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1. 发明申请

WO03018552A3 AROMATIC AND HETEROAROMATIC ACID HALIDES FOR SYNTHESIZING POLYAMIDES 审中-公开
标题翻译：芳香和杂芳酸用于合成聚酰胺
公开(公告)号：WO03018552A3
公开(公告)日：2003-05-30
申请号：PCT/US0227953
申请日：2002-08-30
申请人： PHARMACIA CORP , PHILLION DENNIS P
发明人： PHILLION DENNIS P
IPC分类号： C07C17/16 , C07C17/18 , C07C19/01 , C07C23/08 , C07C51/56 , C07C53/40 , C07C53/42 , C07C63/10 , C07C65/03 , C07C65/05 , C07C201/14 , C07C205/57 , C07C209/00 , C07C209/74 , C07C211/24 , C07C211/29 , C07C269/06 , C07C271/22 , C07C303/02 , C07C303/38 , C07C309/86 , C07C311/16 , C07D207/34 , C07D207/416 , C07D233/90 , C07D307/68 , C07D309/10 , C07D403/14 , C07F7/12 , C07F7/18 , C07F9/12 , C07F9/14 , C07F9/40 , C07F9/42 , C07F9/44 , C08F8/30
CPC分类号： C07D403/14 , C07B2200/11 , C07C17/16 , C07C205/57 , C07C209/74 , C07C269/06 , C07C303/02 , C07D207/34 , C07D233/90 , C07D307/68 , C07F9/12 , C07F9/1406 , C07F9/4015 , C07F9/4075 , C07F9/42 , C07F9/4465 , C08F8/30 , C07C211/24 , C07C271/22 , C07C309/86
摘要： The present invention is directed to protected amino acid halide monomers and oligomers, and to their use in the efficient sythesis of polyamides. The present invention is further directed to the use of -haloenamine reagents, which may optionally be immobilized, for the preparation of the amino acid halides.
摘要翻译：本发明涉及被保护的氨基酸卤化物单体和低聚物，并涉及它们在聚酰胺的有效合成中的用途。本发明进一步涉及可任选地固定化的N-卤代苯胺试剂用于制备氨基酸卤化物的用途。

2. 发明申请

WO2013017564A3 METHOD FOR THE MANUFACTURE OF COMPOUNDS CONTAINING AN ALPHA-OXY PHOSPHORUS GROUP BY USING P-X COMPONENTS 审中-公开
标题翻译：通过使用P-X组分制备含有α-氧代磷酸酯基团的化合物的方法
公开(公告)号：WO2013017564A3
公开(公告)日：2013-05-02
申请号：PCT/EP2012064881
申请日：2012-07-30
申请人： STRAITMARK HOLDING AG , BURCK SEBASTIAN R W , NOTTE PATRICK
发明人： BURCK SEBASTIAN R W , NOTTE PATRICK
IPC分类号： C07F9/30 , C07F9/38 , C07F9/40 , C07F9/42 , C07F9/53 , C07F9/655 , C07F9/6571 , C07F9/6584
CPC分类号： C07F9/301 , C07F9/305 , C07F9/3808 , C07F9/4006 , C07F9/42 , C07F9/5325 , C07F9/65515 , C07F9/657181 , C07F9/65848
摘要： A method for the manufacture of compounds containing an alpha- oxy phosphorus group is disclosed. A P-X component having at least one P-X bond, whereby the phosphorus of the P-X bond has the +3 oxidation state with X being C1 or Br, is reacted in a specific equivalent ratio with a compound containing an alpha-oxy carboxylic acid group, followed by conducting the reaction and optionally adding a quenching agent at the end of the reaction. The compounds containing an alpha-oxy phosphorus group formed are then recovered.
摘要翻译：公开了一种制备含有α-氧磷基团的化合物的方法。具有至少一个PX键的PX组分，其中PX键的磷具有+3氧化态，X为C1或Br，以特定当量比与含有α-氧基羧酸基团的化合物反应，随后通过进行反应和任选地在反应结束时加入猝灭剂。然后回收含有形成的α-氧磷基团的化合物。

