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31. 发明申请

WO2006107273A1 COMPOUNDS HAVING PROGESTOGENIC ACTIVITY AND THEIR USE 审中-公开
标题翻译：具有原发性活性的化合物及其使用
公开(公告)号：WO2006107273A1
公开(公告)日：2006-10-12
申请号：PCT/SG2005/000116
申请日：2005-04-06
申请人： NATIONAL UNIVERSITY OF SINGAPORE , YONG, Eu Leong , LIM, Lis Sa Elissa , SHEN, Ping , GONG, YinHan
发明人： YONG, Eu Leong , LIM, Lis Sa Elissa , SHEN, Ping , GONG, YinHan
IPC分类号： A61K31/343 , A61P5/30 , A61K31/381 , A61K31/407 , A61K36/00 , C07D495/02 , C07D487/02 , C07D491/02 , C07D493/22 , C07D497/02 , C07D498/02 , C07D513/02
CPC分类号： A61K36/236 , A61K31/343 , A61K31/381 , A61K31/407 , C07D493/04 , C07D493/10
摘要： The invention relates to compounds having progestogenic activity and to their use. The invention discloses a compound having the general formula (I) wherein Y, Y', X and X' are independently selected from the group consisting of O, S and N; R 1 is selected from the group consisting of optionally substituted C 1-8 alkyl, optionally substituted C 2-6 alkenyl, optionally substituted C 2-6 alkynyl, optionally substituted C 1-6 alkoxy, optionally substituted C1-6 thioalkyl, optionally substituted C4-10 aryl, optionally substituted C 6-11 alkylaryl, optionally substituted C 1-6 alkylamino, optionally substituted C 1-6 alkylcarbonyl, optionally substituted C 1-6 alkylsulfonamino, optionally substituted (C 1 -C 6 )alkylsulfinyl, optionally substituted C 1-6 alkylcarbonylamino, optionally substituted hetero(C 5 -C 10 )aryl, hydroxyl, halogen, cyano, nitro, amino, formyl, and thiol; R 2 , R 3 , R 4 , R 5 , R 6 and R 7 are independently selected from the group consisting of hydrogen, optionally substituted C 1-8 alkyl, optionally substituted C 2-6 alkenyl, optionally substituted C 2-6 alkynyl, optionally substituted C 1-6 alkoxy, optionally substituted C 1-6 thioalkyl, optionally substituted C 5-10 aryl, optionally substituted C 6-11 alkylaryl, optionally substituted C 1-6 alkylamino, optionally substituted C 1-6 alkylcarbonyl, optionally substituted C 1-6 alkylsulfonamino, optionally substituted (C 1 -C 6 )alkylsulfinyl, optionally substituted C 1-6 alkylcarbonylamino, optionally substituted hetero(C 5 -C 10 )aryl, hydroxyl, halogen, cyano, nitro, amino, formyl, and thiol; ---- indicates an optional double bond.
摘要翻译：本发明涉及具有孕激素活性及其应用的化合物。本发明公开了具有通式（I）的化合物，其中Y，Y'，X和X'独立地选自O，S和N; R 1选自任选取代的C 1-8 - 烷基，任选取代的C 2-6 - 烯基，任选取代的C 1 -C 6 - 任选取代的C 1-6烷氧基，任选取代的C 1-6硫烷基，任选取代的C 4-10芳基，任选取代的C 6-11 - 烷基芳基，任选取代的C 1-6烷基氨基，任选取代的C 1-6烷基羰基，任选取代的C 1-6烷基亚磺酰氨基，任选取代的（C 1 -C 6 -C 6）烷基亚磺酰基，任选取代的C 1-6烷基羰基氨基，任选取代的杂（C 5 -C 6 - 芳基，羟基，卤素，氰基，硝基，氨基，甲酰基和硫醇; R 2，R 3，R 4，R 5，R 6和R 5， R 7独立地选自氢，任选取代的C 1-8 - 烷基，任选取代的C 2-6 - 烯基，任选地取代的C 2-6 - 炔基，任选取代的C 1-6烷氧基，任选取代的C 1-6烷硫基，任选取代的C 1 -C 6 - 任选取代的C 6-11烷基芳基，任选取代的C 1-6烷基氨基，任选取代的C 1-6 - 任选取代的C 1 -C 6烷基亚磺酰基，任选取代的C 1 -C 6烷基亚磺酰基，任选取代的C 1 -C 6烷基亚磺酰基， 1-6烷基羰基氨基，任选取代的杂原子（C 5 -C 10）芳基，羟基，卤素，氰基，硝基，氨基，甲酰基和硫醇; ----表示可选双键。

