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1. 发明授权

US5190933A Substituted propane-phosphinic acid compounds 失效
标题翻译：取代的丙烷 - 次膦酸化合物
公开(公告)号：US5190933A
公开(公告)日：1993-03-02
申请号：US845871
申请日：1992-03-03
申请人： Eric K. Baylis , Ludwig Maier , Stuart J. Mickel , Hans-Rudolf Olpe , Helmut Bittiger , Wolfgang Frostl , Roger G. Hall
发明人： Eric K. Baylis , Ludwig Maier , Stuart J. Mickel , Hans-Rudolf Olpe , Helmut Bittiger , Wolfgang Frostl , Roger G. Hall
IPC分类号： C07F9/30 , C07F9/48
CPC分类号： C07F9/48 , C07F9/301 , Y02P20/55
摘要： Compounds of the formula I ##STR1## wherein R denotes an aliphatic, cycloaliphatic, cycloaliphatic-aliphatic or araliphatic radical having 2 or more carbon atoms, and wherein one of the groups R.sup.1, R.sup.2 and R.sup.3 represents hydrogen or an aliphatic, cycloaliphatic, araliphatic or aromatic radical, another one of R.sup.1, R.sup.2 and R.sup.3 is hydrogen or, in the case of R.sup.1 and R.sup.2, is hydroxy, and the remaining one of R.sup.1, R.sup.2 and R.sup.3 is hydrogen, or wherein R denotes methyl, R.sub.1 denotes hydrogen or hydroxy, R.sub.2 denotes an aromatic radical and R.sub.3 represents hydrogen, and their salts have GABA.sub.B -antagonistic properties and can be used as GABA.sub.B -antagonists. They are obtained when in a compound of formula II ##STR2## in which R, R.sup.1, R.sup.2 and R.sup.3 have their previous significances, Z represents --NH.sub.2 and R.sup.4 denotes a hydroxy-protective group R.sup.5 or, when R.sup.1 and R.sup.3 denote hydrogen and R.sup.2 denotes hydrogen or alkyl, denotes an alkali metal or ammonium ion R.sup.6, or Z represents a protected or latent amino group Z.sup.o and R.sup.4 denotes hydrogen or a hydroxy-protective group R.sup.5, any group R.sup.5 or R.sup.6 is replaced by hydrogen, and/or any group Z.sup.o is converted into --NH.sub.2.
摘要翻译：式I的化合物（I）其中R表示具有2个或更多个碳原子的脂族，脂环族，脂环族 - 脂族或芳脂族基团，其中R1，R2和R3中的一个表示氢或脂族，脂环族，芳脂族或芳族基团，R 1，R 2和R 3中的另一个为氢，或在R 1和R 2的情况下为羟基，其余的R 1，R 2和R 3为氢，或其中R为甲基，R 1为氢或羟基，R 2表示芳族基团，R 3表示氢，并且它们的盐具有GABAB拮抗性质，可用作GABAB-拮抗剂。当其中R，R 1，R 2和R 3具有其先前含义的式II化合物（II）时，它们是得到的，Z表示-NH 2，R4表示羟基保护基R5，或者当R1和R3表示氢和R2表示氢或烷基，表示碱金属或铵离子R6，或Z表示保护或潜在氨基Zo，R4表示氢或羟基保护基R5，任何基团R5或R6被氢代替，以及 /或任何基团Zo被转化为-NH 2。

