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1. 发明申请

WO2007087129A8 FLUORINATED ARYLAMIDE DERIVATIVES 审中-公开
标题翻译：氟化芳酰胺衍生物
公开(公告)号：WO2007087129A8
公开(公告)日：2010-05-14
申请号：PCT/US2007000182
申请日：2007-01-08
申请人： MERCK & CO INC , MILLER THOMAS A , SLOMAN DAVID L , STANTON MATTHEW G , WILSON KEVIN J , WITTER DAVID J
发明人： MILLER THOMAS A , SLOMAN DAVID L , STANTON MATTHEW G , WILSON KEVIN J , WITTER DAVID J
IPC分类号： A61K31/38
CPC分类号： C07D231/40 , C07D333/20 , C07D333/70 , C07D409/12 , C07D409/14 , C07D413/10 , C07D413/12 , C07D413/14
摘要： The present invention relates to a novel class of fluorinated arylamide derivatives. The instant compounds can be used to treat cancer. The fluorinated arylamide derivatives can also inhibit histone deacetylase and are suitable for use in selectively inducing terminal differentiation, and arresting cell growth and/or apoptosis of neoplastic cells, thereby inhibiting proliferation of such cells. Thus, the compounds of the present invention are useful in treating a patient having a tumor characterized by proliferation of neoplastic cells. The compounds of the invention may also be useful in the prevention and treatment of TRX-mediated diseases, such as autoimmune, allergic and inflammatory diseases, and in the prevention and/or treatment of diseases of the central nervous system (CNS), such as neurodegenerative diseases. The present invention further provides pharmaceutical compositions comprising the hydroxamic acid derivatives and safe dosing regimens of these pharmaceutical compositions, which are easy to follow, and which result in a therapeutically effective amount of the hydroxamic acid derivatives in vivo.
摘要翻译：本发明涉及一类新型氟化芳基酰胺衍生物。本化合物可用于治疗癌症。氟化芳基酰胺衍生物还可以抑制组蛋白脱乙酰酶，并且适用于选择性诱导终末分化，并阻止肿瘤细胞的细胞生长和/或凋亡，从而抑制这些细胞的增殖。因此，本发明的化合物可用于治疗具有以肿瘤细胞增殖为特征的肿瘤的患者。本发明的化合物还可用于预防和治疗TRX介导的疾病，例如自身免疫性，过敏性和炎性疾病，以及预防和/或治疗中枢神经系统（CNS）的疾病，例如神经退行性疾病本发明进一步提供包含异羟肟酸衍生物和这些药物组合物的安全投药方案的药物组合物，它们易于遵循，并且其在体内导致治疗有效量的异羟肟酸衍生物。

2. 发明申请

WO2010017046A1 PYRAZOLO[1,5-A]PYRIDINES AS MARK INHIBITORS 审中-公开
标题翻译： PYRAZOLO [1,5-A]吡啶类作为标记抑制剂
公开(公告)号：WO2010017046A1
公开(公告)日：2010-02-11
申请号：PCT/US2009/051785
申请日：2009-07-27
申请人： MERCK & CO., INC. , KATZ, Jason , KNOWLES, Sandra, L. , JEWELL, James, P. , SLOMAN, David, L. , STANTON, Matthew, G. , NOUCTI, Njamkou
发明人： KATZ, Jason , KNOWLES, Sandra, L. , JEWELL, James, P. , SLOMAN, David, L. , STANTON, Matthew, G. , NOUCTI, Njamkou
IPC分类号： A01N43/78 , A61K31/425
CPC分类号： A61K31/425 , C07D417/04 , C07D417/14
摘要： The invention encompasses pyrazolo[1,5-a]pyridine derivatives which selectively inhibit microtubule affinity regulating kinase (MARK) and are therefore useful for the treatment or prevention of Alzheimer's disease. Pharmaceutical compositions and methods of use are also included.
摘要翻译：本发明包括选择性抑制微管亲和调节激酶（MARK）的吡唑并[1,5-a]吡啶衍生物，因此可用于治疗或预防阿尔茨海默氏病。还包括药物组合物和使用方法。

