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81. 发明申请

WO0183500A8 13-SUBSTITUTED MILBEMYCIN DERIVATIVES, THEIR PREPARATION AND THEIR USE AGAINST INSECTS AND OTHER PESTS 审中-公开
标题翻译： 13取代的甲硫咪啶衍生物，其制备及其对药物和其他药物的使用
公开(公告)号：WO0183500A8
公开(公告)日：2003-05-08
申请号：PCT/JP0103656
申请日：2001-04-26
申请人： SANKYO CO , SAITO AKIO , SUGIYAMA YOKO , TOYAMA TOSHIMITSU , NANBA TOSHIHIKO
发明人： SAITO AKIO , SUGIYAMA YOKO , TOYAMA TOSHIMITSU , NANBA TOSHIHIKO
IPC分类号： C07D493/22 , A01N43/90 , A01P5/00 , A01P7/02 , A01P7/04 , C07H19/01
CPC分类号： C07H19/01 , A01N43/90
摘要： Compounds of formula (I) and salts thereof, wherein: R represents methyl, ethyl, isopropyl or s-butyl; R represents hydrogen or alkyl; R represents hydrogen, optionally substituted alkanoyl, optionally substituted alkenoyl, optionally substituted alkynoyl, alkylsulfonyl, or alkoxycarbonyl, or R and R together with the nitrogen atom to which they are attached form a saturated, optionally substituted 4- to 6-membered heterocyclic ring group; andthe moiety -a- together with the carbon atom to which it is attached forms a 3- to 6-membered cycloalkyl group. These compounds have anthelmintic, acaricidal and insecticidal activity.
摘要翻译：式（I）化合物及其盐，其中：R 1表示甲基，乙基，异丙基或仲丁基; R 2表示氢或烷基; R 3表示氢，任选取代的烷酰基，任选取代的烯酰基，任选取代的炔酰基，烷基磺酰基或烷氧基羰基，或R 2和R 3与它们所连接的氮原子一起形成饱和的，任选取代的 4-至6-元杂环基; 并且该部分与其连接的碳原子一起形成3至6元环烷基。这些化合物具有驱虫，杀螨和杀虫活性。

82. 发明申请

WO0067698A3 METHOD FOR CONTROLLING THE FIDELITY AND EXECUTION OF REVERSE TRANSCRIPTASE BY INCORPORATING AND POLYMERISING NUCLEOTIDE ANALOGUES ACCEPTABLE AS SUBSTRATES WITHOUT BLOCKING ITS ELONGATION 审中-公开
标题翻译：通过并入和聚合核苷酸类似物来控制反向转录酶的残留和执行的方法，其不接受其延伸作为基质
公开(公告)号：WO0067698A3
公开(公告)日：2002-02-14
申请号：PCT/FR0001260
申请日：2000-05-10
申请人： CENTRE NAT RECH SCIENT , DERRIEN VALERIE , REISS CLAUDE
发明人： DERRIEN VALERIE , REISS CLAUDE
IPC分类号： C12N15/09 , A61K31/165 , A61K31/4709 , A61K31/4725 , A61K31/496 , A61K31/506 , A61K31/513 , A61K31/519 , A61K31/551 , A61K31/5513 , A61K31/7048 , A61K31/7068 , A61K31/7072 , A61K31/708 , A61P31/14 , A61P31/18 , A61P35/02 , A61P43/00 , C07H19/01 , C07H19/10 , C07H19/14 , C07H19/20 , A61K31/70 , A61K31/47 , A61K31/495 , A61K31/505 , A61K31/55 , A61K31/66
CPC分类号： A61K31/662 , A61K31/165 , A61K31/4709 , A61K31/496 , A61K31/506 , A61K31/519 , A61K31/551 , A61K31/5513 , A61K31/706 , A61K31/7064 , A61K31/7076 , A61K31/708
摘要： The invention concerns the use of nucleotide analogues, defined as molecules acceptable as substrate of the reverse-transcription response and enabling the addition of at least one supplementary nucleotide to the polynucleotide chain during the reverse transcription to affect and/or to control the fidelity and execution of the reverse transcription. The invention also concerns a pharmaceutical composition containing said nucleotide analogues preferably selected among dUTP, dITP, C7dGTP and C7dATP or characterised in that they have modified bases 6H, 8H-3,4-dihydropyrimido[4,5c][1,2]oxazin-7-one (P) and N methoxy-2,6-diaminopurine (K) alone or mixed with 3'-azido-3'deoxythimidine(AZT), 2',3'-dideoxyinosine-(ddI), 2',3'-dideoxycytidine (ddC), (-)2',3'-dideoxy-3'-theacytidine (3TC), 2',3'-didehydro-2',3'-dideoxythymidine (d4T) and (-)2'-deoxy-5-fluoro-3'-theacytidine (FTC), TIBO (tetrahydroimidazo-(4,5,1-1,jk) (1,4)-benzodiapezine-2-(1H)-one, HEPT (1-[(2-hydroxyethoxy)-methyl]-6-phenylthiothymine), TSAO([2', 5'-bis-O-(tert-butylmethylsilyl)-beta-D-ribofuranosyl]-3'-spiro-5''-(4''-amino-1'',2''-dioxide), alpha -APA (alpha-anilinophenylacetamide), neviparine, BAHP (bis(etheroaryl)-piperazine) or phosphonoformic acid (PFA), indinavir, saquinavir.
摘要翻译：本发明涉及定义为可接受作为逆转录反应底物的分子的核苷酸类似物的用途，并且能够在逆转录过程中向多核苷酸链中加入至少一个补充核苷酸以影响和/或控制保真度和执行的逆转录。本发明还涉及含有优选选自dUTP，dITP，C7dGTP和C7dATP的所述核苷酸类似物的药物组合物，或其特征在于它们具有修饰的碱基6H，8H-3,4-二氢嘧啶并[4,5-c] [1,2] 单独或与3'-叠氮基-3'-脱氧西咪酯（AZT），2'，3'-二脱氧肌苷 - （ddI），2'，3'（3'）连接的N-甲氧基-2,6-二氨基嘌呤（dC），（ - ）2'，3'-二脱氧-3'-氨基胞苷（3TC），2'，3'-二脱氢-2'，3'-二脱氧胸苷（d4T）和（ - ）2' （FTC），TIBO（四氢咪唑并 - （4,5,1-1，jk）（1,4） - 苯并二氮烯-2-（1H） - 酮，HEPT（1- [（2-羟基乙氧基） - 甲基] -6-苯硫基胸腺嘧啶），TSAO（[2'，5'-双-O-（叔丁基甲基甲硅烷基）-β-D-呋喃核糖基] -3'-螺-5“ （4“ - 氨基-1”，2“ - 二氧化物），α-APA（α-苯胺基苯基乙酰胺），neviparine，BAHP（双（乙烯基芳基） - 哌嗪）或膦酰甲酸（PFA），茚地那韦，沙奎那韦。

