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31. 发明申请

WO2013134081A3 HALOGENATED COMPOUNDS FOR PHOTODYNAMIC THERAPY 审中-公开
标题翻译：用于光合作用治疗的化合物
公开(公告)号：WO2013134081A3
公开(公告)日：2013-10-24
申请号：PCT/US2013028776
申请日：2013-03-02
申请人： NANOQUANTUM SCIENCES INC
发明人： JONES GARY W , TATARETS ANATOLIY L , PATSENKER LEONID D
IPC分类号： C07D209/30 , A61K31/404 , A61K31/428 , A61P31/00 , A61P33/00 , A61P35/00 , A61P43/00 , C07D209/10 , C07D277/68 , C07D293/10 , C07D403/06 , C07D417/06 , C08G61/12 , C08G67/00 , C09B23/02
CPC分类号： A61K41/0057 , A61K31/403 , A61K31/404 , A61K31/438 , A61K41/0071 , A61N1/30 , A61N5/062 , A61N5/10 , A61N2005/0659 , A61N2005/0663 , C07D209/04 , C07D209/08 , C07D209/10 , C07D209/18 , C07D209/24 , C07D209/58 , C07D209/60 , C07D277/62 , C07D277/64 , C07D293/12 , C07D401/02 , C07D403/06 , C07D403/14 , C07D417/06 , C07D471/10 , C07D487/22 , C09B23/086 , C09B23/105 , C09B47/00 , C09B62/00
摘要： Halo-organic heterocyclic compounds are described, in which at least two halogen atoms are bound to a nitrogen-containing heterocyclic terminal moiety of the compound, with at least one of such halogen atoms being iodine or bromine. Also described are polymethine dyes based on these heterocyclic compounds, and dendrimeric compounds and conjugates of such polymethine dyes. The polymethine dyes are characterized by enhanced properties, e.g., brightness, photostability, sensitivity and/or selective affinity that make them useful to target cancer cells, pathogenic microorganisms, and/or other biological materials, in applications such as photodynamic therapy, photodynamic antimicrobial chemotherapy (PACT), cancer treatment, selective removal or attachment of biological materials, antimicrobial coating materials, and other diagnostic, theranostic, spectrum shifting, deposition/growth, and analytic applications.
摘要翻译：描述了卤代有机杂环化合物，其中至少两个卤素原子与化合物的含氮杂环末端部分结合，其中至少一个这样的卤素原子是碘或溴。还描述了基于这些杂环化合物的聚甲炔染料，以及这些聚甲炔染料的树枝状大分子化合物和共轭物。聚甲炔染料的特征在于在诸如光动力学治疗，光动力学抗微生物化学疗法的应用中增强的性能，例如亮度，光稳定性，敏感性和/或选择性亲和力，使其可用于靶向癌细胞，致病微生物和/或其他生物材料（PACT），癌症治疗，选择性去除或附着生物材料，抗微生物涂层材料以及其他诊断，分析，频谱移位，沉积/生长和分析应用。