3. 发明申请

WO2010005841A1 INHIBITORS OF JANUS KINASES 审中-公开
标题翻译： JANUS KINASES的抑制剂
公开(公告)号：WO2010005841A1
公开(公告)日：2010-01-14
申请号：PCT/US2009/049357
申请日：2009-07-01
申请人： MERCK & CO., INC. , WILSON, Kevin , DE ALMEIDA, Gabriela , HAIDLE, Andrew , KONRAD, Kaleen , MACHACEK, Michelle , ZABIEREK, Anna
发明人： WILSON, Kevin , DE ALMEIDA, Gabriela , HAIDLE, Andrew , KONRAD, Kaleen , MACHACEK, Michelle , ZABIEREK, Anna
IPC分类号： C07D413/00
CPC分类号： C07D333/38 , C07D409/04 , C07D409/12 , C07D413/12
摘要： The instant invention provides for compounds that inhibit the four known mammalian JAK kinases (JAK1, JAK2, JAK3 and TYK2). The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting the activity of JAK1, JAK2, JAK3 and TYK2 by administering the compound to a patient in need of treatment for myeloproliferative disorders or cancer.
摘要翻译：本发明提供了抑制四种已知的哺乳动物JAK激酶（JAK1，JAK2，JAK3和TYK2）的化合物。本发明还提供了包含此类抑制性化合物的组合物和通过将该化合物给予需要治疗骨髓增生性疾病或癌症的患者来抑制JAK1，JAK2，JAK3和TYK2活性的方法。

4. 发明申请

WO2009155024A1 NOVEL SUBSTITUTED INDOLES 审中-公开
标题翻译：新的替代品
公开(公告)号：WO2009155024A1
公开(公告)日：2009-12-23
申请号：PCT/US2009/045403
申请日：2009-05-28
申请人： MERCK & CO., INC. , BARROW, James, C. , HARRISON, Scott , MULHEARN, James , WOLKENBERG, Scott
发明人： BARROW, James, C. , HARRISON, Scott , MULHEARN, James , WOLKENBERG, Scott
IPC分类号： A01N43/56 , A61K31/405
CPC分类号： C07D471/04 , C07D401/04 , C07D401/14
摘要： The present invention relates to novel amyloid binding compounds and methods for measuring effects of the compounds, by measuring changes of amyloid plaque level in living patients. More specifically, the present invention relates to a method of using the compounds of this invention as tracers in positron emission tomography (PET) imaging to study amyloid deposits in brain in vivo to allow diagnosis of Alzheimer's disease. Thus, the present invention relates to use of the novel amyloid binding compounds as a diagnostic. The invention further relates to a method of measuring clinical efficacy of Alzheimer's disease therapeutic agents. Specifically, the present invention relates to novel aryl or heteroaryl substituted indole derivatives, compositions, and therapeutic uses and processes for making such compounds.
摘要翻译：本发明涉及通过测量活体患者淀粉样斑块水平的变化来测量化合物的效果的新型淀粉样蛋白结合化合物和方法。更具体地说，本发明涉及在正电子发射断层摄影（PET）成像中使用本发明化合物作为示踪剂的方法，以在体内研究脑中的淀粉样蛋白沉积物以允许诊断阿尔茨海默氏病。因此，本发明涉及新型淀粉样蛋白结合化合物作为诊断用途。本发明还涉及测量阿尔茨海默病治疗剂的临床疗效的方法。具体地，本发明涉及新的芳基或杂芳基取代的吲哚衍生物，组合物，以及用于制备这些化合物的治疗用途和方法。

5. 发明申请

WO2009152027A1 5,7-DIHYDRO-6H-PYRROLO[2,3-D]PYRIMIDIN-6-ONE DERIVATIVES FOR MARK INHIBITION 审中-公开
标题翻译： 5,7-二氢-6H-吡咯并[2,3-D]嘧啶-6-酮衍生物用于标记抑制
公开(公告)号：WO2009152027A1
公开(公告)日：2009-12-17
申请号：PCT/US2009/046251
申请日：2009-06-04
申请人： MERCK & CO., INC. , HAIDLE, Andrew , STANTON, Matthew , ALTMAN, Michael , KONRAD, Kaleen , ZABIEREK, Anna , KATZ, Jason , JEWELL, James
发明人： HAIDLE, Andrew , STANTON, Matthew , ALTMAN, Michael , KONRAD, Kaleen , ZABIEREK, Anna , KATZ, Jason , JEWELL, James
IPC分类号： A01N43/50 , A61K31/415
CPC分类号： C07D487/04
摘要： Compounds of formula I: are potent and selective inhibitors of microtubule affinity regulating kinase (MARK), and hence find use in treatment of Alzheimer's disease and other conditions associated with hyperphosphorylation of tau.
摘要翻译：式I的化合物是微管亲和调节激酶（MARK）的有效和选择性抑制剂，因此可用于治疗阿尔茨海默病和与tau的过度磷酸化相关的其它病症。

