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31. 发明授权

US3414393A Gasoline compositions containing diphosphonates 失效
标题翻译：含有二膦酸盐的汽油组合物
公开(公告)号：US3414393A
公开(公告)日：1968-12-03
申请号：US59044966
申请日：1966-08-29
申请人： MONSANTO CO
发明人： FITCH STEVEN J , IRANI RIYAD R
IPC分类号： C07F9/38 , C07F9/572 , C11D1/34 , C11D3/36 , D06L1/04
CPC分类号： C07F9/3839 , C07F9/5722 , C11D1/342 , C11D3/361 , D06L1/04

32. 发明授权

US5919774A Pyrroles as sPLA.sub.2 inhibitors 失效
标题翻译：吡咯作为sPLA2抑制剂
公开(公告)号：US5919774A
公开(公告)日：1999-07-06
申请号：US985518
申请日：1997-12-05
申请人： Nicholas J. Bach , Robert D. Dillard , Susan E. Draheim
发明人： Nicholas J. Bach , Robert D. Dillard , Susan E. Draheim
IPC分类号： A61K31/40 , A61P11/00 , A61P11/06 , A61P19/02 , A61P27/16 , A61P29/00 , A61P43/00 , C07D207/32 , C07D207/327 , C07D207/337 , C07F9/572 , C07D207/323 , C07D207/36
CPC分类号： C07D207/327 , C07D207/337 , C07F9/5722
摘要： A class of novel pyrroles is disclosed together with the use of such compounds for inhibiting sPLA.sub.2 mediated release of fatty acids for treatment of conditions such as septic shock.
摘要翻译：一类新颖的吡咯以及这些化合物用于抑制sPLA2介导的脂肪酸释放用于治疗诸如败血性休克的病症的公开。

33. 发明授权

US5770586A Quaternary nitrogen-containing phosphonate compounds, pharmaceutical compositions, and methods of treating abnormal calcium and phosphate metabolism amd methods of treating and preventing dental calculus and plaque 失效
标题翻译：第四纪含氮膦酸酯化合物，药物组合物和治疗异常钙和磷酸盐代谢的方法，治疗和预防牙结石和斑块的方法
公开(公告)号：US5770586A
公开(公告)日：1998-06-23
申请号：US333652
申请日：1994-11-03
申请人： Frank Hallock Ebetino , Susan Mary Kaas , Marion David Francis , Dennis George Anthony Nelson , John Michael Janusz
发明人： Frank Hallock Ebetino , Susan Mary Kaas , Marion David Francis , Dennis George Anthony Nelson , John Michael Janusz
IPC分类号： A61K31/66 , A61K31/663 , A61K31/675 , A61P1/02 , A61P19/08 , A61P29/00 , A61P43/00 , C07F9/38 , C07F9/553 , C07F9/572 , C07F9/576 , C07F9/58 , C07F9/59 , C07F9/6506 , C07F9/653 , C07F9/6539 , C07F9/6561 , A61K31/40 , A61K31/415 , A61K31/42 , A61K31/425
CPC分类号： C07F9/582 , C07F9/3873 , C07F9/5722 , C07F9/5765 , C07F9/592 , C07F9/65062
摘要： The present invention relates to quaternary nitrogen-containing phosphate compounds, and the pharmaceutically-acceptable salts and esters thereof having the general structure: ##STR1## wherein: Z is a saturated, unsaturated, or aromatic, monocyclic or polycyclic carbocycle or monocyclic or polycyclic heterocycle containing one or more heteroatoms selected from O, S, or N; Y is N.sup.+ (R.sup.8).sub.2 or C(R.sup.1).sub.2 and when Y is C(R.sup.1).sub.2, at least one R.sup.2 must be N.sup.+ (R.sup.8).sub.3 ; R.sup.1, R.sup.2, R.sup.5, and R.sup.8 are defined in claim 1, m and n are integers from 0 to 10; m+n is from 0 to 10; R is COOH; PO.sub.3 H.sub.2 ; SO.sub.3 H; or P(O)(OH)R.sub.4, wherein R.sub.4 is substituted or unsubstituted alkyl of 1-8 carbons atoms. The present invention further relates to pharmaceutical compostions containing a safe and effective amount of a compound of the present invention, and pharmaceutically-acceptable excipients. Finally, the present invention relates to methods for treating or preventing pathological conditions characterized by abnormal calcium and phosphate metabolism such as osteoporosis, rheumatoid arthritis, and osteoarthritis in humans or other mammals and to methods for treating or preventing dental calculus, plaque, and gingivitis.
摘要翻译：本发明涉及具有以下一般结构的含季氮含量的磷酸盐化合物及其药学上可接受的盐和酯：其中：Z是饱和的，不饱和的或芳族的单环或多环碳环或单环或多环杂环含有一个或多个选自O，S或N的杂原子; Y为N +（R8）2或C（R1）2，当Y为C（R1）2时，至少一个R2必须为N +（R8）3; R1，R2，R5和R8如权利要求1中所定义，m和n为0至10的整数; m + n为0〜10; R为COOH; PO3H2; SO3H; 或P（O）（OH）R 4，其中R 4是取代或未取代的1-8个碳原子的烷基。本发明还涉及含有安全有效量的本发明化合物和药学上可接受的赋形剂的药物组合物。最后，本发明涉及用于治疗或预防以人或其他哺乳动物为骨质疏松症，类风湿性关节炎和骨关节炎等异常钙和磷酸盐代谢特征的病理状态的方法以及治疗或预防牙结石，斑块和牙龈炎的方法。

