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1. 发明申请

WO2013174017A1 制备全保护的肝素五糖的方法及其中间体审中-公开
公开(公告)号：WO2013174017A1
公开(公告)日：2013-11-28
申请号：PCT/CN2012/076096
申请日：2012-05-25
申请人：浙江海正药业股份有限公司 , 丁毅力 , 郭阳辉 , 白骅 , 吴迎秋 , 杨璇 , 晏青燕 , 柴健
发明人：丁毅力 , 郭阳辉 , 白骅 , 吴迎秋 , 杨璇 , 晏青燕 , 柴健
IPC分类号： C07H5/04 , C07H5/10 , A61K31/702 , A61P7/02
CPC分类号： C07H15/207 , A61K31/702 , C07H1/00 , C07H5/10 , C07H15/04 , C07H15/18 , C07H15/203
摘要：一种化学合成药物中间体的工艺，特别是一种抗凝血药物磺达肝癸钠中间体全保护肝素五糖的合成新工艺及新的中间体被公开，该工艺反应效率高，反应操作简单，反应中间体易纯化，适合全保护肝素五糖工业化生产。

2. 发明申请

WO2004038006A2 PURINE NUCLEOSIDES 审中-公开
标题翻译：嘌呤核苷
公开(公告)号：WO2004038006A2
公开(公告)日：2004-05-06
申请号：PCT/US0333987
申请日：2003-10-24
申请人： US GOV HEALTH & HUMAN SERV , EWHA WOMANS UNIVERSITY , JEONG LAK SHIN , JACOBSON KENNETH A , MOON HYUNG RYONG , KIM HEA OK
发明人： JEONG LAK SHIN , JACOBSON KENNETH A , MOON HYUNG RYONG , KIM HEA OK
IPC分类号： A61K31/52 , A61K31/7076 , A61P29/00 , A61P35/00 , C07D473/00 , C07D473/14 , C07D473/32 , C07D473/34 , C07H19/16 , C07H19/167 , C12N
CPC分类号： C07H5/10 , C07D473/00 , C07D473/32 , C07D473/34 , C07H19/16 , C07H19/167
摘要： Disclosed are purine nucleoside compounds that are selective to A3 adenosine receptors and are useful for the treatment of cancer and inflammatory diseases. The compounds are shown by the following general formula (I), including isomers thereof: wherein X is sulfur or oxygen; Rl is hydrogen, alkyl, benzyl, halobenzyl, or phenylalkyl; R2 is hydrogen, halogen, alkoxy, alkenyl, alkynyl, alkylthio, or thio; R3 and R3' are hydrogen, hydroxyalkyl, alkoxycarbonyl, or alkylaminocabonyl, whereas R3 and R3' do not have identical substituents simultaneously; and R4 is hydrogen or alkyl. Also disclosed are a pharmaceutical composition comprising a compound of formula (I), an isomer, or its pharmacologically acceptable salt as an active ingredient and a method for preventing or treating various diseases, state, or condition, including asthma, inflammation, cerebral ischemia, heart diseases, and cancer.
摘要翻译：公开了对A3腺苷受体具有选择性并可用于治疗癌症和炎性疾病的嘌呤核苷化合物。所述化合物由以下通式（I）表示，包括其异构体：其中X是硫或氧; R1是氢，烷基，苄基，卤代苄基或苯基烷基; R2是氢，卤素，烷氧基，烯基，炔基，烷硫基或硫代; R3和R3'是氢，羟基烷基，烷氧基羰基或烷基氨基羰基，而R3和R3'不同时具有相同的取代基; 和R4是氢或烷基。还公开了包含式（I）化合物，异构体或其药理学上可接受的盐作为活性成分的药物组合物以及用于预防或治疗各种疾病，状态或病症（包括哮喘，炎症，脑缺血，心脏疾病和癌症。

3. 发明申请

WO03097657A9 AN ANTIMICROBIAL AGENT 审中-公开
标题翻译：抗菌药物
公开(公告)号：WO03097657A9
公开(公告)日：2004-03-11
申请号：PCT/AU0300620
申请日：2003-05-22
申请人： UNIV GRIFFITH , VON ITZSTEIN LAURENCE MARK , DAVIS CHRISTOPHER BONNER , THOMSON ROBIN JOY
发明人： VON ITZSTEIN LAURENCE MARK , DAVIS CHRISTOPHER BONNER , THOMSON ROBIN JOY
IPC分类号： A61K31/7004 , A61K31/7028 , A61P31/04 , C07H5/10 , C07H15/14 , C07H15/18
CPC分类号： C07H5/10 , A61K31/7004 , C07H15/14 , C07H15/18
摘要： The present invention relates to novel thioglycosides of D-galactofuranose that have an antimicrobial action, methods for their synthesis, pharmaceutical compositions containing them and methods for the treatment of patients suffering microbial infection.
摘要翻译：本发明涉及具有抗微生物作用的D-半乳糖呋喃糖的新型硫代糖苷，其合成方法，含有它们的药物组合物和用于治疗患有微生物感染的患者的方法。