6. 发明申请

WO2009140163A1 OXAZOLOBENZIMIDAZOLE DERIVATIVES 审中-公开
标题翻译： OXAZOLOBENZIMIDAZOLE衍生物
公开(公告)号：WO2009140163A1
公开(公告)日：2009-11-19
申请号：PCT/US2009/043299
申请日：2009-05-08
申请人： MERCK & CO., INC. , BRNARDIC, Edward, J. , CONVERSO, Antonella , FRALEY, Mark, E. , GARBACCIO, Robert, M. , HUANG, Shaei, Y.
发明人： BRNARDIC, Edward, J. , CONVERSO, Antonella , FRALEY, Mark, E. , GARBACCIO, Robert, M. , HUANG, Shaei, Y.
IPC分类号： A01N43/50 , A01N43/76 , A61K31/42
CPC分类号： C07D498/04
摘要： The present invention is directed to oxazolobenzimidazole derivatives which are potentiators of metabotropic glutamate receptors, particularly the mGluR2 receptor, and which are useful in the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which metabotropic glutamate receptors are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which metabotropic glutamate receptors are involved.
摘要翻译：本发明涉及作为代谢型谷氨酸受体，特别是mGluR2受体的增强剂的恶唑烷并咪唑衍生物，它们可用于治疗或预防与谷氨酸能力障碍相关的神经和精神障碍以及涉及代谢型谷氨酸受体的疾病。本发明还涉及包含这些化合物的药物组合物以及这些化合物和组合物在预防或治疗涉及代谢型谷氨酸受体的疾病中的用途。

7. 发明申请

WO2009140125A2 DEPROTECTION OF SYNTHETIC OLIGONUCLEOTIDES USING AQUEOUS ETHANOLAMINE 审中-公开
标题翻译：使用水性乙酰胺对合成寡核苷酸的保护
公开(公告)号：WO2009140125A2
公开(公告)日：2009-11-19
申请号：PCT/US2009/043064
申请日：2009-05-07
申请人： MERCK & CO., INC. , GOSSELIN, Francis , GOWANI, Amran
发明人： GOSSELIN, Francis , GOWANI, Amran
IPC分类号： C07H21/04
CPC分类号： C07H1/00 , C07H21/00 , Y02P20/55
摘要： This invention concerns an efficient and safer (easy to handle and environmentally less hazardous) protocol for cleavage and deprotection of synthetic oligonucleotides utilizing ethanolamine. Specifically, the present invention features a method for 1) the removal of amide protecting groups from nucleobases and 2) cleavage of the synthetic oligonucleotides from their solid support allowing the isolation and subsequent purification of said oligonucleotides.
摘要翻译：本发明涉及使用乙醇胺的合成寡核苷酸的切割和脱保护的有效和安全（易于处理和环境更少的危害）方案。具体地，本发明的特征在于一种方法，用于1）从核碱基中除去酰胺保护基团，和2）将合成寡核苷酸从其固体支持物切割出来，从而分离和随后纯化所述寡核苷酸。

8. 发明申请

WO2009134668A2 4-OXO-1,4-DIHYDROQUINOLINE M1 RECEPTOR POSITIVE ALLOSTERIC MODULATORS 审中-公开
标题翻译： 4-OXO-1,4-DIHYDROQUINOLINE M1受体阳性免疫调节剂
公开(公告)号：WO2009134668A2
公开(公告)日：2009-11-05
申请号：PCT/US2009/041493
申请日：2009-04-23
申请人： MERCK & CO., INC. , KUDUK, Scott, D. , DI MARCO, Christina, Ng , SHIPE, William, D.
发明人： KUDUK, Scott, D. , DI MARCO, Christina, Ng , SHIPE, William, D.
IPC分类号： C07D401/02
CPC分类号： C07D401/14 , C07D401/06 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14
摘要： The present invention is directed to compounds of formula (I) which are M1 receptor positive allosteric modulators and that are useful in the treatment of diseases in which the M1 receptor is involved, such as Alzheimer's disease, schizophrenia, pain or sleep disorders. The invention is also directed to pharmaceutical compositions comprising the compounds, and to the use of the compounds and compositions in the treatment of diseases mediated by the M1 receptor.
摘要翻译：本发明涉及作为M1受体阳性变构调节剂的式（I）化合物，其可用于治疗涉及M1受体的疾病，例如阿尔茨海默氏病，精神分裂症，疼痛或睡眠障碍。本发明还涉及包含该化合物的药物组合物，以及该化合物和组合物在治疗由M1受体介导的疾病中的用途。