33. 发明申请

WO2006076131A2 CHEMICAL COMPOUNDS 审中-公开
标题翻译：化学化合物
公开(公告)号：WO2006076131A2
公开(公告)日：2006-07-20
申请号：PCT/US2005/045994
申请日：2005-12-16
申请人： SMITHKLINE BEECHAM CORPORATION , GUDMUNDSSON, Kristjan
发明人： GUDMUNDSSON, Kristjan
IPC分类号： A61K31/4741 , C07D491/02
CPC分类号： C07D519/00 , C07D471/04 , C07D491/04
摘要： There is provided novel compounds that demonstrate protective effects on target cells from HIV infection in a manner as to bind specifically to the chemokine receptor, and which affect the binding of the natural ligand or chemokine to a receptor such as CXCR4 and/or CCR5 of a target cell.
摘要翻译：提供了新的化合物，其以特异性结合趋化因子受体的方式证明了对来自HIV感染的靶细胞的保护作用，并且其影响天然配体或趋化因子与受体的结合，例如作为靶细胞的CXCR4和/或CCR5。

34. 发明申请

WO2005051301A3 HETEROCYCLIC INHIBITORS OF MEK AND METHODS OF USE THEREOF 审中-公开
标题翻译： MEK的杂环抑制剂及其使用方法
公开(公告)号：WO2005051301A3
公开(公告)日：2006-05-18
申请号：PCT/US2004039060
申请日：2004-11-18
申请人： ARRAY BIOPHARMA INC , MARLOW ALLISON L , WALLACE ELI , SEO JEONGBEOB , LYSSIKATOS JOSEPH P , YANG HONG WOON , BLAKE JIM
发明人： MARLOW ALLISON L , WALLACE ELI , SEO JEONGBEOB , LYSSIKATOS JOSEPH P , YANG HONG WOON , BLAKE JIM
IPC分类号： A61K31/44 , A01N33/02 , A01N43/42 , A01N43/54 , A01N43/58 , A01N43/60 , A01N43/64 , A01N43/90 , A61K20060101 , A61K31/40 , A61K31/415 , A61K31/416 , A61K31/4439 , A61K31/4745 , A61K31/495 , A61K31/50 , A61K31/501 , A61K31/502 , A61K31/517 , A61K31/519 , A61K31/53 , A61K31/655 , C07D20060101 , C07D209/44 , C07D209/46 , C07D213/80 , C07D213/82 , C07D215/48 , C07D221/04 , C07D231/02 , C07D231/56 , C07D237/02 , C07D237/24 , C07D237/26 , C07D237/28 , C07D237/32 , C07D239/74 , C07D401/00 , C07D401/04 , C07D401/06 , C07D403/02 , C07D413/00 , C07D413/02 , C07D413/04 , C07D413/14 , C07D417/00 , C07D417/02 , C07D417/04 , C07D471/02 , C07D471/04 , C07D487/02 , C07D491/02 , C07D498/02
CPC分类号： C07D209/46 , C07D213/80 , C07D213/82 , C07D215/48 , C07D231/56 , C07D237/24 , C07D237/28 , C07D237/32 , C07D239/74 , C07D401/04 , C07D401/06 , C07D413/04 , C07D413/14 , C07D417/04 , C07D471/04
摘要： Disclosed are compounds of the Formula (I) and pharmaceutically acceptable salts and prodrugs thereof, wherein R 1 , R 2 , R 7 , R 8 and R 9 , W, X and Y are as defined in the specification. Such compounds are MEK inhibitors and useful in the treatment of hyperproliferative diseases, such as cancer and inflammation, in mammals, and inflammatory conditions. Also disclosed are methods of using such compounds in the treatment of hyperproliferative diseases in mammals and pharmaceutical compositions containing such compounds.
摘要翻译：公开了式（I）的化合物及其药学上可接受的盐和前药，其中R 1，R 2，R 7，R 7， SUP> 8和R 9，W，X和Y如说明书中所定义。这些化合物是MEK抑制剂，可用于治疗哺乳动物和炎性病症中的过度增殖性疾病，例如癌症和炎症。还公开了使用这些化合物治疗哺乳动物中过度增殖性疾病的方法和含有这些化合物的药物组合物。