3. 发明申请

WO2006037869A3 FLUOROPHOSPHONOCINNAMIC COMPOUNDS, SYNTHESIS AND USES FOR TREATING DISORDERS CAUSED BY OXIDATIVE STRESS 审中-公开
标题翻译：氟代磷酸化合物，合成和用于治疗由氧化应激引起的疾病的用途
公开(公告)号：WO2006037869A3
公开(公告)日：2006-06-08
申请号：PCT/FR2005002376
申请日：2005-09-26
申请人： CENTRE NAT RECH SCIENT , UNIV TOULOUSE 3 PAUL SABATIER , INST NAT SANTE RECH MED , BALTAS MICHEL , BEDOS-BELVAL FLORENCE , DURAN HUBERT , LAPEYRE CAROLINE , NEGRE-SALVAYRE ANNE-ELISABETH
发明人： BALTAS MICHEL , BEDOS-BELVAL FLORENCE , DURAN HUBERT , LAPEYRE CAROLINE , NEGRE-SALVAYRE ANNE-ELISABETH
IPC分类号： C07F9/42 , A61K31/662 , A61P9/10
CPC分类号： C07F9/425
摘要： The invention concerns a method for specifically fluorinating a phosphorus atom of a phosphonocinnamic compound of general formula (II) or (II'), wherein: X is selected among: an oxygen atom, a sulphur atom; R 1 , R 2 , R 3 , R 4 , R 5 and R 6 being selected among H, an alkyl group, an aryl group, OH, O-alkyl, S-alkyl, NH 2 , NH-alkyl, N-(alkyl) 2 group; R 7 being selected among: H, an alkyl group, an aryl group, a silyl group; R 8 being selected among: H, an alkyl group, an aryl group; TBDPS representing a t-butyldiphenylsilyl group. Said method consists in reacting said compound with a fluorinating agent comprising a complex formed between a tertiary amine and hydrogen fluoride. The invention also concerns novel fluorinated compounds thus prepared, as well as therapeutic compositions comprising such fluorinated compounds, and their uses for treating atherosclerosis.
摘要翻译：本发明涉及一种通式（II）或（II'）的膦腈基化合物的磷原子特异性氟化的方法，其中：X选自：氧原子，硫原子; R 1，R 2，R 3，R 4，R 5和R 5， R 6选自H，烷基，芳基，OH，O-烷基，S-烷基，NH 2，NH-烷基，N-（烷基）2 组; R 7选自：H，烷基，芳基，甲硅烷基; R 8选自：H，烷基，芳基; 代表叔丁基二苯基甲硅烷基的TBDPS。所述方法包括使所述化合物与包含在叔胺和氟化氢之间形成的络合物的氟化剂反应。本发明还涉及由此制备的新型氟化化合物以及包含这种氟化化合物的治疗组合物及其用于治疗动脉粥样硬化的用途。

4. 发明申请

WO2013017564A2 METHOD FOR THE MANUFACTURE OF COMPOUNDS CONTAINING AN ALPHA-OXY PHOSPHORUS GROUP BY USING P-X COMPONENTS 审中-公开
标题翻译：通过使用P-X组分制备含有α-氧代磷酸酯基团的化合物的方法
公开(公告)号：WO2013017564A2
公开(公告)日：2013-02-07
申请号：PCT/EP2012/064881
申请日：2012-07-30
申请人： STRAITMARK HOLDING AG , BURCK, Sebastian, R., W. , NOTTÉ, Patrick
发明人： BURCK, Sebastian, R., W. , NOTTÉ, Patrick
IPC分类号： C07F9/30 , C07F9/38 , C07F9/40 , C07F9/42 , C07F9/53 , C07F9/655 , C07F9/6571 , C07F9/6584
CPC分类号： C07F9/301 , C07F9/305 , C07F9/3808 , C07F9/4006 , C07F9/42 , C07F9/5325 , C07F9/65515 , C07F9/657181 , C07F9/65848
摘要： A method for the manufacture of compounds containing an α- oxy phosphorus group is disclosed. A P-X component having at least one P-X bond, whereby the phosphorus of the P-X bond has the +3 oxidation state with X being C1 or Br, is reacted in a specific equivalent ratio with a compound containing an α-oxy carboxylic acid group, followed by conducting the reaction and optionally adding a quenching agent at the end of the reaction. The compounds containing an α-oxy phosphorus group formed are then recovered.
摘要翻译：公开了一种制备含有α-氧基的化合物的方法。具有至少一个PX键的PX成分，其中PX键的磷具有+3氧化态，其中X为C1或Br，以特定当量比与含有α-氧基羧酸基团的化合物反应，随后通过进行反应和任选地在反应结束时加入猝灭剂。然后回收含有形成的α-氧磷基团的化合物。

