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1. 发明申请

WO2004009608A2 NOVEL AMORPHOUS 9-DEOXO-9A-AZA-9A-METHYL-9A-HOMOERYTHROMYCIN A, PROCESS FOR PREPARING THE SAME, AND USE THEREOF 审中-公开
标题翻译：新型无定形9-脱氧-9A-AZA-9A-甲基-9a-异丙基黄霉素A及其制备方法及其用途
公开(公告)号：WO2004009608A2
公开(公告)日：2004-01-29
申请号：PCT/HR0300040
申请日：2003-07-21
申请人： PLIVA D D , DUMIC MILJENKO , VINKOVIC MLADEN , ORESIC MARINA , MESTROVIC ERNEST , DANILOVSKI ALEKSANDAR , DUMBOVIC ALOJZ , KNEZEVIC ZDRAVKA , LAZAREVSKI GORJANA , FILIC DARKO , CINCIC DOMINIK , LAZARIC KATICA , BUCAR DEJAN-KRESIMIR
发明人： DUMIC MILJENKO , VINKOVIC MLADEN , ORESIC MARINA , MESTROVIC ERNEST , DANILOVSKI ALEKSANDAR , DUMBOVIC ALOJZ , KNEZEVIC ZDRAVKA , LAZAREVSKI GORJANA , FILIC DARKO , CINCIC DOMINIK , LAZARIC KATICA , BUCAR DEJAN-KRESIMIR
IPC分类号： C07H17/08 , C07H17/00
CPC分类号： C07H17/08
摘要： Substantially pure amorphous 9-deoxo-9a-aza-9a-methyl-9a-homoerythromycin A. In addition, this disclosure is directed to a process for the preparation thereof from crude 9-deoxo-9a-aza-9amethyl-9a-homoerythromycin A via orthorhombic isostructural pseudopolymorphs of 9-deoxo9a-aza-9a-methyl-9a-homoerythromycin A, of the general formula I x H2O x S I wherein S represents a water-miscible or water-immiscible organic solvent, characterized by the orthorhombic space group P212121, with average unit cell parameters a = 8.2 to 9.7 Å, b = 11.5 to 13.5 Å, c = 44.5 to 47.0 Å, alpha =beta = gamma = 90°, wherein a, b and c represent the crystal axes lengths and alpha, beta and gamma represent the angles between the crystal axes. In addition, pharmaceutical compositions containing the substantially pure amorphous 9-deoxo9a-aza-9a-methyl-9a-homoerythromycin A are disclosed, as well as a method for the treatment of bacterial and protozoal infections, and inflammation related diseases in humans and animals by administration of a pharmaceutical composition containing same.
摘要翻译：基本上纯的无定形9-脱氧-9a-氮杂-9a-甲基-9a-高红霉素A.此外，本公开涉及由粗制9-脱氧-9a-氮杂-9a-甲基-9a-高红霉素A制备它的方法通过通式I x H 2 O x SI的9-脱氧-9a-氮杂-9a-甲基-9a-高红霉素A的斜方同晶同构假多晶型物，其中S表示水混溶性或与水不混溶的有机溶剂，其特征在于正交空间群P212121 其平均晶胞参数a = 8.2至9.7，b = 11.5至13.5，c = 44.5至47.0，α=β=γ= 90°，其中a，b和c代表晶轴长度和α， β和γ代表晶轴之间的角度。此外，还公开了含有基本上纯的无定形9-脱氧-9a-氮杂-9a-甲基-9a-高红霉素A的药物组合物以及治疗人和动物的细菌和原生动物感染以及炎症相关疾病的方法，给予含有它们的药物组合物。