83. 发明申请

WO01068867A1 POLYKETIDES AND THEIR SYNTHESIS 审中-公开
标题翻译：多晶硅及其合成
公开(公告)号：WO01068867A1
公开(公告)日：2001-09-20
申请号：PCT/GB2000/002072
申请日：2000-05-30
IPC分类号： C07H17/08 , C07H19/01 , C12N15/52 , C12N15/76 , C12P17/18 , C12P19/44 , C12P19/62 , C12Q1/68
CPC分类号： C07H19/01 , C07H17/08 , C07K2319/00 , C12N15/52 , C12N15/76 , C12P17/181 , C12P19/445 , C12P19/62
摘要： The complete sequence of the gene cluster for the monensin type I polyketide synthase, from S. cinnamonensis , is provided. Thus variant polyketides containing monensin-derived elements can be genetically engineered. Furthermore there are features, e.g. a regulatory protein mon RI , which are of wide utility.
摘要翻译：来自S的莫能菌素I型聚酮化合物合酶的完整序列。肉桂属。因此，含有莫能菌素衍生的元件的变体聚酮化合物可以被遗传工程化。此外，还有一些特征，例如一种具有广泛应用的调节性蛋白质单克隆抗体。

84. 发明申请

WO0058328A3 AVERMECTIN DERIVATIVES 审中-公开
标题翻译：阿维菌素衍生物
公开(公告)号：WO0058328A3
公开(公告)日：2001-04-26
申请号：PCT/EP0002189
申请日：2000-03-13
申请人： BAYER AG , HALLENBACH WERNER , HARDER ACHIM , TURBERG ANDREAS , HANSEN OLAF , VON SAMSON HIMMELSTJERNA GEORG
发明人： HALLENBACH WERNER , HARDER ACHIM , TURBERG ANDREAS , HANSEN OLAF , VON SAMSON-HIMMELSTJERNA GEORG
IPC分类号： A61K31/7048 , A61P33/00 , C07H17/08 , C07H19/01 , A01N43/90 , A61K31/70 , A61P33/10
CPC分类号： C07H17/08
摘要： The invention relates to novel avermectin derivatives of formula (I), in which R , R , R and R have the meanings defined in the description. The invention also relates to various methods for producing them, to agents containing them and to their use for producing agents for combating ecto- and endoparasites in animals.
摘要翻译：本发明涉及式（I）中R <1>，R <2>，R <3>和R <4>已经在说明书中给出，其制备方法的几种方法的含义，以组合物以及新型除虫菌素衍生物他们生产的药物在动物控制外部和内部寄生虫使用。