34. 发明授权

US5767144A Endothelin antagonists 失效
标题翻译：内皮素拮抗剂
公开(公告)号：US5767144A
公开(公告)日：1998-06-16
申请号：US442575
申请日：1995-05-30
申请人： Martin Winn , Steven A. Boyd , Charles W. Hutchins , Hwan-Soo Jae , Andrew S. Tasker , Thomas W. von Geldern , Jeffrey A. Kester , Bryan K. Sorensen
发明人： Martin Winn , Steven A. Boyd , Charles W. Hutchins , Hwan-Soo Jae , Andrew S. Tasker , Thomas W. von Geldern , Jeffrey A. Kester , Bryan K. Sorensen
IPC分类号： C07D207/16 , C07D401/04 , C07D403/04 , C07D405/04 , C07D405/14 , C07F9/572 , C07F9/59 , A61K31/40 , C07D207/08
CPC分类号： C07D401/04 , C07D207/16 , C07D403/04 , C07D405/04 , C07D405/14 , C07F9/5722 , C07F9/592
摘要： A compound of the formula (I): ##STR1## or a pharmaceutically acceptable salt thereof is disclosed, as well as processes for and intermediates in the preparation thereof, and a method of antagonizing endothelin.
摘要翻译：公开了式（I）的化合物：其中（I）或其药学上可接受的盐，以及其制备方法和中间体，以及拮抗内皮素的方法。