2. 发明申请

WO9920639A3 NOVEL 3,6-HEMIKETALS FROM THE CLASS OF 9a-AZALIDES 审中-公开
标题翻译： 9a-AZALIDES类新型3,6-HEMGETETALS
公开(公告)号：WO9920639A3
公开(公告)日：1999-07-08
申请号：PCT/HR9800005
申请日：1998-10-13
申请人： PLIVA PHARM & CHEM WORKS , KOBREHEL GABRIJELA , LAZAREVSKI GORJANA , VINKOVIC MLADEN
发明人： KOBREHEL GABRIJELA , LAZAREVSKI GORJANA , VINKOVIC MLADEN
IPC分类号： C07H17/00 , A61K31/70 , A61K31/7042 , A61K31/7048 , A61K31/7052 , A61P31/04 , C07H17/08
CPC分类号： C07H17/08 , C07H17/00
摘要： The invention relates to compounds of general formula (I) characterized in that R individually stands for hydroxyl, L-cladinosyl group of formula (II) wherein R individually stands for hydrogen or a silyl group; R individually stands for hydrogen or together with R stands for an ether group; R individually stands for hydrogen, (C -C )acyl group or -COO-(CH2)n-Ar group, wherein n is 1-7 and Ar individually stands for unsubstituted or substituted aryl group with up to 18 carbon atoms; R individually stands for hydrogen, methyl group or -COO-(CH2)n-Ar group, wherein n is 1-7 and Ar individually stands for unsubstituted or substituted aryl group with up to 18 carbon atoms; R individually stands for a hydroxyl group or together with R stands for an ether group; R individually stands for hydrogen, (C1-C12)alkyl group, silyl group or together with R and C-11/C-12 carbon atoms stands for a cyclic carbonate, R individually stands for hydrogen, (C1-C12)alkyl group, silyl group or together with R and C-11/C-12 carbon atoms stands for a cyclic carbonate; and its pharmaceutically acceptable additions salts with inorganic or organic acids, to a process for the preparation thereof and to the use thereof as antibiotics or as intermediates for the synthesis of other macrolide antibiotics.
摘要翻译：本发明涉及通式（I）的化合物，其特征在于R 1分别代表羟基，式（II）的L-克拉定糖基，其中R 2分别代表氢或甲硅烷基; R 3分别代表氢或与R 6一起代表醚基; R 4分别代表氢，（C 1 -C 4）酰基或-COO-（CH 2）n -Ar基，其中n是1-7，Ar分别代表未取代或取代的芳基具有多达18个碳原子; R 5分别代表氢，甲基或-COO-（CH 2）n -Ar基团，其中n是1-7，Ar分别代表具有至多18个碳原子的未取代或取代的芳基; R 6分别代表羟基或与R 3一起代表醚基; R 7分别代表氢，（C 1 -C 12）烷基，甲硅烷基或与R 8和C-11 / C-12一起代表环碳酸酯，R 8分别代表氢，（C 1 -C 12）烷基，甲硅烷基或与R 7和C-11 / C-12碳原子一起代表环状碳酸酯; 及其与无机或有机酸的药学上可接受的加成盐，其制备方法及其作为抗生素或用作合成其他大环内酯类抗生素的中间体的用途。

3. 发明申请

WO2007010285A3 CRYSTAL STRUCTURE OF HUMAN SOLUBLE ADENYLATE CYCLASE 审中-公开
标题翻译：人溶性腺苷酸环化酶的晶体结构
公开(公告)号：WO2007010285A3
公开(公告)日：2007-05-18
申请号：PCT/GB2006002750
申请日：2006-07-21
申请人： ASTEX THERAPEUTICS LTD , SAALAU-BETHELL SUSANNE MARIA , CLEASBY ANNE , SAMBROOK TRACEY ANN , COYLE JOSEPH , VINKOVIC MLADEN
发明人： SAALAU-BETHELL SUSANNE MARIA , CLEASBY ANNE , SAMBROOK TRACEY ANN , COYLE JOSEPH , VINKOVIC MLADEN
IPC分类号： C12N9/88 , G01N33/00
CPC分类号： C12N9/88 , C07K2299/00
摘要： The invention provides the crystal structure of the solAC catalytic domain. The structure is set out in Tables 1 to 5. The structure may be used in to model the interaction of ligands such as pharmaceutical compounds with this protein, and to determine the structure of related adenylate cyclase molecules.
摘要翻译：本发明提供了solAC催化结构域的晶体结构。该结构列于表1至5中。该结构可用于模拟配体如药物化合物与该蛋白质的相互作用，并确定相关腺苷酸环化酶分子的结构。

4. 发明申请

WO2007129066A8 4- (2,6-DICHLORO-BENZOYLAMINO) -1H-PYRAZOLE-3-CARBOXYLIC ACID (1-METHANESULPHONYL-PIPERIDIN-4-YL) -AMIDE FOR THE TREATMENT OF CANCER 审中-公开
标题翻译：用于治疗癌症的4-（2,6-二氯苯甲酰氨基）-1H-吡唑-3-羧酸（1-甲磺酰基 - 哌啶-4-基）酰胺
公开(公告)号：WO2007129066A8
公开(公告)日：2008-02-21
申请号：PCT/GB2007001655
申请日：2007-05-04
申请人： ASTEX THERAPEUTICS LTD , TREWARTHA GARY , NAVARRO EVA FIGUEROA , REES DAVID CHARLES , VINKOVIC MLADEN , WOODHEAD ANDREW JAMES , WYATT PAUL GRAHAM
发明人： TREWARTHA GARY , NAVARRO EVA FIGUEROA , REES DAVID CHARLES , VINKOVIC MLADEN , WOODHEAD ANDREW JAMES , WYATT PAUL GRAHAM
IPC分类号： C07D401/12 , A61K31/4155 , A61P35/00
CPC分类号： C07D401/12
摘要： The invention provides the compound of formula (I) 4-(2,6-dichloro-benzoylamino)-1H-pyrazole- 3-carboxylic acid (l-methanesulphonyl-piperidin-4-yl)-amide in a substantially crystalline form, therapeutic uses thereof and pharmaceutical compositions containing the crystalline compound. The invention also provides novel pharmaceutical formulations containing 4-(2,6-dichloro-benzoylamino)-1H-pyrazole-3-carboxylic acid (1-methanesulphonyl-piperidin-4-yl)-amide and novel processes for preparing the compound.
摘要翻译：本发明提供基本上为结晶形式的式（I）4-（2,6-二氯 - 苯甲酰基氨基）-1H-吡唑-3-羧酸（1-甲磺酰基 - 哌啶-4-基） - 酰胺的化合物，治疗其用途和含有结晶化合物的药物组合物。本发明还提供了含有4-（2,6-二氯 - 苯甲酰氨基）-1H-吡唑-3-羧酸（1-甲磺酰基 - 哌啶-4-基） - 酰胺的新型药物制剂及其制备方法。