5. 发明申请

WO2004048393A2 NOVEL INHIBITORS OF beta-LACTAMASE 审中-公开
标题翻译：新的β-内酰胺酶抑制剂
公开(公告)号：WO2004048393A2
公开(公告)日：2004-06-10
申请号：PCT/US0336929
申请日：2003-11-19
申请人： METHYLGENE INC , BESTERMAN JEFFREY M , RAHIL JUBRAIL , VAISBURG ARKADII
发明人： BESTERMAN JEFFREY M , RAHIL JUBRAIL , VAISBURG ARKADII
IPC分类号： C07F9/24 , C07F9/38 , C07F9/40 , C07F9/42 , C07F9/44 , C07F9/572 , C07F9/58 , C07F9/60 , C07F9/6506 , C07F9/6524 , C07F9/653 , C07F9/6539 , C07F9/6541 , C07F9/655 , C07F9/6553 , C07F9/6558 , C07F9/00
CPC分类号： C07F9/65586 , C07F9/2491 , C07F9/3808 , C07F9/4006 , C07F9/4084 , C07F9/425 , C07F9/4407 , C07F9/5721 , C07F9/5728 , C07F9/585 , C07F9/588 , C07F9/60 , C07F9/65061 , C07F9/6524 , C07F9/65312 , C07F9/6539 , C07F9/65395 , C07F9/6541 , C07F9/65515 , C07F9/65517 , C07F9/655345 , C07F9/655354 , C07F9/65583
摘要： The invention relates to bacterial antibiotic resistance and, in particular, to compositions and methods for overcoming bacterial antibiotic resistance. The invention provides novel beta-lactamase inhibitors, which are structurally unrelated to the natural product and semi-synthetic beta-lactamase inhibitors presently available, and which do not require beta-lactam pharmacophore. The invention also provides pharmaceutical compositions and methods for inhibiting bacterial growth.
摘要翻译：本发明涉及细菌抗生素抗性，并且特别涉及用于克服细菌抗生素抗性的组合物和方法。本发明提供了新型β-内酰胺酶抑制剂，其在结构上与天然产物和目前可得的半合成β-内酰胺酶抑制剂无关，并且不需要β-内酰胺药效团。本发明还提供了用于抑制细菌生长的药物组合物和方法。

6. 发明申请

WO2016161407A1 FLUORESCENT BISPHOSPHONATE ANALOGS 审中-公开
标题翻译：荧光二磷酸酯类似物
公开(公告)号：WO2016161407A1
公开(公告)日：2016-10-06
申请号：PCT/US2016/025795
申请日：2016-04-02
申请人： UNIVERSITY OF SOUTHERN CALIFORNIA
发明人： MCKENNA, Charles, E. , KASHEMIROV, Boris, A. , SUN, Shuting , NI, Feng
IPC分类号： G01N33/52 , A61K49/08 , A61K49/10 , C07F9/38 , C07F9/42
CPC分类号： A61K49/0052 , A61K49/0021 , A61K49/0032 , A61K49/0043 , C07F9/582 , C07F9/65061 , C07F9/65583 , C07F9/6561
摘要： Fluorescent probes based on N-heterocyclic bisphosphonates or their phosphonocarboxylate analogues are provided. The probes have variable spectroscopic properties, bone mineral binding affinities, and pharmacological activities. Methods for preparing the probes include the use of two complementary linking strategies, one involving an amino group and the other involving a chloride group as a precursor to an amino group. In other versions, bifunctional N-heterocyclic bisphosphonates are provided having an amino group and an azido group as linking moieties. In some versions, the linking chemistry allows attachment of a wide selection of fluorescent dyes in the visible to near-infrared range to any of three clinically important heterocyclic bisphosphonates.
摘要翻译：提供了基于N-杂环二膦酸盐或其膦酰基羧酸酯类似物的荧光探针。探针具有不同的光谱特性，骨矿物结合亲和力和药理活性。制备探针的方法包括使用两种互补连接策略，一种涉及氨基，另一种涉及氯基作为氨基的前体。在其它形式中，提供了具有氨基和叠氮基作为连接部分的双功能N-杂环二膦酸盐。在一些版本中，连接化学物质允许在可见到近红外范围内将广泛选择的荧光染料连接到三种临床上重要的杂环二膦酸盐中的任何一种。