35. 发明授权

US5618803A Targeted drug delivery via phosphonate derivatives 失效
标题翻译：通过膦酸酯衍生物靶向药物递送
公开(公告)号：US5618803A
公开(公告)日：1997-04-08
申请号：US340896
申请日：1994-11-15
申请人： Nicholas S. Bodor
发明人： Nicholas S. Bodor
IPC分类号： A61K31/56 , A61K31/66 , A61K31/675 , A61K31/70 , A61K31/7042 , A61K31/7052 , A61K31/7064 , A61K31/7068 , A61K31/7072 , A61K31/7076 , A61K31/708 , A61K45/00 , A61K47/48 , A61P29/00 , A61P31/12 , A61P43/00 , C07F9/40 , C07F9/553 , C07F9/572 , C07F9/576 , C07F9/58 , C07F9/59 , C07F9/645 , C07F9/6506 , C07F9/6509 , C07F9/6512 , C07F9/6547 , C07F9/6558 , C07F9/6561 , C07H15/252 , C07H19/04 , C07H19/048 , C07H19/052 , C07H19/056 , C07H19/10 , C07H19/12 , C07H19/20 , C07H19/207 , C07H19/23 , C07H19/24 , C07J51/00 , A61K31/135 , C07F9/06
CPC分类号： C07H15/252 , A61K47/48023 , C07F9/4075 , C07F9/4087 , C07F9/5532 , C07F9/5535 , C07F9/5722 , C07F9/5728 , C07F9/5765 , C07F9/582 , C07F9/591 , C07F9/645 , C07F9/65061 , C07F9/650958 , C07F9/65121 , C07F9/65125 , C07F9/6547 , C07F9/65583 , C07F9/65586 , C07F9/6561 , C07F9/65611 , C07F9/65613 , C07F9/65616 , C07H19/04 , C07H19/048 , C07H19/052 , C07H19/056 , C07H19/10 , C07H19/12 , C07H19/20 , C07H19/207 , C07H19/23 , C07H19/24 , C07J51/00 , Y10S514/885
摘要： The invention provides compounds of the formula ##STR1## or a pharmaceutically acceptable salt thereof, wherein [D] is the residue of a drug having a reactive functional group, said functional group being attached, directly or through a bridging group, via an oxygen-phosphorus bond to the phosphorus atom of the ##STR2## moiety; R.sub.1 is C.sub.1 -C.sub.8 alkyl, C.sub.6 -C.sub.10 aryl or C.sub.7 -C.sub.12 aralkyl; R.sub.2 is hydrogen, C.sub.1 -C.sub.8 alkyl, C.sub.6 -C.sub.10 aryl, C.sub.4 -C.sub.9 heteroaryl, C.sub.3 -C.sub.7 cycloalkyl, C.sub.3 -C.sub.7 cycloheteroalkyl or C.sub.7 -C.sub.12 aralkyl; and R.sub.3 is selected from the group consisting of C.sub.1 -C.sub.8 alkyl; C.sub.2 -C.sub.8 alkenyl having one or two double bonds; (C.sub.3 -C.sub.7 cycloalkyl)-C.sub.r H.sub.2r -- wherein r is zero, one, two or three, the cycloalkyl portion being unsubstituted or bearing 1 or 2 C.sub.1 -C.sub.4 alkyl substituents on the ring portion; (C.sub.6 -C.sub.10 aryloxy)C.sub.1 -C.sub.8 alkyl; 2-, 3- or 4-pyridyl; and phenyl-C.sub.r H.sub.2r -- wherein r is zero, one, two or three and phenyl is unsubstituted, or is substituted by 1 to 3 alkyl each having 1 to 4 carbon atoms, alkoxy having 1 to 4 carbon atoms, halo, trifluoromethyl, dialkylamino having 2 to 8 carbon atoms or alkanoylamino having 2 to 6 carbon atoms. The compounds are adapted for targeted drug delivery, especially to the brain.
摘要翻译：本发明提供了式（I）化合物或其药学上可接受的盐，其中[D]是具有反应性官能团的药物的残基，所述官能团直接或通过桥接基团连接，通过与部分的磷原子的氧 - 磷键; R1是C1-C8烷基，C6-C10芳基或C7-C12芳烷基; R2是氢，C1-C8烷基，C6-C10芳基，C4-C9杂芳基，C3-C7环烷基，C3-C7环杂烷基或C7-C12芳烷基; 并且R 3选自C 1 -C 8烷基; 具有一个或两个双键的C 2 -C 8烯基; （C 3 -C 7环烷基）-Cr H 2r-，其中r是0,1,2或3，环烷基部分是未取代的或在环部分带有1或2个C 1 -C 4烷基取代基; （C 6 -C 10芳氧基）C 1 -C 8烷基; 2-，3-或4-吡啶基; 和苯基-CrH 2r-，其中r为0,1,2或3，苯基未取代，或被1至3个具有1至4个碳原子的烷基，具有1至4个碳原子的烷氧基，卤素，三氟甲基， 2至8个碳原子或具有2至6个碳原子的烷酰基氨基。这些化合物适用于靶向药物递送，特别适用于大脑。

36. 发明授权

US5472956A Phosphoramidates useful as antitumor agents 失效
标题翻译：用作抗肿瘤剂的磷酰胺化物
公开(公告)号：US5472956A
公开(公告)日：1995-12-05
申请号：US184305
申请日：1994-01-21
申请人： Richard F. Borch , James P. Schmidt
发明人： Richard F. Borch , James P. Schmidt
IPC分类号： A61K31/66 , A61K31/675 , A61P35/00 , C07F9/572 , C07F9/6506 , C07F9/655 , C07F9/6553 , C07F9/02
CPC分类号： C07F9/65062 , C07F9/5722 , C07F9/65515 , C07F9/655345
摘要： Cyclophosphamide analogs are provided of the general formula: ##STR1## wherein R.sup.1 and R.sup.2 are each (C.sub.2 -C.sub.6)alkyl, substituted with a leaving group such as halo or alkylsulfonyl, R.sup.3 and R.sup.4 are the same as R.sup.1 and R.sup.2 or are H and Ar is a heteroaromatic ring and the pharmaceutically acceptable salts thereof.
摘要翻译：环磷酰胺类似物由以下通式提供：其中R 1和R 2各自为（C 2 -C 6）烷基，被离去基团如卤素或烷基磺酰基取代，R 3和R 4与R 1和R 2相同或为H和 Ar是杂芳环和其药学上可接受的盐。

