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1. 发明授权

US5958905A Phosphoramidates, phosphinic amides and related compounds and the use thereof to modulate the activity of endothelin 失效
标题翻译：磷酰胺化物，次膦酰胺和相关化合物及其用于调节内皮素活性的用途
公开(公告)号：US5958905A
公开(公告)日：1999-09-28
申请号：US624706
申请日：1996-03-26
申请人： Ming Fai Chan , Erik Joel Verner
发明人： Ming Fai Chan , Erik Joel Verner
IPC分类号： A61K31/00 , A61K31/66 , A61K31/661 , A61K31/6615 , A61K31/664 , A61P1/00 , A61P9/00 , A61P9/10 , A61P9/12 , A61P11/00 , A61P11/06 , A61P11/08 , A61P13/12 , A61P15/00 , A61P17/02 , A61P27/02 , A61P29/00 , A61P37/06 , A61P43/00 , C07F9/24 , C07F9/44 , C07F9/6509 , C07F9/6512 , C07F9/653 , C07F9/6539 , A61K31/42 , C07D261/14
CPC分类号： C07F9/650941 , C07F9/247 , C07F9/65127 , C07F9/653
摘要： Phosphoramidates and phosphinic amides and related compounds are provided. Also provided are methods that use the compounds for modulating the activity of the endothelin family of peptides are provided. In particular, compounds having formula: ##STR1## in which A, B, R.sup.1 and R.sup.2 are as described are provided. Also provided are methods for treating endothelin-mediated disorders by administering effective amounts of one or more of these compounds or prodrugs thereof. Methods for elucidating the physiological and pathophysiological roles of endothelin, as well as isolating endothelin receptors are also provided.
摘要翻译：提供了磷酰胺化物和次膦酰胺和相关化合物。还提供了使用化合物调节肽的内皮素家族的活性的方法。特别地，提供了具有下式的化合物：其中A，B，R 1和R 2如上所述。还提供了通过施用有效量的一种或多种这些化合物或其前药来治疗内皮素介导的病症的方法。还提供了阐明内皮素的生理和病理生理学作用以及分离内皮素受体的方法。

2. 发明授权

US5334586A Heterocycle-substituted diphosphonate compounds, pharmaceutical compositions, and methods of treating abnormal calcium and phosphate metabolism 失效
标题翻译：杂环取代的二膦酸盐化合物，药物组合物和治疗异常钙和磷酸盐代谢的方法
公开(公告)号：US5334586A
公开(公告)日：1994-08-02
申请号：US779705
申请日：1991-10-21
申请人： Frank H. Ebetino , James J. Benedict
发明人： Frank H. Ebetino , James J. Benedict
IPC分类号： C07F9/59 , C07F9/6509 , C07F9/6512 , C07F9/6521 , A61K31/675
CPC分类号： C07F9/65122 , C07F9/592 , C07F9/598 , C07F9/650917 , C07F9/650941 , C07F9/650964 , C07F9/650988 , C07F9/65127 , C07F9/65212 , C07F9/65217
摘要： The present invention relates to novel heterocycle-substituted diphosphonic acids, and the pharmaceutically-acceptable salts and esters thereof, in which the diphosphonate-substituted carbon atom moiety is attached to a carbon atom in a nitrogen-containing six membered ring heterocycle, preferably a piperidine ring. The heterocycle-substituted diphosphonic acid compounds have the general structure: ##STR1## wherein Z is a nitrogen-containing six membered ring heterocycle moiety selected from piperidinyl, diazinyl and triazinyl; m, n and m+n are from 0 to 10; Q is a covalent bond or a moiety selected from oxygen, sulfur or nitrogen; and R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are substituent groups.The present invention further relates to pharmaceutical compositions containing these novel compounds. Finally this invention relates to methods for treating or preventing diseases characterized by abnormal calcium and phosphate metabolism by utilizing a compound or pharmaceutical composition of the present invention.
摘要翻译：本发明涉及新颖的杂环取代二膦酸及其药学上可接受的盐和酯，其中二膦酸酯取代的碳原子部分连接到含氮六元环杂环中的碳原子上，优选哌啶环。杂环取代的二膦酸化合物具有以下一般结构：其中Z是选自哌啶基，二嗪基和三嗪基的含氮六元环杂环部分。 m，n和m + n为0〜10; Q是共价键或选自氧，硫或氮的部分; 并且R1，R2，R3和R4是取代基。本发明还涉及含有这些新化合物的药物组合物。最后本发明涉及利用本发明的化合物或药物组合物治疗或预防以异常钙和磷酸盐代谢为特征的疾病的方法。