5. 发明申请

WO2006077426A3 4- (2, 6-DICHLOROBENZOYLAMINO) -lH-PYRAZOLE-3 -CARBOXYLIC ACID PIPERIDIN- 4 -YLAMID ACID ADDITION SALTS AS KINASE INHIBITORS 审中-公开
标题翻译： 4-（2,6-二氯苯甲酰氨基）-1H-吡唑-3-羧酸哌啶-4-基氨基酸添加剂作为激酶抑制剂
公开(公告)号：WO2006077426A3
公开(公告)日：2006-09-28
申请号：PCT/GB2006000207
申请日：2006-01-20
申请人： ASTEX THERAPEUTICS LTD , WYATT PAUL GRAHAM , REES DAVID CHARLES , VINKOVIC MLADEN , TREWARTHA GARY
发明人： WYATT PAUL GRAHAM , REES DAVID CHARLES , VINKOVIC MLADEN , TREWARTHA GARY
IPC分类号： C07D401/12 , A61K31/4155 , A61K31/454 , A61P35/00 , A61P35/02
CPC分类号： C07D231/40 , C07D401/12
摘要： The invention provides an acid addition salt of 4-(2,6-dichloro-benzoylamino)-lH- pyrazole-3-carboxylic acid piperidin-4-ylamide and crystals thereof, the salt being formed with an acid selected from methanesulphonic acid and acetic acid and mixtures thereof. Also provided are the novel uses of salts of 4-(2,6-dichloro-benzoylamino)-lH- pyrazole-3-carboxylic acid piperidin-4-ylamide, processes for the preparation of 4- (2,6-dichloro-benzoylamino)-lH-pyrazole-3-carboxylic acid piperidin-4-ylamide and its salts and novel chemical intermediates.
摘要翻译：本发明提供4-（2,6-二氯 - 苯甲酰基氨基）-1H-吡唑-3-羧酸哌啶-4-基酰胺及其晶体的酸加成盐，该盐与选自甲磺酸和乙酸的酸形成酸及其混合物。还提供4-（2,6-二氯 - 苯甲酰基氨基）-1H-吡唑-3-羧酸哌啶-4-基酰胺的盐的新用途，制备4-（2,6-二氯 - 苯甲酰基氨基）-1H-吡唑-3-羧酸哌啶-4-基酰胺及其盐和新的化学中间体。

6. 发明申请

WO2006070195A8 PYRAZOLE COMPOUNDS THAT MODULATE THE ACTIVITY OF CDK, GSK AND AURORA KINASES 审中-公开
标题翻译：调节CDK，GSK和AURORA KINASES活性的吡咯化合物
公开(公告)号：WO2006070195A8
公开(公告)日：2006-08-24
申请号：PCT/GB2005005097
申请日：2005-12-30
申请人： ASTEX THERAPEUTICS LTD , BERDINI VALERIO , CARR MARIA GRAZIA , GILL ADRIAN LIAM , HOWARD STEVEN , NAVARRO EVA FIGUEROA , TREWARTHA GARY , REES DAVID CHARLES , VINKOVIC MLADEN , WYATT PAUL GRAHAM
发明人： BERDINI VALERIO , CARR MARIA GRAZIA , GILL ADRIAN LIAM , HOWARD STEVEN , NAVARRO EVA FIGUEROA , TREWARTHA GARY , REES DAVID CHARLES , VINKOVIC MLADEN , WYATT PAUL GRAHAM
IPC分类号： C07D403/04 , A61K31/4184 , A61P35/00 , C07D407/14 , C07D513/04
CPC分类号： C07D401/14 , C07D403/04 , C07D403/14 , C07D405/14 , C07D407/14 , C07D413/14 , C07D487/04 , C07D513/04
摘要： The invention provides a compound of the formula (I): or a salt, solvate, tautomer or N-oxide thereof, wherein M is selected from a group D1 and a group D2: and R', E, A and X are as defined in the claims. Also provided are pharmaceutical compositions containing the compounds, processes for making the compounds and the use of the compounds in the prophylaxis or treatment of a disease state mediated by a CDK kinase, GSK-3 kinase or Aurora kinase.
摘要翻译：本发明提供式（I）化合物或其盐，溶剂化物，互变异构体或N-氧化物，其中M选自D1和D2组：R'，E，A和X如上所定义在权利要求中。还提供了含有化合物的药物组合物，制备该化合物的方法以及该化合物在预防或治疗由CDK激酶，GSK-3激酶或极光激酶介导的疾病状态中的用途。

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