2. 发明授权

US5064819A Substituted propane-phosphinic acid compounds 失效
标题翻译：取代的丙酸 - 磷酸化合物
公开(公告)号：US5064819A
公开(公告)日：1991-11-12
申请号：US502399
申请日：1990-03-30
申请人： Eric K. Baylis , Helmut Bittiger , Wolfgang Frostl , Roger G. Hall , Ludwig Maier , Stuart J. Mickel , Hans-Rudolf Olpe
发明人： Eric K. Baylis , Helmut Bittiger , Wolfgang Frostl , Roger G. Hall , Ludwig Maier , Stuart J. Mickel , Hans-Rudolf Olpe
IPC分类号： A61K31/66 , A61P25/20 , A61P25/24 , A61P25/26 , A61P25/28 , A61P39/02 , A61P43/00 , C07F9/30 , C07F9/48
CPC分类号： C07F9/48 , C07F9/301 , Y02P20/55
摘要： Compounds of the formula I ##STR1## wherein R denotes an aliphatic, cycloaliphatic, cycloaliphatic-aliphatic or araliphatic radical having 2 or more carbon atoms, and wherein one of the groups R.sup.1, R.sup.2 and R.sup.3 represents hydrogen or an aliphatic, cycloaliphatic, araliphatic or aromatic radical, another one of R.sup.1, R.sup.2 and R.sup.3 is hydrogen or, in the case of R.sup.1 and R.sup.2, is hydroxy, and the remaining one of R.sup.1, R.sup.2 and R.sup.3 is hydrogen, or wherein R denotes methyl, R.sub.1 denotes hydrogen or hydroxy, R.sub.2 denotes an aromatic radical and R.sub.3 represents hydrogen, and their salts have GABA.sub.B -antagonistic properties and can be used as GABA.sub.B -antagonists. They are obtained when in a compound of formula II ##STR2## in which R, R.sup.1, R.sup.2 and R.sup.3 have their previous significances, Z represents --NH.sub.2 and R.sup.4 denotes a hydroxy-protective group R.sup.5 or, when R.sup.1 and R.sup.3 denote hydrogen and R.sup.2 denotes hydrogen or alkyl, denotes an alkali metal or ammonium ion R.sup.6, or Z represents a protected or latent amino group Z.sup.0 and R.sup.4 denotes hydrogen or a hydroxy-protective group R.sup.5, any group R.sup.5 or R.sup.6 is replaced by hydrogen, and/or any group Z.sup.0 is converted into --NH.sub.2.

3. 发明授权

US5300679A Substituted propane-phosphinic acid compounds 失效
标题翻译：取代的丙烷 - 次膦酸化合物
公开(公告)号：US5300679A
公开(公告)日：1994-04-05
申请号：US968101
申请日：1992-10-29
申请人： Eric K. Baylis , Helmut Bittiger , Wolfgang Frostl , Roger G. Hall , Ludwig Maier , Stuart J. Mickel , Hans-Rudolf Olpe
发明人： Eric K. Baylis , Helmut Bittiger , Wolfgang Frostl , Roger G. Hall , Ludwig Maier , Stuart J. Mickel , Hans-Rudolf Olpe
IPC分类号： C07F9/30 , C07F9/48 , A61K31/13 , A61K31/185
CPC分类号： C07F9/301 , C07F9/48 , Y02P20/55
摘要： Compounds of the formula I ##STR1## wherein R denotes an aliphatic, cycloaliphatic, cycloaliphatic-aliphatic or araliphatic radical having 2 or more carbon atoms, and wherein one of the groups R.sup.1, R.sup.2 and R.sup.3 represents hydrogen or an aliphatic, cycloaliphatic, araliphatic or aromatic radical, another one of R.sup.1, R.sup.2 and R.sup.3 is hydrogen or, in the case of R.sup.1 and R.sup.2, is hydroxy, and the remaining one of R.sup.1, R.sup.2 and R.sup.3 is hydrogen, or wherein R denotes methyl, R.sub.1 denotes hydrogen or hydroxy, R.sub.2 denotes an aromatic radical and R.sub.3 represents hydrogen, and their salts have GABA.sub.B -antagonistic properties and can be used as GABA.sub.B -antagonists. They are obtained when in a compound of formula II ##STR2## in which R, R.sup.1, R.sup.2 and R.sup.3 have their previous significances, Z represents --NH.sub.2 and R.sup.4 denotes a hydroxy-protective group R.sup.5 or, when R.sup.1 and R.sup.3 denote hydrogen and R.sup.2 denotes hydrogen or alkyl, denotes an alkali metal or ammonium ion R.sup.6, or Z represents a protected or latent amino group Z.sup.o and R.sup.4 denotes hydrogen or a hydroxy-protective group R.sup.5, any group R.sup.5 or R.sup.6 is replaced by hydrogen, and/or any group Z.sup.o is converted into --NH.sub.2.
摘要翻译：式I的化合物（I）其中R表示具有2个或更多个碳原子的脂族，脂环族，脂环族 - 脂族或芳脂族基团，其中R1，R2和R3中的一个表示氢或脂族，脂环族，芳脂族或芳族基团，R 1，R 2和R 3中的另一个为氢，或在R 1和R 2的情况下为羟基，其余的R 1，R 2和R 3为氢，或其中R为甲基，R 1为氢或羟基，R 2表示芳族基团，R 3表示氢，并且它们的盐具有GABAB拮抗性质，可用作GABAB-拮抗剂。当其中R，R 1，R 2和R 3具有其先前含义的式II化合物（II）时，它们是得到的，Z表示-NH 2，R4表示羟基保护基R5，或者当R1和R3表示氢和R2表示氢或烷基，表示碱金属或铵离子R6，或Z表示保护或潜在氨基Zo，R4表示氢或羟基保护基R5，任何基团R5或R6被氢代替，以及 /或任何基团Zo被转化为-NH 2。