32. 发明申请

WO2013134081A2 HALOGENATED COMPOUNDS FOR PHOTODYNAMIC THERAPY 审中-公开
标题翻译：卤化化合物的光动力疗法
公开(公告)号：WO2013134081A2
公开(公告)日：2013-09-12
申请号：PCT/US2013/028776
申请日：2013-03-02
申请人： NANOQUANTUM SCIENCES. INC.
发明人： JONES, Gary, W. , TATARETS, Anatoliy, L. , PATSENKER, Leonid, D.
CPC分类号： A61K41/0057 , A61K31/403 , A61K31/404 , A61K31/438 , A61K41/0071 , A61N1/30 , A61N5/062 , A61N5/10 , A61N2005/0659 , A61N2005/0663 , C07D209/04 , C07D209/08 , C07D209/10 , C07D209/18 , C07D209/24 , C07D209/58 , C07D209/60 , C07D277/62 , C07D277/64 , C07D293/12 , C07D401/02 , C07D403/06 , C07D403/14 , C07D417/06 , C07D471/10 , C07D487/22 , C09B23/086 , C09B23/105 , C09B47/00 , C09B62/00
摘要： Halo-organic heterocyclic compounds are described, in which at least two halogen atoms are bound to a nitrogen-containing heterocyclic terminal moiety of the compound, with at least one of such halogen atoms being iodine or bromine. Also described are polymethine dyes based on these heterocyclic compounds, and dendrimeric compounds and conjugates of such polymethine dyes. The polymethine dyes are characterized by enhanced properties, e.g., brightness, photostability, sensitivity and/or selective affinity that make them useful to target cancer cells, pathogenic microorganisms, and/or other biological materials, in applications such as photodynamic therapy, photodynamic antimicrobial chemotherapy (PACT), cancer treatment, selective removal or attachment of biological materials, antimicrobial coating materials, and other diagnostic, theranostic, spectrum shifting, deposition/growth, and analytic applications.
摘要翻译：描述了卤代有机杂环化合物，其中至少两个卤素原子键合到化合物的含氮杂环末端部分上，其中至少一个这样的卤素原子是碘或溴。还描述了基于这些杂环化合物的聚甲炔染料，以及这些聚甲炔染料的树枝状化合物和缀合物。聚甲炔染料的特征在于在诸如光动力治疗，光动力学抗微生物化学疗法的应用中使其可用于靶向癌细胞，致病微生物和/或其他生物材料的亮度，光稳定性，敏感性和/或选择性亲和力（PACT），癌症治疗，选择性去除或附着生物材料，抗菌涂层材料以及其他诊断，诊断，频谱转移，沉积/生长和分析应用。

33. 发明申请

WO2011126544A3 THYMOQUINONE ANALOGS FOR THE TREATMENT OF PANCREATIC CANCER 审中-公开
标题翻译： THYMOQUINONE用于治疗胰腺癌的模拟物
公开(公告)号：WO2011126544A3
公开(公告)日：2012-04-19
申请号：PCT/US2011000561
申请日：2011-03-28
申请人： UNIV WAYNE STATE , SARKAR FAZLUL H , MOHAMMAD RAMZI M
发明人： SARKAR FAZLUL H , MOHAMMAD RAMZI M
IPC分类号： A01N35/00 , A61K31/12 , C07C49/00
CPC分类号： C07D401/02
摘要： Analogs of thymoquinone, an active compound extracted from Nigella sativa (black seed oil) are 2,5-bis (alkyl/aryl amino) 1, 4-benzoquinones, are more potent than the naturally-occurring compound (e.g, have a lower IC50) in terms of inhibition of cell growth, induction of apoptosis, and modulation of transcription fact NF-?B. Used in conjunction with conventional chemotherapeutic agents, such as gemcitibine or oxaliplatin, the analogs sensitize gemcitabine-resistant pancreatic cancer cells to gemcitabine-induced apoptosis. A preferred compound is 2,5-dichloro- 3,6-bis[3-methoxyphenyl)amino]cyclohexa-2,5,-diene- 1,4-dione.
摘要翻译：从Nigella sativa（黑籽油）提取的活性化合物的胸腺醌类似物是2,5-双（烷基/芳基氨基）1,4-苯醌，比天然化合物更有效（例如，具有较低的IC 50 ）在抑制细胞生长，诱导凋亡以及调控转录事实NF-κB方面。与常规化学治疗剂（如吉西他滨或奥沙利铂）结合使用，类似物可将吉西他滨耐药胰腺癌细胞增强为吉西他滨诱导的细胞凋亡。优选的化合物是2,5-二氯-3,6-双[3-甲氧基苯基]氨基]环己-1,5-二烯-1,4-二酮。

