Imgemar S. Kvarnstrom , Lars G. Svansson , Stefan C. T. Svensson
IPC分类号： A61K31/505 , A61K31/52 , A61K31/70 , A61K31/7042 , A61K31/7052 , A61K31/7064 , A61K31/7068 , A61K31/7072 , A61K31/7076 , A61K31/708 , A61P31/12 , A61P33/10 , C07D239/46 , C07D405/04 , C07D473/00 , C07D473/02 , C07F9/6512 , C07F9/6558 , C07F9/6561 , C07H19/04 , C07H19/06 , C07H19/10 , C07H19/16 , C07H19/20 , C07H3/02 , C07H5/08
CPC分类号： A61K31/70 , A61K31/505 , A61K31/52 , C07D405/04 , C07D473/00 , C07F9/65121 , C07F9/65586 , C07F9/65616 , C07H19/04 , C07H19/06 , C07H19/10 , C07H19/16 , C07H19/20
摘要： Compounds of formulae ##STR1## wherein X is O;R.sup.1 is OH, phosphate, diphosphate, triphosphate or (CH.sub.2).sub.n --O--CH.sub.2 --O--P(.dbd.O)(OH).sub.2 wherein n is 0-2;R.sup.2 is H and R.sup.3 is CH.sub.3, CH.sub.2 OH, CH.sub.2 --O--CH.sub.3, CH.sub.2 SH, CH.sub.2 F or CH.sub.2 N.sub.3 ; orR3 is H and R.sup.2 is CH.sub.3, CH.sub.2 OH, CH.sub.2 --O--CH.sub.3, CH.sub.2 SH, CH.sub.2 F or CH.sub.2 N.sub.3 ;and Z is Cl, Br, I, acyloxy or alkoxy;are synthesized from acyclic intermediates and are subsequently useful in the preparation of nucleoside analogues with antiviral activity against retroviruses such as HIV and hepatitis B.
摘要翻译： PCT No.PCT / SE91 / 00653 Sec。 371日期：1993年5月20日 102（e）日期1993年5月30日PCT 1991年9月27日PCT PCT。公开号WO92 / 06102 日期：1992年4月16日。公式或的化合物，其中X为O; R1是OH，磷酸酯，二磷酸酯，三磷酸酯或（CH2）n-O-CH2-O-P（= O）（OH）2，其中n是0-2; R2是H，R3是CH3，CH2OH，CH2-O-CH3，CH2SH，CH2F或CH2N3; 或R 3为H且R 2为CH 3，CH 2 OH，CH 2 -O-CH 3，CH 2 SH，CH 2 F或CH 2 N 3; Z为Cl，Br，I，酰氧基或烷氧基; 由无环中间体合成，随后可用于制备具有针对逆转录病毒如HIV和乙型肝炎的抗病毒活性的核苷类似物。

43. 发明授权

US5461152A Carbocyclic nucleosides containing bicycle rings, oligonucleotides therefrom, process for their preparation, their use and intermediates 失效
标题翻译：含有自行车环的碳环核苷，其寡核苷酸，其制备方法，用途及中间体
公开(公告)号：US5461152A
公开(公告)日：1995-10-24
申请号：US83812
申请日：1993-06-28
申请人： Karl-Heinz Altmann , Rene Imwinkelried , Albert Eschenmoser
发明人： Karl-Heinz Altmann , Rene Imwinkelried , Albert Eschenmoser
IPC分类号： A61K31/435 , A61K31/505 , A61K31/52 , A61K31/522 , A61P31/12 , C07C215/44 , C07C275/50 , C07D239/46 , C07D239/47 , C07D239/48 , C07D239/50 , C07D239/54 , C07D471/04 , C07D473/00 , C07D473/02 , C07D473/16 , C07D473/18 , C07D473/26 , C07D487/04 , C07F7/18 , C07F9/6512 , C07F9/6561 , C07F9/02 , C07D239/02 , A61K31/695
CPC分类号： C07D239/47 , C07C215/44 , C07C275/50 , C07D239/48 , C07D239/50 , C07D239/54 , C07D473/00 , C07F7/1856 , C07F9/65121 , C07F9/65616 , Y02P20/55
摘要： Compounds of the formulae I and Ia and their racemates ##STR1## in which A is --CH.sub.2 -- or --CH.sub.2 CH.sub.2 --, R.sub.1 is hydrogen or a protective group, R.sub.2 is hydrogen or a protective group or a radical forming a phosphorus-containing nucleotide bridge group and B is a purine or pyrimidine radical or an analogue thereof, can be used as antiviral active ingredients or for the preparation of biologically active oligonucleotides.
摘要翻译：式I和Ia化合物及其外消旋物（Ⅰ）其中A为-CH2-或-CH2CH2-，R1为氢或保护基，R2为氢或保护基或形成含磷核苷酸桥基的基团，B是嘌呤或嘧啶基或其类似物，可以用作抗病毒活性成分或用于制备生物活性寡核苷酸。