7. 发明申请

WO2010009791A1 VERFAHREN ZUR HERSTELLUNG VON BIS(FLUORALKYL)PHOSPHINSÄURECHLORIDEN ODER FLUORALKYLPHOSPHONSÄUREDICHLORIDEN 审中-公开
标题翻译：用于生产双（氟代烷基）PHOSPHINSÄURECHLORIDENORFLUORALKYLPHOSPHONSÄUREDICHLORIDEN
公开(公告)号：WO2010009791A1
公开(公告)日：2010-01-28
申请号：PCT/EP2009/004535
申请日：2009-06-24
申请人： MERCK PATENT GMBH , IGNATYEV, Nikolai (Mykola) , AUST, Emil Ferdinand , BEJAN, Dana , WILLNER, Helge
发明人： IGNATYEV, Nikolai (Mykola) , AUST, Emil Ferdinand , BEJAN, Dana , WILLNER, Helge
IPC分类号： C07F9/30 , C07F9/34 , C07F9/38 , C07F9/42 , C07F9/535
CPC分类号： C07F9/301 , C07F9/34 , C07F9/3808 , C07F9/42 , C07F9/535
摘要： Die Erfindung betrifft ein Verfahren zur Herstellung von Bis(fluoralkyl)phosphinsäurechloriden oder Fluoralkylphosphonsäuredichloriden durch Umsetzung der entsprechenden Bis(fluoralkyl)phosphinsäure oder Fluoralkylphosphonsäure mit Aryltetrachlorphosphoran als Chlorierungsmittel.
摘要翻译：本发明涉及一种用于双（氟烷基）phosphinsäurechloridenFluoralkylphosphonsäuredichloriden的制备或由相应的双（氟代烷基）次膦酸或Fluoralkylphosphonsäure与aryltetrachlorophosphorane作为氯化剂反应。

8. 发明申请

WO03068784A2 ACYL- AND BISACYLPHOSPHINE DERIVATIVES 审中-公开
标题翻译：酰基和二酰基
公开(公告)号：WO03068784A2
公开(公告)日：2003-08-21
申请号：PCT/EP0301053
申请日：2003-02-04
申请人： BASF AG , NOE RALF , HENNE ANDREAS , MAASE MATTHIAS
发明人： NOE RALF , HENNE ANDREAS , MAASE MATTHIAS
IPC分类号： C07F9/30 , C07F9/32 , C07F9/34 , C07F9/36 , C07F9/40 , C07F9/42 , C08F2/50 , C08F4/00 , G03F7/029 , C07F9/50 , C07F9/52
CPC分类号： C07F9/3294 , C07F9/3252 , C07F9/34 , C07F9/36 , C07F9/4065 , C07F9/409 , C07F9/4093 , C07F9/4096 , C07F9/425 , G03F7/029
摘要： The invention relates to the acyl- and bisacylphosphine derivatives according to formula (I), wherein Y represents O, S, NR3, N-OR3 or N-NR3R4, Z represents O, S, NR3, N-OR3, N-NR3R4 or a free pair of electrons, and FG represents a leaving group and the remaining groups are defined as in the description. The invention further relates to a method for the production of the inventive derivatives and to their use.
摘要翻译：根据式I，其中Y是酰基和二酰基膦衍生物O，S，NR 3，N-OR 3或N-NR 3 R 4，Z是O，S，NR 3，N-NR 3 R 4，或自由电子对，和FG是指离去基团，并且其它基团如在所描述的刚才提到的含义，其制备方法及其用途。