3. 发明授权

US5824679A Phosphanoxides--preparation and use 失效
标题翻译：磷氧化物 - 制备和使用
公开(公告)号：US5824679A
公开(公告)日：1998-10-20
申请号：US793446
申请日：1997-02-28
申请人： Wolfgang Von Der Saal , Herbert Leinert , Karlheinz Stegmeier
发明人： Wolfgang Von Der Saal , Herbert Leinert , Karlheinz Stegmeier
IPC分类号： A61K31/675 , A61P7/02 , C07F9/53 , C07F9/58 , C07F9/6509 , A61K31/535 , A01N43/58 , C07D401/00 , C07D211/68
CPC分类号： C07F9/650941 , C07F9/5304 , C07F9/588
摘要： The invention concerns novel phosphanoxides of formula 1 in which R.sup.1 means aryl or heteroaryl group. The invention further concern the optically active forms, racemates and diastereomers mixtures of these compounds, a method of preparing them and pharmaceutical compositions containing these compounds, and methods of use to produce a thrombin-inhibiting effect.
摘要翻译： PCT No.PCT / EP95 / 03382 Sec。 371日期1997年2月28日 102（e）日期1997年2月28日PCT 1995年8月26日PCT PCT。公开号WO96 / 06849 日期1996年3月7日本发明涉及式1的新型氧膦化物，其中R 1表示芳基或杂芳基。本发明还涉及这些化合物的光学活性形式，外消旋体和非对映体混合物，其制备方法和含有这些化合物的药物组合物，以及用于产生凝血酶抑制作用的方法。

4. 发明授权

US5563268A Heterobiaryl derivatives 失效
标题翻译：异二醇衍生物
公开(公告)号：US5563268A
公开(公告)日：1996-10-08
申请号：US375084
申请日：1995-01-19
申请人： Guenter Linz , Helmut Pieper , Frank Himmelsbach , Volkhard Austel , Thomas Mueller , Johannes Weisenberger , Elke Seewaldt-Becker
发明人： Guenter Linz , Helmut Pieper , Frank Himmelsbach , Volkhard Austel , Thomas Mueller , Johannes Weisenberger , Elke Seewaldt-Becker
IPC分类号： A61K31/44 , A61K31/4402 , A61K31/4406 , A61K31/4409 , A61K31/4418 , A61K31/4425 , A61K31/4427 , A61K31/445 , A61K31/495 , A61K31/50 , A61K31/505 , A61P7/02 , A61P29/00 , A61P35/00 , C07D213/75 , C07D213/81 , C07D237/14 , C07D237/20 , C07D237/24 , C07D239/28 , C07D239/34 , C07D239/36 , C07D241/20 , C07D401/06 , C07D401/12 , C07D417/12 , C07F9/40 , C07F9/6509 , C07D403/02
CPC分类号： C07D239/36 , C07D237/14 , C07D237/20 , C07D237/24 , C07D401/06 , C07D401/12 , C07F9/650941
摘要： Heterobiaryl derivatives of the formulaR.sub.1 NH--X.sub.1 --X.sub.2 --X.sub.3 --Y.sub.1 --Y.sub.2 --Y.sub.3 --Y.sub.4 --E (I)whereinR.sub.1, X.sub.1 to X.sub.3 and Y.sub.1 to Y.sub.4 are as defined herein, the tautomers, stereoisomers and mixtures thereof, and the salts, particularly the physiologically acceptable salts, thereof with organic or inorganic acids or bases. The derivatives have valuable pharmacological properties, such as inhibiting cell-cell aggregation and cell-matrix interactions.
摘要翻译：式R1NH-X1-X2-X3-Y1-Y2-Y3-Y4-E（Ⅰ）的杂芳基衍生物其中R1，X1至X3和Y1至Y4如本文所定义，互变异构体，立体异构体及其混合物，以及盐，特别是其生理上可接受的盐与有机或无机酸或碱反应。该衍生物具有有价值的药理学性质，例如抑制细胞 - 细胞聚集和细胞 - 基质相互作用。