34. 发明申请

WO2010131922A4 AMIDE COMPOUND, PREPARATION METHOD THEREOF AND PHARMACEUTICAL COMPOSITION COMPRISING SAME 审中-公开
标题翻译：酰胺化合物，其制备方法和包含它们的药物组合物
公开(公告)号：WO2010131922A4
公开(公告)日：2011-05-26
申请号：PCT/KR2010003060
申请日：2010-05-14
申请人： KOREA RES INST CHEM TECH , HEO JUNG NYOUNG , KIM BUM TAE , LEE HYUK , CHANG SUNG YOUN , LEE ZANG HEE , KIM SEONG HWAN , RYOO HYUN-MO
发明人： HEO JUNG NYOUNG , KIM BUM TAE , LEE HYUK , CHANG SUNG YOUN , LEE ZANG HEE , KIM SEONG HWAN , RYOO HYUN-MO
IPC分类号： C07C237/40 , A61K31/76 , A61P19/00 , C07D209/46
CPC分类号： C07D209/46 , C07D401/02 , C07D405/04 , C07D409/10
摘要： The present invention relates to an amide compound or a pharmaceutically acceptable salt thereof, a preparation method thereof, and a pharmaceutical composition comprising the same. The inventive amide compound facilitates bone formation and inhibits bone loss, and is therefore useful for preventing and treating bone disorders such as osteoporosis, osteodystrophy, bone fracture, periodontal disease, Paget's disease, bone metastasis, and rheumatoid arthritis.
摘要翻译：本发明涉及酰胺化合物或其药学上可接受的盐，其制备方法和包含其的药物组合物。本发明的酰胺化合物促进骨形成并抑制骨损失，因此可用于预防和治疗骨疾病，例如骨质疏松症，骨营养不良，骨折，牙周病，佩吉特氏病，骨转移和类风湿性关节炎。

35. 发明申请

WO2010007046A3 HETEROARYL DERIVATIVES AS DGAT1 INHIBITORS 审中-公开
标题翻译：异丙肾上腺素衍生物作为DGAT1抑制剂
公开(公告)号：WO2010007046A3
公开(公告)日：2010-07-22
申请号：PCT/EP2009058960
申请日：2009-07-14
申请人： NOVARTIS AG , FORSTER CORNELIA JUTTA , KWAK YOUNG-SHIN , NAKAJIMA KATSUMASA , WANG BING
发明人： FORSTER CORNELIA JUTTA , KWAK YOUNG-SHIN , NAKAJIMA KATSUMASA , WANG BING
IPC分类号： A61P3/10 , A61K31/427 , A61P3/04 , C07D213/75 , C07D231/40 , C07D249/14 , C07D277/46 , C07D401/12 , C07D403/12 , C07D413/12 , C07D417/04 , C07D417/06 , C07D417/12 , C07D417/14 , C07D471/10
CPC分类号： C07D249/14 , C07D401/02 , C07D401/12 , C07D403/12 , C07D405/12 , C07D413/12
摘要： The invention relates to compounds of formula (I): where A is an optionally substituted heteroaryl, useful for treating disorders mediated by acyl coA- diacylglycerol acyl transferase 1 (DGAT1), e.g. metabolic disorders. The invention also provides methods of treating such disorders, and compounds and compositions etc. for their treatment.
摘要翻译：本发明涉及式（I）的化合物：其中A是可用于治疗由酰基辅酶A - 二酰基甘油酰基转移酶1（DGAT1）介导的病症的任选取代的杂芳基，例如。代谢紊乱。本发明还提供了治疗这些病症的方法，以及用于治疗的化合物和组合物等。

36. 发明申请

WO2010034671A1 PYRINE OR PYRAZINE DERIVATIVES FOR TREATING HCV 审中-公开
标题翻译：用于治疗HCV的吡嗪或吡嗪衍生物
公开(公告)号：WO2010034671A1
公开(公告)日：2010-04-01
申请号：PCT/EP2009/062103
申请日：2009-09-18
申请人： F. HOFFMANN-LA ROCHE AG , CHIN, Elbert , LI, Jim , TALAMAS, Francisco Xavier , WANG, Beihan
发明人： CHIN, Elbert , LI, Jim , TALAMAS, Francisco Xavier , WANG, Beihan
IPC分类号： C07D401/02 , C07D401/14 , C07D405/02 , C07D405/14 , C07D413/14 , A61K31/44 , A61K31/5377 , A61P31/12
CPC分类号： C07D405/02 , C07D401/02 , C07D401/14 , C07D405/14 , C07D413/14
摘要： Compounds having the formula I wherein R 1 , R 2a , R 2b , R 2c , R 3 , Y and p are as defined herein and C2-C3 is a single or double bond are Hepatitis C virus NS5b polymerase inhibitors. Also disclosed are compositions and methods for treating an HCV infection and inhibiting HCV replication.
摘要翻译：具有式I的化合物，其中R1，R2a，R2b，R2c，R3，Y和p如本文所定义，C2-C3是单键或双键，是丙型肝炎病毒NS5b聚合酶抑制剂。还公开了用于治疗HCV感染和抑制HCV复制的组合物和方法。