9. 发明申请

WO01002411A1 SULFONAMIDOMETHYL PHOSPHONATE INHIBITORS OF beta -LACTAMASE 审中-公开
标题翻译： β-LACTAMASE的磺酰亚胺乙酸盐抑制剂
公开(公告)号：WO01002411A1
公开(公告)日：2001-01-11
申请号：PCT/US2000/018344
申请日：2000-07-05
IPC分类号： A61K45/00 , A61K31/662 , A61K31/664 , A61P31/00 , A61P31/04 , A61P43/00 , C07F9/24 , C07F9/38 , C07F9/40 , C07F9/42 , C07F9/44 , C07F9/572 , C07F9/58 , C07F9/60 , C07F9/6503 , C07F9/6506 , C07F9/653 , C07F9/6539 , C07F9/6541 , C07F9/655 , C07F9/6553 , A61K31/66
CPC分类号： C07F9/655354 , C07F9/2491 , C07F9/3808 , C07F9/4006 , C07F9/425 , C07F9/4407 , C07F9/5721 , C07F9/5728 , C07F9/585 , C07F9/588 , C07F9/60 , C07F9/6539 , C07F9/65395 , C07F9/6541 , C07F9/65515 , C07F9/65517 , C07F9/655345
摘要： The intention relates to bacterial antibiotic resistance and, in particular, to compositions and methods for overcoming bacterial antibiotic resistance. The invention provides novel beta -lactamase inhibitors, which are structurally unrelated to the natural product and semi-synthetic beta -lactamase inhibitors presently available, and which do not require a beta -lactam pharmacophore. The invention also provides pharmaceutical compositions and methods for inhibiting bacterial growth.
摘要翻译：意图涉及细菌抗生素抗性，特别涉及克服细菌抗生素抗性的组合物和方法。本发明提供了新型β-内酰胺酶抑制剂，其在结构上与目前可获得的天然产物和半合成β-内酰胺酶抑制剂无关，并且不需要β-内酰胺药效团。本发明还提供用于抑制细菌生长的药物组合物和方法。

10. 发明申请

WO00002566A1 PREPARATION AND USE OF SULFUR-CONTAINING PHOSPHONOFORMATE DERIVATIVES AND ANALOGS 审中-公开
标题翻译：含硫磺化合物衍生物和类似物的制备和使用
公开(公告)号：WO00002566A1
公开(公告)日：2000-01-20
申请号：PCT/US1999/015775
申请日：1999-07-13
IPC分类号： C07F9/38 , C07F9/40 , C07F9/42 , A61K31/66
CPC分类号： C07F9/3891 , C07F9/4065 , C07F9/425
摘要： Preparation of phosphonoformic acid analogues containing one, two, three, or more sulfur atoms are described, with specific examples. Such compounds, not excluding cognates, derivatives, and homologues thereof, are proposed to be used directly, or as prodrugs, in treating viral infections, including but not limited to HIV, herpesviruses including HSV, EBV, VZV, CMV, HSV-6 and HSV-8 (Kaposi's sarcoma); HPV; rhinoviruses; and hepatitis-linked viruses. They are also proposed to be used in treating neoplasms, and for diagnosis and therapy of diseases of bone metabolism. The compounds of the present invention are also designed as to create novel biologically active compounds or prodrugs.
摘要翻译：具体实例描述了含有一个，两个，三个或更多个硫原子的膦酰基甲酸类似物的制备。提出这种不排除同源物，衍生物和同系物的化合物直接或作为前药用于治疗病毒感染，包括但不限于HIV，疱疹病毒，包括HSV，EBV，VZV，CMV，HSV-6和 HSV-8（卡波西肉瘤）; HPV; 鼻病毒; 和肝炎病毒。它们也被用于治疗肿瘤，用于骨代谢疾病的诊断和治疗。本发明的化合物也被设计成产生新的生物活性化合物或前药。

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