37. 发明授权

US5442102A Gem-diphosphonic acid nitrosocarbamoyl derivatives, a process for the preparation thereof and pharmaceutical compositions containing them 失效
标题翻译：双膦酸亚硝基氨基甲酰基衍生物，其制备方法和含有它们的药物组合物
公开(公告)号：US5442102A
公开(公告)日：1995-08-15
申请号：US129099
申请日：1993-10-08
申请人： Sergio Tognella , Valeria Livi , Ernesto Menta , Silvano Spinelli
发明人： Sergio Tognella , Valeria Livi , Ernesto Menta , Silvano Spinelli
IPC分类号： A61K31/66 , A61K31/675 , A61P35/00 , C07F9/38 , C07F9/40 , C07F9/553 , C07F9/572 , C07F9/59 , C07F9/6509
CPC分类号： C07F9/5727 , C07F9/3873 , C07F9/5722 , C07F9/592 , C07F9/650958
摘要： Diphosphonic acids of formula (I) are disclosed. These compounds are useful as antitumor agents.
摘要翻译： PCT No.PCT / EP92 / 00745 Sec。 371日期：1993年10月8日 102（e）日期1993年10月8日PCT提交1992年4月3日PCT公布。出版物WO92 / 日期：1992年10月29日。公开了式（I）的二膦酸。这些化合物可用作抗肿瘤剂。

38. 发明授权

US5403838A .alpha.-arylacrylic acid derivatives, their preparation and use for controlling pests and fungi 失效
标题翻译： α-芳基丙烯酸衍生物，它们的制备和用途，用于防治害虫和真菌
公开(公告)号：US5403838A
公开(公告)日：1995-04-04
申请号：US928038
申请日：1992-08-11
申请人： Reinhard Kirstgen , Hans Theobald , Hartmann Koenig , Albrecht Harreus , Klaus Oberdorf , Uwe Kardorff , Volker Harries , Gisela Lorenz , Eberhard Ammermann
发明人： Reinhard Kirstgen , Hans Theobald , Hartmann Koenig , Albrecht Harreus , Klaus Oberdorf , Uwe Kardorff , Volker Harries , Gisela Lorenz , Eberhard Ammermann
IPC分类号： A01N43/36 , A01N43/56 , A01N43/76 , A01N43/80 , C07D207/32 , C07D207/327 , C07D207/337 , C07D207/34 , C07D207/416 , C07D231/12 , C07D231/38 , C07D261/08 , C07D261/10 , C07D261/18 , C07D271/02 , C07D275/02 , C07D275/03 , C07D413/04 , C07D417/04 , C07F9/572 , C07F9/6503 , C07F9/653 , C07F9/6539 , C07D213/30 , C07D307/12 , C07D261/20
CPC分类号： C07D207/337 , A01N43/36 , A01N43/56 , A01N43/80 , C07D231/12 , C07D261/08 , C07D261/10 , C07D275/02 , C07D275/03 , C07D413/04 , C07F9/5722 , C07F9/65033 , C07F9/653 , C07F9/6539
摘要： .alpha.-Arylacrylic acid derivatives of the formula I ##STR1## where the substituents have the following meanings: X C, NY CR.sup.4, N, O, SZ CR.sup.5, N, O, Sn 0 to 4R.sup.1 hydrogen, nitro, cyano, halogen; alkyl, alkoxy, halogenated alkyl, halogenated alkoxy or alkylthio, or, when n is 2, 3 or 4, two adjacent substituents R.sup.1 may together denote a 1,3-butadien-1,4-diyl group which may be substituted;R.sup.2 alkyl; halogenated alkyl, halogen, cyano, nitro, alkoxycarbonyl, dimethylamino, R.sup.2 additionally denotes hydrogen;R.sup.3 hydrogen; substituted or unsubstituted alkyl; a substituted or unsubstituted cyclic structure, which may contain, in addition to carbon atoms, one to three heteroatoms; or a substituted or unsubstituted aromatic system, which may contain, in addition to carbon atoms, one to four nitrogen atoms and one to three heteroatoms;R.sup.4, R.sup.5 hydogen, alkyl; halogenated alKyl, halogen, cyano, nitro, dimethylamino, alkoxycarbonyland pesticides and fungicidal agents containing these compounds.
摘要翻译：式I的α-丙烯酰基丙酸衍生物（I）其中取代基具有以下含义：XC，NY CR4，N，O，SZ CR5，N，O，Sn 0至4 R1氢，硝基，氰基，卤素; 烷基，烷氧基，卤代烷基，卤代烷氧基或烷硫基，或当n为2,3或4时，两个相邻的取代基R1可以一起表示可被取代的1,3-丁二烯-1,4-二基; R2烷基; 卤代烷基，卤素，氰基，硝基，烷氧基羰基，二甲基氨基，R2另外表示氢; R3氢; 取代或未取代的烷基; 取代或未取代的环状结构，除了碳原子外，还可含有一至三个杂原子; 或取代或未取代的芳族体系，除了碳原子外，还可以含有一至四个氮原子和一至三个杂原子; R4，R5氢原子，烷基; 卤代烷基，卤素，氰基，硝基，二甲基氨基，烷氧基羰基，农药和含有这些化合物的杀真菌剂。