9. 发明申请

WO2008115415A8 POLYPEPTIDES FOR INDUCING A PROTECTIVE IMMUNE RESPONSE AGAINST STAPHYLOCOCCUS EPIDERMIDIS 审中-公开
标题翻译：用于诱导针对斑马鱼肺炎的保护性免疫应答的多肽
公开(公告)号：WO2008115415A8
公开(公告)日：2009-11-05
申请号：PCT/US2008003389
申请日：2008-03-14
申请人： MERCK & CO INC , ANDERSON ANNALIESA S , MCNEELY TESSIE , COOK JAMES C III , MCCLEMENTS WILLIAM L , MONTGOMERY DONNA L
发明人： ANDERSON ANNALIESA S , MCNEELY TESSIE , COOK JAMES C III , MCCLEMENTS WILLIAM L , MONTGOMERY DONNA L
IPC分类号： C12N15/00 , C07H21/04 , C07K1/00 , C12N1/20 , C12Q1/68
CPC分类号： A61K39/085
摘要： The present invention features polypeptides comprising an amino acid sequence structurally related to SEQ ID NO: 1 and uses of such polypeptides. SEQ ID NO: 1 is a truncated derivative of a full-length S. epidermidis polypeptide. The full-length naturally occurring polypeptide is referred to herein as full-length ORF2695e. A His-tagged derivative of SEQ ID NO: 1 was found to produce a protective immune response against S. epidermidis.
摘要翻译：本发明的特征在于包含与SEQ ID NO：1结构相关的氨基酸序列的多肽和这种多肽的用途。 SEQ ID NO：1是全长表皮葡萄球菌多肽的截短的衍生物。全长天然存在的多肽在本文中称为全长ORF2695e。发现SEQ ID NO：1的His标签衍生物对表皮葡萄球菌产生保护性免疫应答。

10. 发明申请

WO2009131930A1 NANOPARTICLE FORMATION VIA RAPID PRECIPITATION 审中-公开
标题翻译：通过快速降解的纳米颗粒形成
公开(公告)号：WO2009131930A1
公开(公告)日：2009-10-29
申请号：PCT/US2009/041083
申请日：2009-04-20
申请人： MERCK & CO., INC. , TUNG, Hsien-hsin , WANG, Lei , PANMAI, Santipharp , RIEBE, Michael
发明人： TUNG, Hsien-hsin , WANG, Lei , PANMAI, Santipharp , RIEBE, Michael
IPC分类号： A61K9/14
CPC分类号： A61K9/5161 , A61K9/14 , A61K9/1688 , A61K9/1694 , A61K9/5192 , B01D9/0054 , B01F5/0256 , B01F5/10 , B01F11/0258 , B01F13/1027
摘要： The invention encompasses a method for making nano-sized particles of water-insoluble pharmaceuticals comprising: (1) dissolving the water-insoluble pharmaceutical in a water-miscible solvent, optionally with water and inactive pharmaceutical ingredients, to make a solution; (2) rapidly mixing the solution with an anti-solvent which creates a high level of supersaturation, wherein the anti-solvent is water with optional inactive pharmaceutical ingredients; (3) simultaneously applying energy to the resulting mixture during the mixing of solution and anti-solvent as nano-sized drug particles precipitate out and form a slurry mixture under supersaturation; and (4) optionally isolating the nano-sized particles of water-insoluble pharmaceuticals from the slurry mixture.
摘要翻译：本发明包括制备水不溶性药物的纳米尺寸颗粒的方法，包括：（1）将水不溶性药物溶解在水混溶性溶剂中，任选地用水和非活性药物成分溶解; （2）将溶液与抗溶剂快速混合，产生高水平的过饱和度，其中抗溶剂是具有任选的非活性药物成分的水; （3）在溶液和反溶剂的混合过程中同时向所得混合物施加能量作为纳米尺寸药物颗粒沉淀并在过饱和下形成浆料混合物; 和（4）任选地从浆料混合物中分离纳米尺寸的水不溶性药物颗粒。

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