85. 发明申请

WO0039751A3 SYSTEM AND METHOD FOR STRUCTURE-BASED DRUG DESIGN THAT INCLUDES ACCURATE PREDICTION OF BINDING FREE ENERGY 审中-公开
标题翻译：基于结构的药物设计的系统和方法，包括精确预测结合自由能
公开(公告)号：WO0039751A3
公开(公告)日：2001-01-04
申请号：PCT/US9930948
申请日：1999-12-22
申请人： UNIV HARVARD
发明人： DEWITTE ROBERT S , SHAKHNOVICH EUGENE I
IPC分类号： C07D473/00 , C07B61/00 , C07H7/06 , C40B30/02 , C40B40/04 , C40B40/12 , C40B50/02 , G06F17/30 , G06F17/50 , G06F19/16 , G06F19/18 , C07H19/01
CPC分类号： G06F19/706 , G06F19/16 , G06F19/18
摘要： A system and method for providing improved de novo structure-based drug design that includes a method for more accurately predicting binding free energy. The system and method use a coarse-graing model with corresponding knowledge-based potential data to grow ligand candidates and libraries of ligand candidates. In light of the present inventions using coarse-graining model, the novel growth method of the present invention uses a Metropolis Monte Carlo selection process which result in a low energy structure that is not necessarily the lowest energy structure, yet results in a better ligand candidate.
摘要翻译：一种用于提供改进的从头结构的药物设计的系统和方法，其包括用于更准确地预测结合自由能的方法。该系统和方法使用具有相应的基于知识的潜在数据的粗略模型来生长配体候选物和候选配体文库。鉴于使用粗粒度模型的本发明，本发明的新颖生长方法使用大都会蒙特卡罗选择方法，其导致低能量结构，其不一定是最低能量结构，但是导致更好的配体候选。

86. 发明申请

WO0031100A3 BENZYLMALTOSIDES AS INHIBITORS OF SMOOTH MUSCLE CELL PROLIFERATION 审中-公开
标题翻译：苄基马来酰亚胺作为平滑肌细胞增殖的抑制剂
公开(公告)号：WO0031100A3
公开(公告)日：2000-11-23
申请号：PCT/US9927824
申请日：1999-11-23
申请人： AMERICAN HOME PROD
发明人： DOLLINGS PAUL JEFFREY
IPC分类号： A61K31/7028 , A61K31/7056 , A61P9/04 , A61P9/12 , A61P9/14 , A61P11/06 , A61P21/00 , A61P29/00 , A61P35/00 , A61P43/00 , C07H15/18 , C07H19/04 , C07H19/052 , C07H19/01 , A61K31/70 , A61P9/06
CPC分类号： C07H15/18
摘要： This invention provides smooth muscle cell proliferation inhibitors of formula (I) having the structure (I), wherein X is (a), or a pharmaceutically acceptable salt thereof.
摘要翻译：本发明提供具有结构式（I）的式（I）的平滑肌细胞增殖抑制剂，其中X是（a）或其药学上可接受的盐。

87. 发明申请

WO00032617A1 PROCESS FOR PREPARING LIPOPHILIC OLIGOSACCHARIDE ANTIBIOTICS 审中-公开
标题翻译：制备低密度脂蛋白胆固醇抗体的方法
公开(公告)号：WO00032617A1
公开(公告)日：2000-06-08
申请号：PCT/US1999/026020
申请日：1999-11-24
IPC分类号： C07H19/01
CPC分类号： C07H19/01
摘要： Process for preparing a lipophilic oligosaccharide antibiotic containing a nitro group using oxidizing agents and catalysts such as cobalt, manganese and copper having an oxidation state of +2 are disclosed.
摘要翻译：公开了使用氧化剂和氧化态为+2的催化剂如钴，锰和铜制备含有硝基的亲脂寡糖抗生素的方法。

88. 发明申请

WO99043667A1 NOVEL CYCLIC PRO-PERFUMES HAVING MODIFIABLE FRAGRANCE RAW MATERIAL ALCOHOL RELEASE RATE 审中-公开
标题翻译：具有可改性的FRAGRANCE原料酒精释放率的新型循环型
公开(公告)号：WO99043667A1
公开(公告)日：1999-09-02
申请号：PCT/US1999/002732
申请日：1999-02-08
IPC分类号： A61K8/49 , A61Q13/00 , C07D317/34 , C07D317/46 , C07D317/72 , C07D319/06 , C07D319/08 , C07H9/04 , C11B9/00 , A61K7/46 , C07H19/01
CPC分类号： C07H9/04 , C07D317/34 , C07D317/46 , C07D317/72 , C07D319/06 , C07D319/08 , C11B9/00 , C11B9/0073
摘要： The present invention relates to novel cyclic pro-perfumes having general formula (I), wherein -OR is a moiety derived from a fragrance raw material alcohol, preferably a tertiary alcohol. The cyclic pro-perfumes of the present invention preferably comprise dioxolane and glucosyl orthoesters suitable for use in delivering enhanced fragrance longevity to human skin when used in perfumes and fine fragrances.
摘要翻译：本发明涉及具有通式（I）的新型环状前香料，其中-OR是衍生自香料原料醇，优选叔醇的部分。本发明的环状前体香料优选包含二氧戊环和葡萄糖基原酸酯，当用于香料和精细香料时，其适合用于向人体皮肤递送增强的香料寿命。