39. 发明授权

US5391743A Quaternary nitrogen-containing phosphonate compounds, pharmaceutical compositions, and methods of treating abnormal calcium and phosphate metabolism and methods of treating and preventing dental calculus and plaque 失效
标题翻译：第四纪含氮膦酸酯化合物，药物组合物和治疗异常钙和磷酸盐代谢的方法及治疗和预防牙垢和斑块的方法
公开(公告)号：US5391743A
公开(公告)日：1995-02-21
申请号：US52695
申请日：1993-04-30
申请人： Frank H. Ebetino , Susan M. Kaas , Marion D. Francis , Dennis G. A. Nelson , John M. Janusz
发明人： Frank H. Ebetino , Susan M. Kaas , Marion D. Francis , Dennis G. A. Nelson , John M. Janusz
IPC分类号： C07F9/38 , C07F9/553 , C07F9/572 , C07F9/576 , C07F9/58 , C07F9/59 , C07F9/6506 , C07F9/6512 , C07F9/6561 , C07D211/92 , C07D213/72 , C07D213/74 , C07D211/94
CPC分类号： C07F9/6561 , C07F9/3808 , C07F9/3873 , C07F9/5532 , C07F9/5721 , C07F9/5722 , C07F9/5765 , C07F9/582 , C07F9/588 , C07F9/592 , C07F9/598 , C07F9/65061 , C07F9/65062 , C07F9/65127
摘要： The present invention relates to quaternary nitrogen-containing phosphonate compounds, and the pharmaceutically-acceptable salts and esters thereof and having the general structure: ##STR1## wherein R.sup.1, R.sup.2, R.sup.5 and R.sup.8 are defined in claim 1, m and n are integers from 0 to 10; m+n is from 0 to 10;Z is a saturated, unsaturated, or aromatic, monocyclic or polycyclic carbocycle or monocyclic or polycyclic heterocycle containing one or more heteroatoms selected from O, S, or N, wherein at least one heteroatom is a quaternary nitrogen atom;R is COOH; PO.sub.3 H.sub.2 ; SO.sub.3 H; or P(O)(OH)R.sub.4, wherein R.sub.4 is substituted or unsubstituted alkyl of 1-8 carbon atoms;The present invention further relates to pharmaceutical compositions containing a safe and effective amount of a compound of the present invention, and pharmaceutically-acceptable excipients. Finally, the present invention relates to methods for treating or preventing pathological conditions characterized by abnormal calcium and phosphate metabolism such as osteoporosis, rheumatoid arthritis, and osteoarthritis in humans or other mammals and to methods for treating or preventing dental calculus, plaque and gingivitis.
摘要翻译：本发明涉及含季氮的膦酸酯化合物及其药学上可接受的盐和酯，并具有以下一般结构：其中R 1，R 2，R 5和R 8如权利要求1中所定义，m和n为 0至10; m + n为0〜10; Z是含有一个或多个选自O，S或N的杂原子的饱和，不饱和或芳族单环或多环碳环或单环或多环杂环，其中至少一个杂原子是季氮原子; R为COOH; PO3H2; SO3H; 或P（O）（OH）R 4，其中R 4是取代或未取代的1-8个碳原子的烷基; 本发明还涉及含有安全有效量的本发明化合物和药学上可接受的赋形剂的药物组合物。最后，本发明涉及用于治疗或预防以人或其他哺乳动物为骨质疏松症，类风湿性关节炎和骨关节炎等异常钙和磷酸盐代谢特征的病理状态的方法以及治疗或预防牙结石，斑块和牙龈炎的方法。