44. 发明授权

US5338743A New use of the adenosine antagonist 失效
标题翻译：新使用的腺苷拮抗剂
公开(公告)号：US5338743A
公开(公告)日：1994-08-16
申请号：US847286
申请日：1992-03-10
申请人： Youichi Shiokawa , Atsushi Akahane , Hirohito Katayama , Takafumi Mitsunaga
发明人： Youichi Shiokawa , Atsushi Akahane , Hirohito Katayama , Takafumi Mitsunaga
IPC分类号： A61K31/44 , A61K31/445 , A61K31/495 , A61K31/50 , A61K31/505 , A61K31/52 , A61K31/535 , A61K31/55 , C07D471/04 , C07D473/02 , A61K31/33 , A61K31/395 , A61K31/435 , A61K31/53 , A61K31/54
CPC分类号： C07D471/04 , A61K31/44 , A61K31/445 , A61K31/495 , A61K31/50 , A61K31/505 , A61K31/52 , A61K31/535 , A61K31/55 , C07D473/02
摘要： The present method for the treatment of pancreatitis, which comprises administering an effective amount of a pyrazolopyridine compound of the following formula: ##STR1## wherein R.sup.1 is lower alkyl, (substituted) aryl, or a heterocyclic group,R.sup.2 is a group of the formula ##STR2## wherein R.sup.4 is protected amino or hydroxy and R.sup.5 is hydrogen or lower alkyl; cyano; a group of the formula --A--R.sup.6, wherein R.sup.6 is an acyl group, and A is (halogenated) lower aliphatic hydrocarbon group; amidated carboxy; an unsaturated heterocyclic group; or (protected) amino; andR.sup.3 is hydrogen, lower alkyl, lower alkoxy or halogen; or a pharmaceutically acceptable salt thereof, to a human being having pancreatitis or an animal having pancreatitis in need thereof.
摘要翻译：本发明的治疗胰腺炎的方法包括给予有效量的下式的吡唑并吡啶化合物：其中R1是低级烷基，（取代的）芳基或杂环基，R2是式其中R 4是保护的氨基或羟基，R 5是氢或低级烷基; 氰基; 式-A-R6的基团，其中R6是酰基，A是（卤代）低级脂族烃基; 酰胺羧基; 不饱和杂环基; 或（保护）氨基; 并且R 3是氢，低级烷基，低级烷氧基或卤素; 或其药学上可接受的盐对具有胰腺炎的人或具有需要的胰腺炎的动物。

45. 发明授权

US5258380A (4-piperidinylmethyl and -hetero)purines 失效
标题翻译：（4-哌啶基甲基和 - 杂）嘌呤
公开(公告)号：US5258380A
公开(公告)日：1993-11-02
申请号：US719273
申请日：1991-06-21
申请人： Frans E. Janssens , Gaston S. M. Diels
发明人： Frans E. Janssens , Gaston S. M. Diels
IPC分类号： C07D473/00 , C07D473/30 , C07D473/40 , C07D519/00 , C07D473/02 , A61K31/52
CPC分类号： C07D473/40 , C07D473/00 , C07D473/30
摘要： (4-Piperidinylmethyl and -hetero)purines having antihistaminic properties and being useful agents in the treatment of allergic diseases.
摘要翻译：（4-哌啶基甲基和 - 杂）嘌呤具有抗组胺性质，并且是用于治疗过敏性疾病的有用物质。