37. 发明申请

WO2006058201A2 HETEROCYCLIC AND BICYCLIC COMPOUNDS, COMPOSITIONS AND METHODS 审中-公开
标题翻译：杂环和双环化合物，组合物和方法
公开(公告)号：WO2006058201A2
公开(公告)日：2006-06-01
申请号：PCT/US2005042723
申请日：2005-11-23
申请人： REDDY US THERAPEUTICS INC , PAL MANOJIT , KHANNA ISH , SUBRAMANIAN VENKATARAMAN , PADAKANTI SRINIVAS , PILLARISETTI SIVARAM
发明人： PAL MANOJIT , KHANNA ISH , SUBRAMANIAN VENKATARAMAN , PADAKANTI SRINIVAS , PILLARISETTI SIVARAM
IPC分类号： A61K31/5377 , A61K31/4706 , A61K31/4709 , C07D215/38 , C07D413/02
CPC分类号： C07D215/38 , C07D215/44 , C07D401/02 , C07D401/04 , C07D403/04 , C07D409/04 , C07D413/02
摘要： The present invention provides, among other things, new bicyclo heterocyclic compounds, compositions comprising these heterocyclic compounds, methods of making the heterocyclic compounds, and methods of using these heterocyclic compounds for treating a variety of conditions and disease states associated with, for example, cellular proliferation, inflammation, glycosidase expression, or the low expression of Perlecan.
摘要翻译：本发明尤其提供了新的双环杂环化合物，包含这些杂环化合物的组合物，制备杂环化合物的方法，以及使用这些杂环化合物治疗与例如细胞相关的多种病症和疾病状态的方法增殖，炎症，糖苷酶表达或Perlecan的低表达。

38. 发明申请

WO2005004866A1 THERAPEUTIC AGENTS USEFUL FOR TREATING PAIN 审中-公开
标题翻译：治疗药物有用的治疗药物
公开(公告)号：WO2005004866A1
公开(公告)日：2005-01-20
申请号：PCT/US2004/019189
申请日：2004-06-14
申请人： EURO-CELTIQUE, S.A. , KYLE, Donald, J. , SUN, Qun , TAFESSE, Laykea
发明人： KYLE, Donald, J. , SUN, Qun , TAFESSE, Laykea
IPC分类号： A61K31/44
CPC分类号： C07D211/78 , C07D213/02 , C07D401/02 , C07D401/04 , C07D401/14 , C07D405/12 , C07D405/14 , C07D413/14 , C07D417/04 , C07D417/14
摘要： A compound of formula: wherein Ar 1 , Ar 2 , V, X, R 3 , R 4 , and m are as disclosed herein or a pharmaceutically acceptable salt thereof (a "Cyclo(hetero)alkenyl Compound"); compositions comprising an effective amount of a Cyclo(hetero)alkenyl Compound; and methods for treating or preventing, e.g., pain, UI, an ulcer, IBD, or IBS in an animal, comprising administering to an animal in need thereof an effective amount of a Cyclo(hetero)alkenyl Compound are disclosed herein.
摘要翻译：下式化合物：其中Ar 1，Ar 2，V，X，R 3，R 4和m如本文所公开或其药学上可接受的盐（“环（杂）烯基化合物”）; 包含有效量的环（杂）烯基化合物的组合物; 以及用于在动物中治疗或预防例如疼痛，UI，溃疡，IBD或IBS的方法，包括向有需要的动物施用有效量的环（杂）烯基化合物。