35. 发明申请

WO2006028961A2 TRICYCLIC HETEROARYL PIPERAZINES, PYRROLIDINES AND AZETIDINES AS SEROTONIN RECEPTOR MODULATORS 审中-公开
标题翻译：三环戊二烯受体调节剂三环戊二烯哌嗪，吡咯烷和炔丙菊酯
公开(公告)号：WO2006028961A2
公开(公告)日：2006-03-16
申请号：PCT/US2005/031306
申请日：2005-09-01
申请人： ATHERSYS, INC. , BENNANI, Youssef, L. , BOM, David, C. , ROBARGE, Michael, J.
发明人： BENNANI, Youssef, L. , BOM, David, C. , ROBARGE, Michael, J.
IPC分类号： A61K31/407 , C07D491/02
CPC分类号： C07D491/04 , C07D495/04
摘要： The present invention generally relates to a series of compounds, to pharmaceutical compositions containing the compounds, and to use the compounds and compositions as therapeutic agents. More specifically, compounds of the present invention are hexahydroazepinoindole and octahydroazepinoindole compounds. These compounds are serotonin receptor (5-HT) ligands and are useful for treating diseases, disorders, and conditions wherein modulation of the activity of serotonin receptors (5-HT) is desired (e.g. anxiety, depression and obesity).
摘要翻译：本发明一般涉及一系列化合物，含有该化合物的药物组合物，以及使用该化合物和组合物作为治疗剂。更具体地说，本发明的化合物是六氢氮杂吲哚和八氢氮杂并吲哚化合物。这些化合物是血清素受体（5-HT）配体，可用于治疗其中需要调节血清素受体（5-HT）活性（例如焦虑，抑郁和肥胖）的疾病，病症和病症。