4. 发明申请

WO2003097657A1 AN ANTIMICROBIAL AGENT 审中-公开
标题翻译：抗菌药物
公开(公告)号：WO2003097657A1
公开(公告)日：2003-11-27
申请号：PCT/AU2003/000620
申请日：2003-05-22
申请人： GRIFFITH UNIVERSITY , VON ITZSTEIN, Laurence, Mark , DAVIS, Christopher, Bonner , THOMSON, Robin, Joy
发明人： VON ITZSTEIN, Laurence, Mark , DAVIS, Christopher, Bonner , THOMSON, Robin, Joy
IPC分类号： C07H15/14
CPC分类号： C07H5/10 , A61K31/7004 , C07H15/14 , C07H15/18
摘要： The present invention relates to novel thioglycosides of D-galactofuranose that have an antimicrobial action, methods for their synthesis, pharmaceutical compositions containing them and methods for the treatment of patients suffering microbial infection.
摘要翻译：本发明涉及具有抗微生物作用的D-半乳糖呋喃糖的新型硫代糖苷，其合成方法，含有它们的药物组合物和用于治疗患有微生物感染的患者的方法。

5. 发明申请

WO01057053A1 METHOD FOR PREPARING FUNCTIONALISED BETA-(1,3)-GLUCAN DERIVATIVES 审中-公开
标题翻译：制备功能性β-（1,3） - 葡萄糖衍生物的方法
公开(公告)号：WO01057053A1
公开(公告)日：2001-08-09
申请号：PCT/FR2001/000329
申请日：2001-02-02
IPC分类号： A61K8/60 , A61K8/73 , A61K31/7028 , A61P43/00 , C07H5/10 , C07H13/02 , C07H15/04 , C07H15/18 , C07H1/00
CPC分类号： C07H5/10 , C07H13/02 , C07H15/04
摘要： The invention concerns a novel method for preparing by chemical process functionalised beta -(1,3)-glucan derivatives, enabling to obtain free oligosaccharides or comprising specific groups such as, for instance, sulphate, phosphate, methyl, in predetermined positions. Said method consists in reacting a glycosyl donor of formula (Ia) or (Ib) with a glycosyl scavenger of formula (II), as defined in the claims. The invention is useful for preparing biologically active principles for use in the agricultural, cosmetic or pharmaceutical field.
摘要翻译：本发明涉及一种通过化学方法制备官能化β-（1,3） - 葡聚糖衍生物的新方法，其能够获得游离的寡糖或包含特定基团，例如硫酸根，磷酸根，甲基，在预定位置。所述方法包括使式（Ia）或（Ib）的糖供体与如权利要求中所定义的式（II）的糖基清除剂反应。本发明可用于制备用于农业，化妆品或制药领域的生物活性成分。

6. 发明申请

WO99028312A1 NOVEL ANTICOAGULANT GLYCOSIDES AND PHARMACEUTICAL COMPOSITIONS THEREOF 审中-公开
标题翻译：新型抗血清糖蛋白及其药物组合物
公开(公告)号：WO99028312A1
公开(公告)日：1999-06-10
申请号：PCT/HU1998/000099
申请日：1998-12-03
IPC分类号： C07D335/02 , C07H5/10 , A61K31/70 , C07H15/14
CPC分类号： C07H5/10 , C07D335/02
摘要： This invention relates to novel 1,5-dithio-L- and D-arabinopyranosides of formula (I), wherein R represents a cyano, nitro, aminothiocarbonyl, amidino or an acetamido group and the acid addition salts thereof formed with organic or inorganic acids, if possible as well as pharmaceutical compositions containing them. The compounds of the invention possess valuable therapeutic, particularly anticoagulant properties.
摘要翻译：本发明涉及式（I）的新的1,5-二硫代-L-和D-阿拉伯吡喃糖苷，其中R表示氰基，硝基，氨基硫代羰基，脒基或乙酰氨基，并且其与有机或无机酸形成的酸加成盐如果可能，以及含有它们的药物组合物。本发明的化合物具有有价值的治疗，特别是抗凝血性质。