46. 发明授权

US5244906A Insect control with substituted oxadiazole and thiadiazole compounds 失效
标题翻译：具有取代的奥沙利多和噻唑烷化合物的防护
公开(公告)号：US5244906A
公开(公告)日：1993-09-14
申请号：US824658
申请日：1992-01-23
申请人： Michael R. Dick , Chi-Ping Chang , James E. Dripps , Susan Wollowitz
发明人： Michael R. Dick , Chi-Ping Chang , James E. Dripps , Susan Wollowitz
IPC分类号： A01N43/824 , A01N43/82 , A01N43/836 , A01N43/90 , C07D401/04 , C07D403/04 , C07D413/04 , C07D471/08 , C07D473/02 , C07D487/08
CPC分类号： C07D413/04 , A01N43/82 , A01N43/90 , C07D471/08 , C07D473/02 , C07D487/08
摘要： Insects, especially sucking insects, such as brown planthoppers, and phytophageous mites, such as two-spotted spider mites, are controlled by applying an oxadiazole or thiadiazole compound substituted on a carbon atom by an aliphatic nitrogen heterocyclic moiety composed of at least one five or six membered ring. The compound 3-(3-amino-1,2,4-oxadiazol-5-yl)-1-azabicyclo[2,2,2]octane is typical.
摘要翻译：昆虫，特别是吮吸昆虫，如褐飞虱和植物螨，如双斑螨，是通过将被二取代的恶二唑或噻二唑化合物置于碳原子上的脂肪族氮杂环部分，由至少一个五六元环。化合物3-（3-氨基-1,2,4-恶二唑-5-基）-1-氮杂双环[2,2,2]辛烷是典型的。

47. 发明授权

US5128458A 2',3'-dideoxy-4'-thioribonucleosides as antiviral agents 失效
标题翻译： 2'，3'-二脱氧-4'-硫脲核苷作为抗病毒剂
公开(公告)号：US5128458A
公开(公告)日：1992-07-07
申请号：US639021
申请日：1991-01-09
申请人： John A. Montgomery , John A. Secrist, III
发明人： John A. Montgomery , John A. Secrist, III
IPC分类号： A61K31/505 , A61K31/52 , A61K31/70 , A61K31/7042 , A61K31/7052 , A61K31/7064 , A61K31/7068 , A61K31/7072 , A61K31/7076 , A61K31/708 , A61K31/7135 , A61P31/12 , C07D409/04 , C07D473/00 , C07D473/02 , C07H19/04 , C07H19/06 , C07H19/16 , C07H23/00
CPC分类号： C07D473/00 , C07D409/04 , C07H19/04 , C07H19/06 , C07H19/16
摘要： 2'3'-dideoxy-4'-thioribonucleosides useful as antiviral agents in the treatment and prevention of AIDS are disclosed. In accordance with one aspect of the invention there are provided compounds of the formula ##STR1## where X=H, N.sub.3 or F, and B is a member selected from the group consisting of pyrimidine, 5-azapyrimidine, 6-azapyrimidine, 3-deazapyrimidine, purine, 3-deazapurine, 7-deazapurine, 8-azapurine, and 2-azapurine bases.The intermediate 1-O-acetyl-5-O-t-butyldiphenylsilyl-4-thio-2,3-dideoxyribofuranose useful in the production of certain of the 2',3'-dideoxy-4'-thioribonucleosides is also disclosed.
摘要翻译：公开了用作治疗和预防艾滋病的抗病毒剂的2'3'-二脱氧-4'-硫脲核苷。根据本发明的一个方面，提供式（I）的化合物，其中X = H，N 3或F，B是选自嘧啶，5-氮杂嘧啶，6-氮杂嘧啶，去氮吡啶，嘌呤，3-脱氮嘌呤，7-脱氮嘌呤，8-氮杂嘌呤和2-氮杂嘌呤碱基。还公开了可用于生产某些2'，3'-二脱氧-4'-硫脲核苷的中间体1-O-乙酰基-5-O-叔丁基二苯基甲硅烷基-4-硫代-2,3-二脱氧呋喃核糖。