36. 发明申请

WO2005067900A3 AZABENZOFURAN SUBSTITUTED THIOUREAS AS INHIBITORS OF VIRAL REPLICATION 审中-公开
标题翻译：作为病毒复制的抑制剂的AZABENZOFURAN替代THI
公开(公告)号：WO2005067900A3
公开(公告)日：2005-09-29
申请号：PCT/US2005000339
申请日：2005-01-05
申请人： ACHILLION PHARMACEUTICALS INC , THURKAUF ANDREW , CHEN DAWEI , PHADKE AVINASH , LI SHOUMING , DESHPANDE MILIND
发明人： THURKAUF ANDREW , CHEN DAWEI , PHADKE AVINASH , LI SHOUMING , DESHPANDE MILIND
IPC分类号： A61K31/00 , A61K31/4355 , A61K31/4741 , A61K38/21 , C07D471/04 , C07D491/02 , C07D491/04 , A61P31/14
CPC分类号： A61K31/00 , A61K31/4355 , C07D491/04
摘要： The present invention provides compounds of Formula: (1), wherein the variables Ar, A1, A2, A3, A4, R5, R6, R7, V, W, X, and Y are defined herein. Certain compounds of Formula (1) described herein possess potent antiviral activity. The invention also provides compounds of Formula (1) that are potent and/ or selective inhibitors of Hepatitis C virus replication. The invention also provides pharmaceutical compositions containing one or more compounds of Formula (1), or a salt, solvate, or acylated prodrug of such compounds, and one or more pharmaceutically acceptable carriers, excipients, or diluents. The invention further comprises methods of treating patients suffering from certain infectious diseases by administering to such patients an amount of a compound of Formula (1) effective to reduce signs or symptoms of the disease. These infectious diseases include viral infections, particularly HCV infections. The invention is particularly includes methods of treating human patients suffering from an infectious disease, but also encompasses methods of treating other animals, including livestock and domesticated companion animals, suffering from an infectious disease. Methods of treatment include administering a compound of Formula (1) as a single active agent or administering a compound of Formula (1) in combination with on or more other therapeutic agent.
摘要翻译：本发明提供式（1）的化合物，其中变量Ar，A1，A2，A3，A4，R5，R6，R7，V，W，X和Y在本文中定义。某些本文所述的式（1）化合物具有有效的抗病毒活性。本发明还提供了作为丙型肝炎病毒复制的有效和/或选择性抑制剂的式（1）化合物。本发明还提供了含有一种或多种式（1）化合物或这些化合物的盐，溶剂化物或酰化前药以及一种或多种药学上可接受的载体，赋形剂或稀释剂的药物组合物。本发明还包括通过向这些患者施用一定量的有效减少疾病体征或症状的式（1）化合物来治疗患有某些感染性疾病的患者的方法。这些传染病包括病毒感染，特别是HCV感染。本发明特别包括治疗患有感染性疾病的人类患者的方法，还包括治疗其它动物（包括患有传染病的家畜和驯养的伴侣动物）的方法。治疗方法包括施用作为单一活性剂的式（1）化合物或将式（1）的化合物与一种或多种其它治疗剂组合施用。

37. 发明申请

WO2005025507A3 DIHYDROPYRIDINE COMPOUNDS FOR TREATING OR PREVENTING METABOLIC DISORDERS 审中-公开
标题翻译：用于治疗或预防代谢障碍的二氢吡啶化合物
公开(公告)号：WO2005025507A3
公开(公告)日：2005-09-29
申请号：PCT/US2004029636
申请日：2004-09-10
申请人： SYNTA PHAMACEUTICALS CORP , ONO MITSUNORI , WADA YUMIKO , SUN LIJUN , CHEN SHOUJUN , PRZEWLOKA TERESA , ZHANG SHIJIE , BORELLA CHRISTOPHER , KOYA KEIZO , FOLEY KEVIN , XIA ZHI-QIANG , LI HAO , ZHOU DAN
发明人： ONO MITSUNORI , WADA YUMIKO , SUN LIJUN , CHEN SHOUJUN , PRZEWLOKA TERESA , ZHANG SHIJIE , BORELLA CHRISTOPHER , KOYA KEIZO , FOLEY KEVIN , XIA ZHI-QIANG , LI HAO , ZHOU DAN
IPC分类号： A61K31/47 , A61K31/4741 , A61K31/4743 , A61K31/4745 , C07D215/54 , C07D221/20 , C07D401/04 , C07D401/12 , C07D401/14 , C07D405/04 , C07D471/02 , C07D491/02 , C07D491/04 , C07D498/02 , A61K31/4709 , C07D215/20
CPC分类号： C04B35/632 , C07D215/54 , C07D221/20 , C07D401/04 , C07D401/12 , C07D401/14 , C07D405/04 , C07D491/04
摘要： This invention relates to dihydropyridine compounds of formula: (I) or a pharmaceutically acceptable salt, solvate, clathrate, or prodrug thereof wherein A2, R12, R13, R14, R15, R16, R17, R18, R19, R20, R21, R22, and m are defined herein, and compositions comprising such compounds. The invention also relates to methods of preventing or treating metabolic disorders, such as diabetes mellitus, and conditions and complications associated with diabetes mellitus, comprising administering to a subject in need thereof a compound of formula (I) or a composition comprising such a compound. The invention further relates to kits comprising a compound of formula (I).
摘要翻译：本发明涉及式（I）的二氢吡啶化合物或其药学上可接受的盐，溶剂合物，包合物或前药，其中A2，R12，R13，R14，R15，R16，R17，R18，R19，R20，R21，和m在本文中定义，组合物包含这些化合物。本发明还涉及预防或治疗诸如糖尿病的代谢疾病以及与糖尿病有关的病症和并发症的方法，其包括向有需要的受试者施用式（I）化合物或包含这种化合物的组合物。本发明还涉及包含式（I）化合物的试剂盒。