7. 发明申请

WO9846243A3 PHARMACEUTICAL COMPOSITIONS HAVING APPETITE SUPPRESSANT ACTIVITY 审中-公开
标题翻译：具有显着抑制活性的药物组合物
公开(公告)号：WO9846243A3
公开(公告)日：1999-02-25
申请号：PCT/GB9801100
申请日：1998-04-15
申请人： CSIR , ABRAMS MICHAEL JOHN , HEERDEN FANIE RETIEF VAN , VLEGGAAR ROBERT , HORAK ROELOF MARTHINUS , LEARMONTH ROBIN ALEC , MAHARAJ VINESH , WHITTAL RORY DESMOND
发明人： VAN HEERDEN FANIE RETIEF , VLEGGAAR ROBERT , HORAK ROELOF MARTHINUS , LEARMONTH ROBIN ALEC , MAHARAJ VINESH , WHITTAL RORY DESMOND
IPC分类号： A23L1/30 , A23L1/307 , A61K20060101 , A61K9/14 , A61K9/19 , A61K31/44 , A61K31/57 , A61K31/58 , A61K31/704 , A61K31/75 , A61K31/78 , A61K36/00 , A61K36/18 , A61K36/27 , A61K39/385 , A61K45/00 , A61P3/04 , C07D20060101 , C07F20060101 , C07G99/00 , C07H20060101 , C07H3/02 , C07H3/04 , C07H3/06 , C07H5/10 , C07H13/08 , C07J20060101 , C07J7/00 , C07J15/00 , C07J17/00 , C07J71/00 , A61K35/78
CPC分类号： A61K31/57 , A23L33/105 , A61K31/58 , A61K31/704 , A61K31/78 , A61K36/27 , C07H3/04 , C07H3/06 , C07H5/10 , C07H13/08 , C07J7/002 , C07J7/0025 , C07J7/0035 , C07J7/007 , C07J15/00 , C07J17/00 , C07J17/005 , C07J41/00 , Y02P20/582 , A61K2300/00
摘要： A pharmaceutical composition contains an extract obtainable from a plant of the genus Trichocaulon or Hoodia containing an appetite suppressant agent having the formula (1). A process for obtaining the extract and a process for synthesizing compound (1) and its analogues and derivatives is also provided. The invention also extends to the use of such extracts and compound (1) and its analogues for the manufacture of medicaments having appetite suppressant activity. The invention further provides novel intermediates for the synthesis of compound (1).
摘要翻译：药物组合物含有可从含有具有式（1）的食欲抑制剂的Trichocaulon或Hoodia属的植物获得的提取物。还提供了获得提取物的方法和合成化合物（1）的方法及其类似物和衍生物。本发明还涉及这种提取物和化合物（1）及其类似物用于制造具有食欲抑制活性的药物的用途。本发明还提供了用于合成化合物（1）的新型中间体。

8. 发明申请

WO99007719A1 PRODRUGS AND CONJUGATES OF THIOL- AND SELENOL- CONTAINING COMPOUNDS AND METHODS OF USE THEREOF 审中-公开
标题翻译：含硫和含SELENOL的化合物的制备和结合及其使用方法
公开(公告)号：WO99007719A1
公开(公告)日：1999-02-18
申请号：PCT/US1998/016324
申请日：1998-08-06
IPC分类号： C07D293/06 , C07H5/00 , C07H5/10 , C07H15/26 , C07H17/00 , C07H5/04 , C07H5/06 , C07H15/00
CPC分类号： C07H5/00 , C07D293/06 , C07H5/10 , C07H15/26 , C07H17/00
摘要： Disclosed is a prodrugs of the formula (I) where A is a sulfur or a selenium, and R is derived from a mono- di- or oligosaccharide. Also disclosed is a prodrug of the formulas (II); where A is sulfur or selenium, R' is derived from a sugar and R' has the formula (CHOH)nCH2OH, where n is 1 to 5, or R' is an alkyl or aryl group, or R' is =O, and the R'' groups may be the same or different and may be hydrogen, alkyl, alkoxy, carboxy. Also disclosed is a conjugate of an antioxidant vitamin and a thiolamine or selenolamine. Also disclosed is a prodrug of the formula (III); where A is sulfur or selenium, and R' is derived from a sugar and R' has the formula (CHOH)nCH2OH, where n is 1 to 5, or R' is also an alkyl or aryl group, or R' is =O, and R is an alkoxy, or an amine group. Also disclosed is a prodrug of the formula (IV) R is COOH or H, and R' is derived from a sugar and R' has the formula (CHOH)nCH2OH, where n is 1 to 5, or R' is an alkyl or aryl group, or R' is =O.
摘要翻译：公开了式（I）的前药，其中A是硫或硒，R衍生自单糖或寡糖。还公开了式（II）的前药; 其中A是硫或硒，R'衍生自糖，R'具有式（CHOH）n CH 2 OH，其中n为1至5，或R'为烷基或芳基或R'为= O，和 R“可以相同或不同，可以是氢，烷基，烷氧基，羧基。还公开了抗氧化维生素和硫胺或硒胺的缀合物。还公开了式（III）的前药; 其中A是硫或硒，R'来自糖，R'具有式（CHOH）nCH 2 OH，其中n为1至5，或R'也为烷基或芳基，或R'为= O ，R +是烷氧基或胺基。还公开了式（IV）的前药：R是COOH或H，R'来自糖，R'具有式（CHOH）n CH 2 OH，其中n为1至5，或R'为烷基或芳基或R'= O。