48. 发明授权

US4556659A Substituted 9-(1-0- or 3-0-monosubstituted or 1,3-Di-0-substituted propoxymethyl)-purines as antiviral agents 失效
标题翻译：取代的9-（1-0或3-0-单取代或1,3-二-O-取代的丙氧基甲基） - 嘌呤作为抗病毒剂
公开(公告)号：US4556659A
公开(公告)日：1985-12-03
申请号：US406583
申请日：1982-08-09
申请人： Julien P. H. Verheyden , John C. Martin
发明人： Julien P. H. Verheyden , John C. Martin
IPC分类号： C07D473/18 , A61K31/52 , A61K31/522 , A61P31/12 , C07C43/174 , C07C43/178 , C07D473/00 , C07D473/34 , C07D473/40 , C07D473/02
CPC分类号： C07D473/00 , C07C43/1745 , C07C43/1785
摘要： Compounds useful as antiviral agents are defined by the following formula: ##STR1## wherein R.sup.1 is hydrogen, --C(Y)OR.sup.7 or --C(O)NHR.sup.7 wherein R.sup.7 is alkyl of one to twelve carbon atoms, alkenyl of two to twelve carbon atoms, cyclopentyl, cyclohexyl, phenyl or benzyl;R.sup.2 is --C(Y)OR.sup.7 or --C(O)NHR.sup.7 wherein R.sup.7 is as defined above;Y is oxygen or sulfur;R.sup.3 is hydrogen, halo, thio, lower alkylthio of one to six carbon atoms, azido, NR.sup.9 R.sup.10 wherein R.sup.9 and R.sup.10 are independently hydrogen or lower alkyl of one to six carbon atoms or --NHC(O)R.sup.8 wherein R.sup.8 is hydrogen, alkyl of one to nineteen carbon atoms or 1-adamantyl; and(a) R.sup.6 is hydrogen, halo, lower alkoxy of one to six carbon atoms, azido, thio, lower alkylthio of one to six carbon atoms, --NR.sup.9 R.sup.10 wherein R.sup.9 and R.sup.10 are as defined above or --NHC(O)R.sup.8 wherein R.sup.8 is as defined above and R.sup.4 together with R.sup.5 is a bond; or(b) R.sup.5 together with R.sup.6 is a keto group and R.sup.4 is hydrogen.
摘要翻译：可用作抗病毒剂的化合物由下式定义：其中R 1是氢，-C（Y）OR 7或-C（O）NHR 7，其中R 7是1至12个碳原子的烷基，至十二个碳原子，环戊基，环己基，苯基或苄基; R 2是-C（Y）OR 7或-C（O）NHR 7，其中R 7如上所定义; Y是氧或硫; R3是氢，卤素，硫代，1-6个碳原子的低级烷硫基，叠氮基，NR9R10，其中R9和R10独立地是氢或1-6个碳原子的低级烷基或-NHC（O）R8，其中R8是氢，一至十九个碳原子或1-金刚烷基; 和（a）R6是1-6个碳原子的氢，卤素，低级烷氧基，1-6个碳原子的叠氮基，硫代，低级烷硫基，-NR9R10，其中R9和R10如上所定义，或-NHC（O）R 8，其中 R8如上所定义，R4与R5一起是键; 或（b）R 5与R 6一起为酮基，且R 4为氢。

49. 发明授权

US4172829A 2,9-Disubstituted adenine derivatives and their use as non-adrenergic bronchodilators 失效
标题翻译： 2,9-二取代腺嘌呤衍生物及其作为非肾上腺素能支气管扩张剂的用途
公开(公告)号：US4172829A
公开(公告)日：1979-10-30
申请号：US904146
申请日：1978-05-09
申请人： Takayuki Naito , Susumu Nakagawa , Tetsuro Yamasaki , Taka-aki Okita , Haruhiro Yamashita
发明人： Takayuki Naito , Susumu Nakagawa , Tetsuro Yamasaki , Taka-aki Okita , Haruhiro Yamashita
IPC分类号： C07D473/40 , A61K31/52 , A61K31/522 , A61P1/00 , A61P11/08 , C07D473/00 , C07D473/18 , C07D473/02
CPC分类号： C07D473/00 , Y10S514/826
摘要： Purine derivatives of the formula ##STR1## wherein R is C.sub.1 -C.sub.6 alkyl and R.sub.1 is ##STR2## OR ##STR3## AND THEIR PHARMACEUTICALLY ACCEPTABLE ACID ADDITION SALTS ARE NON-ADRENERGIC BRONCHODILATORS.
摘要翻译：式Ⅰ的嘌呤衍生物，其中R是C 1 -C 6烷基，R 1是“或”，并且它们的药物可接受的酸添加剂是非特异性的BRONCHODICATOR。

50. 发明申请

US20180290983A1 INHIBITORS OF NEDD8-ACTIVATING ENZYME 审中-公开
公开(公告)号：US20180290983A1
公开(公告)日：2018-10-11
申请号：US15808491
申请日：2017-11-09
申请人： Millennium Pharmaceuticals, Inc.
发明人： Ashley Sue MCCARRON , Todd B. SELLS , Matthew STIRLING , Stephen G. STROUD
IPC分类号： C07D239/47 , C07D473/02 , C07D239/46
摘要： Disclosed are chemical entities which are inhibitors of Nedd8-activating enzyme (NAE), namely, the compound {(1S,2S,4R)-4-[(6-{[(1R,2S)-5-chloro-2-methoxy-2,3-dihydro-1H-inden-1-yl]amino}pyrimidin-4-yl)oxy]-2-hydroxycyclopentyl}methyl sulfamate and pharmaceutically acceptable salts thereof; solid state forms thereof; and prodrugs thereof. Also disclosed are methods of using the chemical entities to treat disorders such as cancer.

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