40. 发明授权

US5244857A Diphosphines containing silane groups, immobilise diphosphines and the use thereof as hydrogenation catalysts 失效
标题翻译：含有硅烷基团的二羟基磷灰石，硫化二磷酸酯及其作为氢化催化剂的用途
公开(公告)号：US5244857A
公开(公告)日：1993-09-14
申请号：US823517
申请日：1992-01-21
申请人： Benoit Pugin , Manfred Muller , Felix Spindler
发明人： Benoit Pugin , Manfred Muller , Felix Spindler
IPC分类号： B01J31/02 , B01J31/16 , B01J31/22 , B01J31/24 , C07C29/145 , C07F9/572 , C07F15/00
CPC分类号： C07F15/008 , B01J31/1633 , B01J31/2291 , B01J31/2409 , C07F15/004 , C07F9/5722 , C07F9/5726 , B01J2231/643 , B01J2231/645 , B01J2531/822 , B01J2531/827 , Y02P20/588
摘要： Compounds of formula II ##STR1## wherein the groups (R.sub.1).sub.2 P(CH.sub.2).sub.m and n are in o- or m-position to each other and the substituents R.sub.1 are identical or different radicals, m and n are each independently of the other 0 or 1, R.sub.1 is linear or branched C.sub.1 -C.sub.12 alkyl, unsubstituted C.sub.5 -C.sub.6 cycloalkyl or C.sub.5 -C.sub.6 cycloalkyl which is substituted by C.sub.1 -C.sub.4 alkyl or C.sub.1 -C.sub.4 alkoxy, or is phenyl or benzyl, or both substituents R.sub.1 in a group (R.sub.1).sub.2 P together are o,o'-diphenylene, --R.sub.2 --X-- is a bond or --(C.sub.x H.sub.2x --O).sub.y --, or X-- is O-- and R.sub.2 is C.sub.1 -C.sub.6 alkylene, x is an integer from 2 to 6 and y is an integer from 2 to 6, R.sub.3 is C.sub.2 -C.sub.18 alkylene, phenylene or benzylene, and R.sub.4 is C.sub.1 -C.sub.6 alkyl or phenyl, can be applied to solid carriers, such as silica gel or aerosils, and complexed with rhodium or iridium compounds. These materials are heterogeneous and separable catalysts for the asymmetrical hydrogenation of prochiral compounds containing carbon double bonds or carbon/hetero atom double bonds, for example ketones and imines.
摘要翻译：式（II）化合物其中基团（R 1）2 P（CH 2）m和n彼此相邻或相邻位置，并且取代基R 1是相同或不同的基团，m和n各自独立地为的另一个0或1，R 1是被C 1 -C 4烷基或C 1 -C 4烷氧基取代的直链或支链C 1 -C 12烷基，未取代的C 5 -C 6环烷基或C 5 -C 6环烷基，或是苯基或苄基，或两个取代基R 1 R1）2P一起是o，o'-二亚苯基，-R 2 -X-是键或 - （C x H 2 O-O）y - ，或X是O-，R 2是C 1 -C 6亚烷基，x是从2到 6，y为2〜6的整数，R3为C2-C18亚烷基，亚苯基或亚苯基，R4为C1-C6烷基或苯基，可用于固体载体如硅胶或气溶胶，并与铑或铱络合化合物。这些材料是用于不对称氢化含有双键或碳/杂原子双键的前手性化合物的非均相和可分离的催化剂，例如酮和亚胺。

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