4. 发明授权

US5051524A Substituted propane-phosphinic acid compounds 失效
公开(公告)号：US5051524A
公开(公告)日：1991-09-24
申请号：US484716
申请日：1990-02-26
申请人： Eric K. Baylis , Helmut Bittiger , Wolfgang Frostl , Roger G. Hall , Ludwig Maier , Stuart J. Mickel , Hans-Rudolf Olpe
发明人： Eric K. Baylis , Helmut Bittiger , Wolfgang Frostl , Roger G. Hall , Ludwig Maier , Stuart J. Mickel , Hans-Rudolf Olpe
IPC分类号： A61K31/66 , A61P25/20 , A61P25/24 , A61P25/26 , A61P25/28 , A61P39/02 , A61P43/00 , C07F9/30 , C07F9/48
CPC分类号： C07F9/48 , C07F9/301 , Y02P20/55
摘要： Compounds of the formula I ##STR1## wherein R denotes an aliphatic, cycloaliphatic, cycloaliphatic-aliphatic or araliphatic radical having 2 or more carbon atoms, and wherein one of the groups R.sup.1, R.sup.2 and R.sup.3 represents hydrogen or an aliphatic, cycloaliphatic, araliphatic or aromatic radical, another one of R.sup.1, R.sup.2 and R.sup.3 is hydrogen or, in the case of R.sup.1 and R.sup.2, is hydroxy, and the remaining one of R.sup.1, R.sup.2 and R.sup.3 is hydrogen, or wherein R denotes methyl, R.sub.1 denotes hydrogen or hydroxy, R.sub.2 denotes an aromatic radical and R.sub.3 represents hydrogen, and their salts have GABA.sub.B -antagonistic properties and can be used as GABA.sub.B -antagonists. They are obtained when in a compound of formula II ##STR2## in which R, R.sup.1, R.sup.2 and R.sup.3 have their previous significances, Z represents --NH.sub.2 and R.sup.4 denotes a hydroxy-protective group R.sup.5 or, when R.sup.1 and R.sup.3 denote hydrogen and R.sup.2 denotes hydrogen or alkyl, denotes an alkali metal or ammonium ion R.sup.6, or Z represents a protected or latent amino group Z.degree. and R.sup.4 denotes hydrogen or a hydroxy-protective group R.sup.5, any group R.sup.5 or R.sup.6 is replaced by hydrogen, and/or any group Z.degree. is converted into --NH.sub.2.

5. 发明授权

US5013863A Substituted propane-phosphinic acid compounds 失效
标题翻译：取代的丙烷 - 次膦酸化合物
公开(公告)号：US5013863A
公开(公告)日：1991-05-07
申请号：US378887
申请日：1989-07-12
申请人： Eric K. Baylis , Helmut Bittiger , Wolfgang Froostl , Roger G. Hall , Ludwig Maier , Stuart J. Mickel , Hans-Rudolf Olpe
发明人： Eric K. Baylis , Helmut Bittiger , Wolfgang Froostl , Roger G. Hall , Ludwig Maier , Stuart J. Mickel , Hans-Rudolf Olpe
IPC分类号： A61K31/66 , A61P25/20 , A61P25/24 , A61P25/26 , A61P25/28 , A61P39/02 , A61P43/00 , C07F9/30 , C07F9/48
CPC分类号： C07F9/48 , C07F9/301 , Y02P20/55
摘要： Compounds of the formula I ##STR1## wherein R denotes an aliphatic, cycloaliphatic, cycloaliphatic-aliphatic or araliphatic radical having 2 or more carbon atoms, and wherein one of the groups R.sup.1, R.sup.2 and R.sup.3 represents hydrogen or an aliphatic, cycloaliphatic, araliphatic or aromatic radical, another one of R.sup.1, R.sup.2 and R.sup.3 is hydrogen or, in the case of R.sup.1 and R.sup.2, is hydroxy, and the remaining one of R.sup.1, R.sup.2 and R.sup.3 is hydrogen, and their salts have GABA.sub.B -antagonistic properties and can be used as GABA.sub.B -antagonists. They are obtained when in a compound of formula II ##STR2## in which R, R.sup.1, R.sup.2 and R.sup.3 have their previous significances, Z represents --NH.sub.2 and R.sup.4 denotes a hydroxy-protective group R.sup.5 or, when R.sup.1 and R.sup.3 denote hydrogen and R.sup.2 denotes hydrogen or alkyl, denotes an alkali metal or ammonium ion R.sup.6, or Z represents a protected or latent amino group Z.sup.0 and R.sup.4 deontes hydrogen or a hydroxy-protective group R.sup.5, any group R.sup.5 or R.sup.6 is replaced by hydrogen, and/or any group Z.sup.0 is converted into --NH.sub.2.