9. 发明申请

WO99007718A2 SUBSTITUTED TETRAHYDROPYRANE DERIVATIVES, METHOD FOR PRODUCING SAME, THEIR USE AS MEDICINE OR DIAGNOSTIC AGENT, AS WELL AS MEDICINE CONTAINING SAME 审中-公开
标题翻译：取代的四氢，制造方法药物或诊断和含有药物的使用
公开(公告)号：WO99007718A2
公开(公告)日：1999-02-18
申请号：PCT/EP1998/005025
申请日：1998-08-07
IPC分类号： C07H15/00 , A61K31/7028 , A61K31/7034 , C07H5/10 , C07H15/04 , C07H15/12 , C07H
CPC分类号： C07H15/12 , C07H5/10 , C07H15/04
摘要： The invention relates to compounds of the formula (I), in which the rests R , R , R , R , R and X have the meaning given to them in the description, a method for producing the compounds of formula (I) in a solid phase, and their use as medicines.
摘要翻译：本发明涉及式（I）的化合物，其中基团R <1>，R <2>，R <3>，R <4>，R <5>和X具有说明书中给出的含义，一种方法式（I）在固相上的化合物的制备以及它们作为药物的用途。

10. 发明申请

WO98058940A1 ACTIVATED MONO-, DI-, OLIGO- AND POLYSACCHARIDES, REACTION PRODUCTS THEREOF, THEIR PREPARATION AND USES 审中-公开
标题翻译：活性单体，二 - ，二乙酸和多元醇，其反应产物，其制备和用途
公开(公告)号：WO98058940A1
公开(公告)日：1998-12-30
申请号：PCT/US1998/012767
申请日：1998-06-19
IPC分类号： C07H3/04 , C07H5/10 , C08B11/00 , C08B15/00 , C08B33/00 , C07H3/06 , C07H3/10 , C07H5/02 , C07H15/04 , C08B11/04 , C08B11/10 , C08B31/12 , C08B33/04 , C08B37/00
CPC分类号： C07H3/04 , C07H5/10 , C08B11/00 , C08B15/00 , C08B33/00
摘要： Reaction at the interface of an organic solution containing an acidic reactant and an aqueous alkaline solution containing nonreducing carbohydrates such as sucrose, sugar alcohols, cyclodextrines, and polysaccharides imparts a specificity to the reaction for one or more of the primary alcohol groups of the carbohydrate reactant. The resulting activated, nonreducing carbohydrate intermediate can then be converted to a series of substantially pure, low molecular weight reaction products, including a sucrose trimer and dianhydrosucrose, and to a series of substantially pure, higher molecular weight reaction products, including 6-O-sucro cyclodextrins and poly-6-O-sucro amylose.
摘要翻译：在含有酸性反应物的有机溶液和含有非还原性碳水化合物如蔗糖，糖醇，环糊精和多糖的碱性水溶液的界面处的反应赋予碳水化合物反应物的一个或多个伯醇基团的反应特异性。然后将所得活化的非还原性碳水化合物中间体转化为一系列基本上纯的低分子量反应产物，包括蔗糖三聚体和二氢蔗糖，以及一系列基本上纯的较高分子量的反应产物，包括6-O- 蔗糖环糊精和聚-6-O-琥珀酸直链淀粉。

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