38. 发明申请

WO2005051302A2 BICYCLIC INHIBITORS OF MEK AND METHODS OF USE THEREOF 审中-公开
标题翻译：双酚A抑制剂及其使用方法
公开(公告)号：WO2005051302A2
公开(公告)日：2005-06-09
申请号：PCT/US2004039061
申请日：2004-11-18
申请人： ARRAY BIOPHARMA INC , WALLACE ELI , YANG HONG WOON , BLAKE JIM
发明人： WALLACE ELI , YANG HONG WOON , BLAKE JIM
IPC分类号： A01N33/02 , A01N43/42 , A01N43/54 , A01N43/58 , A01N43/60 , A01N43/64 , A01N43/90 , A61K20060101 , A61K31/40 , A61K31/415 , A61K31/416 , A61K31/44 , A61K31/4439 , A61K31/4745 , A61K31/495 , A61K31/50 , A61K31/501 , A61K31/502 , A61K31/517 , A61K31/519 , A61K31/53 , A61K31/655 , C07D20060101 , C07D209/44 , C07D209/46 , C07D213/80 , C07D213/82 , C07D215/48 , C07D221/04 , C07D231/56 , C07D237/24 , C07D237/26 , C07D237/28 , C07D237/32 , C07D239/74 , C07D401/04 , C07D401/06 , C07D403/02 , C07D413/02 , C07D413/04 , C07D413/14 , C07D417/02 , C07D417/04 , C07D471/02 , C07D471/04 , C07D487/02 , C07D491/02 , C07D498/02 , A61K
CPC分类号： C07D209/46 , C07D213/80 , C07D213/82 , C07D215/48 , C07D231/56 , C07D237/24 , C07D237/28 , C07D237/32 , C07D239/74 , C07D401/04 , C07D401/06 , C07D413/04 , C07D413/14 , C07D417/04 , C07D471/04
摘要： Disclosed are compounds of the Formula (I) and pharmaceutically acceptable salts and prodrugs thereof, wherein R , R , R , R and R , W, X, and Z are as defined in the specification. Such compounds are MEK inhibitors and useful in the treatment of hyperproliferative diseases, such as cancer and inflammation, in mammals, and inflammatory conditions. Also disclosed are methods of using such compounds in the treatment of hyperproliferative diseases in mammals and pharmaceutical compositions containing such compounds.
摘要翻译：公开了式（I）化合物及其药学上可接受的盐和前药，其中R 1，R 2，R 8，R 9和R 10，W，X和Z是如说明书中所定义。这些化合物是MEK抑制剂，可用于治疗哺乳动物和炎性病症中的过度增殖性疾病，例如癌症和炎症。还公开了使用这些化合物治疗哺乳动物中过度增殖性疾病的方法和含有这些化合物的药物组合物。