5. 发明授权

US5418233A Heterobiarly derivatives and pharmaceutical compositions thereof 失效
标题翻译：异源性衍生物及其药物组合物
公开(公告)号：US5418233A
公开(公告)日：1995-05-23
申请号：US961135
申请日：1992-10-14
申请人： Guenter Linz , Helmut Pieper , Frank Himmelsbach , Austel: Volkhard , Thomas Mueller , Johannes Weisenberger , Elke Seewaldt-Becker
发明人： Guenter Linz , Helmut Pieper , Frank Himmelsbach , Austel: Volkhard , Thomas Mueller , Johannes Weisenberger , Elke Seewaldt-Becker
IPC分类号： A61K31/44 , A61K31/4402 , A61K31/4406 , A61K31/4409 , A61K31/4418 , A61K31/4425 , A61K31/4427 , A61K31/445 , A61K31/495 , A61K31/50 , A61K31/505 , A61P7/02 , A61P29/00 , A61P35/00 , C07D213/75 , C07D213/81 , C07D237/14 , C07D237/20 , C07D237/24 , C07D239/28 , C07D239/34 , C07D239/36 , C07D241/20 , C07D401/06 , C07D401/12 , C07D417/12 , C07F9/40 , C07F9/6509
CPC分类号： C07D239/36 , C07D237/14 , C07D237/20 , C07D237/24 , C07D401/06 , C07D401/12 , C07F9/650941
摘要： Heterobiaryl derivatives of the formulaR.sub.1 NH--X.sub.1 --X.sub.2 --X.sub.3 --Y.sub.1 --Y.sub.2 --Y.sub.3 --Y.sub.4 --E (I)whereinR.sub.1, X.sub.1 to X.sub.3 and Y.sub.1 to Y.sub.4 are as defined herein, the tautomers, stereoisomers and mixtures thereof, and the salts, particularly the physiologically acceptable salts, thereof with organic or inorganic acids or bases. The derivatives have valuable pharmacological properties, such as inhibiting cell-cell aggregation and cell-matrix interactions.
摘要翻译：式R1NH-X1-X2-X3-Y1-Y2-Y3-Y4-E（Ⅰ）的杂芳基衍生物其中R1，X1至X3和Y1至Y4如本文所定义，互变异构体，立体异构体及其混合物，以及盐，特别是其生理上可接受的盐与有机或无机酸或碱反应。该衍生物具有有价值的药理学性质，例如抑制细胞 - 细胞聚集和细胞 - 基质相互作用。

6. 发明授权

US5071840A Certain heterocyclic substituted diphosphonate compounds pharmaceutical compositions, and methods of treating abnormal calcium and phosphate metabolism 失效
标题翻译：某些杂环取代的二膦酸盐化合物药物组合物，以及治疗异常钙和磷酸盐代谢的方法
公开(公告)号：US5071840A
公开(公告)日：1991-12-10
申请号：US378530
申请日：1989-07-11
申请人： Frank H. Ebetino , James J. Benedict
发明人： Frank H. Ebetino , James J. Benedict
IPC分类号： C07F9/59 , C07F9/6509 , C07F9/6512 , C07F9/6521
CPC分类号： C07F9/65122 , C07F9/592 , C07F9/598 , C07F9/650917 , C07F9/650941 , C07F9/650964 , C07F9/650988 , C07F9/65127 , C07F9/65212 , C07F9/65217
摘要： The present invention relates to novel heterocycle-substituted diphosphonic acids, and the pharmaceutically-acceptable salts and esters thereof, in which the diphosphonate-substituted carbon atom moiety is attached to a carbon atom in a nitrogen-containing six membered ring heterocycle, preferably a piperidine ring. The heterocycle-substituted diphosphonic acid compounds have the general structure: ##STR1## wherein Z is a nitrogen-containing six membered ring heterocycle moiety selected from piperidinyl, diazinyl and triazinyl; m, n and m+n are from 0 to 10; Q is a covalent bond or a moiety selected from oxygen, sulfur or nitrogen; and R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are substituent groups.The present invention further relates to pharmaceutical compositions containing these novel compounds. Finally this invention relates to methods for treating or preventing diseases characterized by abnormal calcium and phosphate metabolism by utilizing a compound or pharmaceutical composition of the present invention.
摘要翻译：本发明涉及新颖的杂环取代二膦酸及其药学上可接受的盐和酯，其中二膦酸酯取代的碳原子部分连接到含氮六元环杂环中的碳原子上，优选哌啶环。杂环取代的二膦酸化合物具有以下一般结构：其中Z是选自哌啶基，二嗪基和三嗪基的含氮六元环杂环部分。 m，n和m + n为0〜10; Q是共价键或选自氧，硫或氮的部分; 并且R1，R2，R3和R4是取代基。本发明还涉及含有这些新化合物的药物组合物。最后本发明涉及利用本发明的化合物或药物组合物治疗或预防以异常钙和磷酸盐代谢为特征的疾病的方法。