39. 发明申请

WO99024422A1 AZARING-ETHER DERIVATIVES AND THEIR USE AS NICOTINIC ACH RECEPTOR MODULATORS 审中-公开
标题翻译：亚胺衍生物及其作为非线性ACH受体调节剂的用途
公开(公告)号：WO99024422A1
公开(公告)日：1999-05-20
申请号：PCT/DK1998/000478
申请日：1998-11-05
IPC分类号： A61K31/4427 , A61K31/4439 , A61K31/4545 , A61K31/55 , A61P25/00 , A61P25/14 , A61P25/16 , A61P25/28 , A61P25/30 , A61P29/00 , C07D401/12 , C07D403/12 , A61K31/44
CPC分类号： C07D401/02 , C07D401/12 , C07D403/12
摘要： The present invention discloses compounds represented by general formula (I) any of its enantiomers or any mixture thereof, or a pharmaceutically acceptable salt thereof; wherein m is 1, 2 or 3; n is 1, 2 or 3; R represents hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkylalkyl, aryl or aralkyl; and R represents a monocyclic 5 to 6 membered heterocyclic group which may be substituted one or more times with substituents selected from the group consisting of alkyl, cycloalkyl, cycloalkylalkyl, alkenyl, alkynyl, alkoxy, cycloalkoxy, methylenedioxy, halogen, CF3, OCF3, CN, amino, nitro, -COOR , -CONR R , -NH-CO2R , NHCO-R , -OCO-NR R ; wherein R and R independently represents hydrogen or alkyl; aryl optionally substituted one or more times with alkyl, cycloalkyl, cycloalkylalkyl alkenyl, alkynyl, alkoxy, cycloalkoxy, methylenedioxy, halogen, CF3, OCF3, CN, amino and nitro; -X-alkyl-Y-alkyl wherein X and Y independently represents O, S, NH, N-alkyl or Se; and alkyl is optionally substituted with alkoxy or thioalkoxy; -X-(alkyl)o-aryl- wherein o is 0 or 1 and X represents O, S, NH, N-alkyl or Se; optionally substituted one or more times with alkyl, cycloalkyl, cycloalkylalkyl alkenyl, alkynyl, alkoxy, cycloalkoxy, methylenedioxy, halogen, CF3, OCF3, CN, amino and nitro; -X-(alkyl)o-5- or 6-membered heterocyclic monocyclic group wherein o is 0 or 1 and X represents O, S, NH, N-alkyl or Se; optionally substituted one or more times with alkyl, cycloalkyl, cycloalkylalkyl alkenyl, alkynyl, alkoxy, cycloalkoxy, methylenedioxy, halogen, CF3, OCF3, CN, amino and nitro; a monocyclic 5 to 6 membered heterocyclic group optionally substituted one or more times with alkyl, cycloalkyl, cycloalkylalkyl, alkenyl, alkynyl, alkoxy, cycloalkoxy, methylenedioxy, halogen, CF3, OCF3, CN, amino and nitro; or R represents a bicyclic heterocyclic group, composed of a 5 to 6 membered monocyclic heterocyclic group fused to a benzene ring, and which may be substituted one or more times with substituents selected from the group consisting of alkyl, cycloalkyl, cycloalkylalkyl alkenyl, alkynyl, alkoxy, alkoxy-alkoxy, cycloalkoxy, methylenedioxy, halogen, CF3, OCF3, CN, amino, nitro, aryl optionally substituted one or more times with alkyl, cycloalkyl, cycloalkylalkyl alkenyl, alkynyl, alkoxy, cycloalkoxy, methylenedioxy, halogen, CF3, OCF3, CN, amino and nitro; and a monocyclic 5 to 6 membered heterocyclic group optionally substituted one or more times with alkyl, cycloalkyl, cycloalkylalkyl alkenyl, alkynyl, alkoxy, cycloalkoxy, methylenedioxy, halogen, CF3, OCF3, CN, amino and nitro. The compounds of the invention are useful as nicotinic ACh receptor ligands.
摘要翻译：本发明公开了通式（I）表示的任何对映体或其任何混合物或其药学上可接受的盐; 其中m为1,2或3; n为1,2或3; R代表氢，烷基，烯基，炔基，环烷基，环烷基烷基，芳基或芳烷基; R 1表示可以被选自烷基，环烷基，环烷基烷基，链烯基，炔基，烷氧基，环烷氧基，亚甲二氧基，卤素，CF 3， OCF 3，CN，氨基，硝基，-COOR 3，-CONR 2 R 3，-NH-CO 2 R 2，NHCO-R 2，-OCO-NR 2 R 3 ; 其中R 2和R 3独立地表示氢或烷基; 芳基任选被一个或多个烷基，环烷基，环烷基烷基烯基，炔基，烷氧基，环烷氧基，亚甲二氧基，卤素，CF 3，OCF 3，CN，氨基和硝基取代; -X-烷基-N-烷基，其中X和Y独立地表示O，S，NH，N-烷基或Se; 烷基任选被烷氧基或硫代烷氧基取代; -X-（烷基）邻 - 芳基 - 其中o是0或1，X代表O，S，NH，N-烷基或Se; 任选地被烷基，环烷基，环烷基烷基烯基，炔基，烷氧基，环烷氧基，亚甲二氧基，卤素，CF 3，OCF 3，CN，氨基和硝基取代一次或多次; 其中o为0或1，X代表O，S，NH，N-烷基或Se的-X-（烷基）邻-5-或6-元杂环单环基; 任选地被烷基，环烷基，环烷基烷基烯基，炔基，烷氧基，环烷氧基，亚甲二氧基，卤素，CF 3，OCF 3，CN，氨基和硝基取代一次或多次; 任选被烷基，环烷基，环烷基烷基，烯基，炔基，烷氧基，环烷氧基，亚甲二氧基，卤素，CF 3，OCF 3，CN，氨基和硝基取代一次或多次的单环5至6元杂环基; 或R 1表示双环杂环基，其由与苯环稠合的5至6元单环杂环基组成，并且可以被取代基取代一次或多次，所述取代基选自烷基，环烷基，环烷基烷基烯基炔基，烷氧基，烷氧基 - 烷氧基，环烷氧基，亚甲二氧基，卤素，CF 3，OCF 3，CN，氨基，硝基，任选被烷基，环烷基，环烷基烷基烯基，炔基，烷氧基，环烷氧基，亚甲二氧基， CF 3，OCF 3，CN，氨基和硝基; 和任选被烷基，环烷基，环烷基烷基烯基，炔基，烷氧基，环烷氧基，亚甲二氧基，卤素，CF 3，OCF 3，CN，氨基和硝基取代一次或多次的单环5至6元杂环基。本发明的化合物可用作烟碱ACh受体配体。