39. 发明申请

WO2005007084A2 PANCRATISTATIN CYCLIC PHOSPHATE PRODRUGS AN PHENPANSTATIN CYCLIC PHOSPHATE PRODRUGS 审中-公开
标题翻译： PANRATTISTATTIN CYCLIC PHOSPHATE PRODRUGS PHENPANSTATTIN CYCLIC PHOSPHATE PRODRUGS
公开(公告)号：WO2005007084A2
公开(公告)日：2005-01-27
申请号：PCT/US2004019725
申请日：2004-06-18
申请人： UNIV ARIZONA , PETTIT GEORGE R , MELODY NOELEEN
发明人： PETTIT GEORGE R , MELODY NOELEEN
IPC分类号： A61K20060101 , A61K31/473 , A61K31/4741 , C07D491/02 , C07D491/12 , C07F9/6561 , C07F9/6574 , A61K
CPC分类号： A61K31/675 , C07F9/6561 , C07F9/65744
摘要： Selective phosphorylation of phenpanstatin (3a) with tetrabutylammonium dihydrogen phosphate and dicyclohexylcarbodiimide in pyridine followed by cation exchange chromatographic procedures was found to provide an efficient route to a new series (3b-3d) of promising 3,4-O-cyclic phosphate prodrugs designated phenpanstatin phosphates. Application of analogous reaction conditions to pancratistatin (1a) led to a mixture of monophosphate derivatives where sodium paancratistatin 4-O-phosphate (4a) was isolated and the structure confirmed by x-ray craxtallography. Modification of the reaction conditions allowed direct phosphorylation of pancratistatin followed by cation exchange chromatography to afford sodium pancratistatin 3,4-O-cyclic phosphate (5b) which was selected for preclinical development.
摘要翻译：发现用吡啶中的四丁基磷酸二氢铵和二环己基碳化二亚胺，然后用阳离子交换色谱法选择性磷酸化phenpanstatin（3a），提供了一种有效的路线，以提供一种有效途径到新的系列（3b-3d）有希望的3,4-O-环磷酸酯前药，磷酸盐。类似反应条件应用于pancratistatin（1a）产生单磷酸酯衍生物的混合物，其中分离出paancratistatin 4-O-磷酸钠（4a）并且通过X射线裂纹成像确认结构。反应条件的改变允许pancratistatin的直接磷酸化，接着进行阳离子交换层析，以提供选择用于临床前开发的钠pancratistatin 3,4-O-环磷酸酯（5b）。

40. 发明申请

WO01074821A1 NOVEL PROCESS FOR PRODUCING FUSED IMIDAZOPYRIDINE DERIVATIVE AND NOVEL CRYSTAL FORM 审中-公开
标题翻译：用于生产熔融咪唑并吡啶衍生物和新型晶体形式的新工艺
公开(公告)号：WO01074821A1
公开(公告)日：2001-10-11
申请号：PCT/JP2001/002620
申请日：2001-03-29
IPC分类号： C07D487/04 , C07D491/02 , C07D491/14 , C07D491/147
CPC分类号： C07D487/04 , C07D491/14
摘要： A process for producing a compound represented by the formula (I) (wherein R is an aromatic heterocycle, etc. and A is a heteroalicyclic group, etc.), characterized by reacting a compound represented by the formula (II) (wherein Hal is halogeno, and R and A have the same meanings as the above) in the presence of a sulfinic acid salt and a salt of an acid or organic base; and a novel crystal of 2-(3-isooxazolyl)-3,6,7,9-tetrahydroimidazo[4,5-d]pyrano[4,3-b]pyridine phosphate monohydrate.
摘要翻译：一种制备由式（I）表示的化合物（其中R是芳族杂环等，A是杂脂基基团等）的化合物的方法，其特征在于使由式（II）表示的化合物（其中Hal为卤素，R和A具有与上述相同的含义）在亚磺酸盐和酸或有机碱的盐的存在下反应; 和2-（3-异恶唑基）-3,6,7,9-四氢咪唑并[4,5-d]吡喃并[4,3-b]吡啶一水合物的新晶体。

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