7. 发明授权

US3907541A Pyridazonylphosphoric acid derivatives as herbicides 失效
标题翻译：哒嗪基磷酸衍生物作为除草剂
公开(公告)号：US3907541A
公开(公告)日：1975-09-23
申请号：US50962874
申请日：1974-09-26
申请人： CIBA GEIGY CORP
发明人： BADER JORG , BADER-LUDWIG LEGAL REPRESENTAT
IPC分类号： C07F9/6509 , A01N9/36
CPC分类号： C07F9/650941
摘要： Phosphoric and thiophosphoric-diester-N-(1-phenyl-5-halogeno6(1H)-pyridazonyl-(4))-amides possess selective herbicidal properties. They can be used for combating grass-like and dicotyledonous weeds in useful plants.
摘要翻译：磷和硫代磷酸二酯-N- [1-苯基-5-卤代-6（1H） - 哒嗪基 - （4）] - 化合物具有选择性除草性质。它们可用于在有用的植物中对抗草和双子叶杂草。

8. 发明申请

WO2004096287A2 INOSINE MONOPHOSPHATE DEHYDROGENASE INHIBITORY PHOSPHONATE COMPOUNDS 审中-公开
标题翻译：单磷酸脱氢酶抑制性磷酸酯化合物
公开(公告)号：WO2004096287A2
公开(公告)日：2004-11-11
申请号：PCT/US2004/013064
申请日：2004-04-26
申请人： GILEAD SCIENCES, INC. , CANNIZZARO, Carina, E. , CHEN, James, M. , CHEN, Xiaowu , CHO, Aesop , CHONG, Lee, S. , FARDIS, Maria , KIRSCHBERG, Thorsten, A. , PYUN, Hyung-Jung , WATKINS, Will , ZHANG, Jennifer, R.
发明人： CANNIZZARO, Carina, E. , CHEN, James, M. , CHEN, Xiaowu , CHO, Aesop , CHONG, Lee, S. , FARDIS, Maria , KIRSCHBERG, Thorsten, A. , PYUN, Hyung-Jung , WATKINS, Will , ZHANG, Jennifer, R.
IPC分类号： A61K47/48
CPC分类号： C07F9/4075 , A61K31/662 , A61K47/548 , C07D205/04 , C07D211/58 , C07D409/06 , C07D409/14 , C07D413/14 , C07D475/00 , C07F9/5728 , C07F9/582 , C07F9/588 , C07F9/60 , C07F9/65037 , C07F9/650941 , C07F9/653 , C07F9/6539 , C07F9/65515 , C07F9/655354 , C07F9/6561
摘要： The invention is related to phosphorus substituted IMPDH inhibitory compounds, compositions containing such compounds, and therapeutic methods that include the administration of such compounds, as well as to processes and intermediates useful for preparing such compounds.
摘要翻译：本发明涉及磷取代的IMPDH抑制化合物，含有这些化合物的组合物，以及包括施用这些化合物的治疗方法以及可用于制备这些化合物的方法和中间体。