89. 发明申请

WO99018798A1 COMPOSITIONS AND METHODS FOR THE TREATMENT OF PRIMARY AND METASTATIC NEOPLASTIC DISEASES USING ARSENIC COMPOUNDS 审中-公开
标题翻译：用ARSENIC化合物治疗原发性和分化性神经性疾病的组合物和方法
公开(公告)号：WO99018798A1
公开(公告)日：1999-04-22
申请号：PCT/US1998/021782
申请日：1998-10-15
IPC分类号： C07D239/553 , A61K9/08 , A61K31/05 , A61K31/166 , A61K31/17 , A61K31/203 , A61K31/282 , A61K31/337 , A61K31/433 , A61K31/519 , A61K31/522 , A61K31/525 , A61K31/565 , A61K31/568 , A61K31/7008 , A61K31/7028 , A61K31/7034 , A61K31/704 , A61K31/7042 , A61K31/7048 , A61K33/24 , A61K33/36 , A61K38/00 , A61K39/00 , A61K45/00 , A61K45/06 , A61P35/00 , A61P35/02 , A61P35/04 , C07D305/14 , C07D475/04 , C07D519/04 , C07H5/06 , C07H15/252 , C07H19/01 , C07J41/00 , A01N59/22
CPC分类号： A61K45/06 , A61K31/568 , A61K33/36 , Y10S514/908 , A61K31/00 , A61K2300/00
摘要： The invention relates to the use of arsenic compounds to treat a variety of neoplastic diseases (see the dose response curves in the Figure). Further, the arsenic compounds may be used to treat metastatic neoplastic diseases.
摘要翻译：本发明涉及砷化合物用于治疗各种肿瘤疾病（参见图中的剂量反应曲线）。此外，砷化合物可用于治疗转移性肿瘤疾病。

90. 发明申请

WO99005156A1 PRODUCTION OF AVERMECTIN COMPOUNDS 审中-公开
标题翻译：生产化合物
公开(公告)号：WO99005156A1
公开(公告)日：1999-02-04
申请号：PCT/IB1998/000988
申请日：1998-06-25
IPC分类号： A61K31/7048 , A61P33/10 , C07H17/08 , C07H19/01 , A61K31/70
CPC分类号： C07H17/08 , Y02P20/55
摘要： This invention provides a process for preparing a compound of formula (I): wherein R is H or a hydroxyimino-protecting group; R is H, C1-4 alkyl or C1-4 alkoxy; R is C1-8 alkyl, C2-8 alkenyl or C3-8 cycloalkyl; and R is H, halo, C1-4 alkyl or C1-4 alkoxy, which process comprises the steps of: (a) reacting an avermectin B2 derivative with an oxidizing agent to form a 5-oxo compound; (b) allowing the 5-oxo compound to react with a compound of formula R -O-NH2 wherein R is H or a hydroxyimino-protecting group, to form a 5-imino compound; (c) reacting the 5-imino compound with a thionocarbonizing agent to form a 4'', 23-bisthionocarbonyl ester; (d) reacting the 4'', 23-bisthionocarbonyl ester with a deoxygenation agent to form a 4'', 23-dideoxy compound; and (e) reacting the 4'', 23-dideoxy compound with an acid to form a compound of formula (I).
摘要翻译：本发明提供制备式（I）化合物的方法：其中R 1是H或羟基亚氨基保护基; R 2是H，C 1-4烷基或C 1-4烷氧基; R 3是C 1-8烷基，C 2-8链烯基或C 3-8环烷基; 和R 4是H，卤素，C 1-4烷基或C 1-4烷氧基，该方法包括以下步骤：（a）使除虫菌素B2衍生物与氧化剂反应形成5-氧代化合物; （b）使5-氧代化合物与式R 1 -O-NH 2的化合物反应，其中R 1为H或羟基亚氨基保护基，形成5-亚氨基化合物; （c）使5-亚氨基化合物与硫羰化剂反应形成4“，23-双硫羰基酯; （d）使4“，23-双硫代羰基酯与脱氧剂反应以形成4”，23-二脱氧化合物; 和（e）使4“，23-二脱氧化合物与酸反应以形成式（I）的化合物。

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