40. 发明申请

WO2017121647A1 3-((HETERO-)ARYL)-8-AMINO-2-OXO-1,3-DIAZA-SPIRO-[4.5]-DECANE DERIVATIVES 审中-公开
标题翻译： 3 - （（杂芳基）芳基）-8-氨基-2-氧杂-1,3-二氮杂 - 螺[4.5] - 二十烷衍生物
公开(公告)号：WO2017121647A1
公开(公告)日：2017-07-20
申请号：PCT/EP2017/025005
申请日：2017-01-13
申请人： GRÜNENTHAL GMBH
发明人： KÜHNERT, Sven , KOENIGS, René Michael , KLESS, Achim , WEGERT, Anita , KONETZKI, Ingo , RATCLIFFE, Paul , JOSTOCK, Ruth , KOCH, Thomas , LINZ, Klaus , SCHRÖDER, Wolfgang
IPC分类号： C07D235/02 , A61K31/4166 , A61P25/00
CPC分类号： C07D487/04 , C07D235/02 , C07D401/02 , C07D401/04 , C07D401/14 , C07D403/04 , C07D403/14 , C07D405/02 , C07D405/06 , C07D405/14 , C07D409/04 , C07D409/14 , C07D413/02 , C07D413/14 , C07D417/04 , C07D471/04
摘要： The invention relates to 3-((hetero-)aryl)-8-amino-2-oxo-1,3-diaza-spiro-[4.5]-decane derivatives, their preparation and their use in medicine, particularly in the treatment of pain.
摘要翻译：本发明涉及3 - （（杂） - 芳基）-8-氨基-2-氧代-1,3-二氮杂 - 螺[4.5] - 癸烷衍生物，其制备方法和用途在医学上，特别是在治疗疼痛方面。

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