9. 发明授权

US5519013A Heterocycle-substituted diphosphonate compounds, pharmaceutical compositions, and methods of treating abnormal calcium and phosphate metabolism 失效
标题翻译：杂环取代的二膦酸盐化合物，药物组合物和治疗异常钙和磷酸盐代谢的方法
公开(公告)号：US5519013A
公开(公告)日：1996-05-21
申请号：US224615
申请日：1994-04-07
申请人： Frank H. Ebetino , James J. Benedict
发明人： Frank H. Ebetino , James J. Benedict
IPC分类号： C07F9/59 , C07F9/6509 , C07F9/6512 , C07F9/6521 , A61K31/675
CPC分类号： C07F9/65122 , C07F9/592 , C07F9/598 , C07F9/650917 , C07F9/650941 , C07F9/650964 , C07F9/650988 , C07F9/65127 , C07F9/65212 , C07F9/65217
摘要： The present invention relates to novel heterocycle-substituted diphosphonic acids, and the pharmaceutically-acceptable salts and esters thereof, in which the diphosphonate-substituted carbon atom moiety is attached to a carbon atom in a nitrogen-containing six membered ring heterocycle, preferably a piperidine ring. The heterocycle-substituted diphosphonic acid compounds have the general structure: ##STR1## wherein Z is a nitrogen-containing six membered ring heterocycle moiety selected from piperidinyl, diazinyl and triazinyl; m, n and m+n are from 0 to 10; Q is a covalent bond or a moiety selected from oxygen, sulfur or nitrogen; and R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are substituent groups.The present invention further relates to pharmaceutical compositions containing these novel compounds. Finally this invention relates to methods for treating or preventing diseases characterized by abnormal calcium and phosphate metabolism by utilizing a compound or pharmaceutical composition of the present invention.
摘要翻译：本发明涉及新颖的杂环取代二膦酸及其药学上可接受的盐和酯，其中二膦酸酯取代的碳原子部分连接到含氮六元环杂环中的碳原子上，优选哌啶环。杂环取代的二膦酸化合物具有以下一般结构：其中Z是选自哌啶基，二嗪基和三嗪基的含氮六元环杂环部分。 m，n和m + n为0〜10; Q是共价键或选自氧，硫或氮的部分; 并且R1，R2，R3和R4是取代基。本发明还涉及含有这些新化合物的药物组合物。最后本发明涉及利用本发明的化合物或药物组合物治疗或预防以异常钙和磷酸盐代谢为特征的疾病的方法。

10. 发明授权

US3879189A Control of weeds with 1-phenyl-4-phosphoranylideneamino-5-halo-6(1H)-pyridazones 失效
标题翻译：用1-苯基-4-亚正膦基氨基-5-卤代-6（1H） - 哒嗪酮控制杂草
公开(公告)号：US3879189A
公开(公告)日：1975-04-22
申请号：US46632974
申请日：1974-05-02
申请人： CIBA GEIGY CORP
发明人： BADER JOERG , VOGEL CHRISTIAN
IPC分类号： C07F9/6509 , A01N9/36
CPC分类号： C07F9/650941
摘要： WHEREIN R1 and R2 independently represent alkoxy, alkenyloxy, alkoxyalkoxy, alkylthio or both together with the phosphorus atom from a five- or six-membered ring containing at least one other hetero atom, R3 is alkoxy, alkenyloxy, alkoxyalkoxy, alkylthio or dialkylamino, R4 and R5 are hydrogen, halogen, lower alkyl, alkoxy or halogenalkyl, X being chlorine or bromine. Preferably the three radicals R1, R2, R3 are identical and represent lower alkoxy and R4 and R5 are hydrogen. There is also provided an agent for the control of weeds comprising the said pyridazone derivatives as active component. The new compounds are especially useful as selective herbicides in cultivated crops.
The invention is concerned with new pyridazone derivatives of formula
摘要翻译：本发明涉及式WHERE R1的新的哒唑衍生物，R 1和R 2独立地表示烷氧基，链烯氧基，烷氧基烷氧基，烷硫基或两者与含有至少一个其它杂原子的五元或六元环的磷原子，R3是烷氧基，烯氧基，烷氧基烷氧基，烷硫基或二烷基氨基，R4和R5是氢，卤素，低级烷基，烷氧基或卤代烷基，X是氯或溴。优选地，三个基团R 1，R 2，R 3相同并且表示低级烷氧基，并且R 4和R 5是氢。还提供了用于控制杂草的试剂，其包含所述哒嗪衍生物作为活性成分。新化合物特别适用于栽培作物中的选择性除草剂。

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