6. 发明授权

US4147780A .alpha.-Amino-phosphonous acids for inhibiting bacteria and yeast 失效
标题翻译： {60 - 用于抑制细菌和酵母的氨基膦酸
公开(公告)号：US4147780A
公开(公告)日：1979-04-03
申请号：US799428
申请日：1977-05-23
申请人： John G. Dingwall , Eric K. Baylis , Colin D. Campbell
发明人： John G. Dingwall , Eric K. Baylis , Colin D. Campbell
IPC分类号： C07F9/30 , A61K31/66 , A61K31/665 , A61K31/67 , A61K31/675 , A61P31/00 , C07F9/48 , C07F9/572 , C07F9/58 , C07F9/655 , C07F9/6553
CPC分类号： C07F9/48 , A61K31/66 , C07F9/582
摘要： The present invention relates to new phosphonous acid derivatives, especially to .alpha.-amino-phosphonous acids and processes for their production. The new phosphonous acids are valuable chemotherapeutica in the treatment of pathogenic bacteria, gram-negative bacteria and yeast.
摘要翻译：本发明涉及新的膦酸衍生物，特别是涉及α-氨基膦酸及其生产方法。新型膦酸是治疗病原菌，革兰氏阴性细菌和酵母菌的重要化学治疗剂。

7. 发明授权

US4933478A Process for the manufacture of aliphatylphosphinic acid derivatives 失效
标题翻译：制备脂肪酰基次膦酸衍生物的方法
公开(公告)号：US4933478A
公开(公告)日：1990-06-12
申请号：US239233
申请日：1988-09-01
申请人： Peter S. Wardleworth , Eric K. Baylis
发明人： Peter S. Wardleworth , Eric K. Baylis
IPC分类号： C07F9/30 , C07B61/00 , C07F9/32 , C07F9/48
CPC分类号： C07F9/4816
摘要： A process for the production of aliphatylphosphinic acid derivatives, especially of alkyl dialkoxyalkylphosphinates having the formula I ##STR1## in which R is C.sub.1 -C.sub.4 -alkyl and R' is hydrogen or C.sub.1 -C.sub.4 -alkyl, comprising reacting, in the presence of an acidic catalyst, aqueous phosphonic acid with the corresponding trialkyl orthoester having the formula II:(RO).sub.3 CR' IIin whicih R and R' have their previous significances, the amount of the orthoester of formula II used being equal to, or in excess of the stoichiometric amount of both water and phosphinic acid present in the aqueous phosphinic acid reactant.
摘要翻译：一种制备脂肪酰基次膦酸衍生物的方法，特别是具有式I I烷基二烷氧基烷基次膦酸盐的方法，其中R是C 1 -C 4 - 烷基且R'是氢或C 1 -C 4烷基，包括在酸性催化剂，具有式II的相应三烷基原酸酯的水性膦酸：R和R'中的（RO）3CR'II具有以前的意义，所用式II的原酸酯的量等于或超过化学计算量存在于次膦酸水溶液中的水和次膦酸。

8. 发明授权

US4205977A Agent and method for influencing plant growth 失效
标题翻译：影响植物生长的代理和方法
公开(公告)号：US4205977A
公开(公告)日：1980-06-03
申请号：US960357
申请日：1978-11-13
申请人： John G. Dingwall , Eric K. Baylis , Colin D. Campbell
发明人： John G. Dingwall , Eric K. Baylis , Colin D. Campbell
IPC分类号： A01N57/20 , C07F9/38 , C07F9/40 , C07F9/48 , A01N5/00
CPC分类号： A01N57/20 , C07F9/4816
摘要： Agent for influencing plant growth, in particular a herbicidal and plant growth-inhibiting agent containing in addition to carriers and/or other additives, at least one compound of the formula: ##STR1## in which R is hydrogen an alkyl group having from 1 to 5C atoms, which is unsubstituted or substituted by hydroxyl, salts thereof with either strong monobasic or polybasic acids or with inorganic or organic bases, or optical isomers thereof, as the active component.
摘要翻译：用于影响植物生长的试剂，特别是含有载体和/或其它添加剂的除草和植物生长抑制剂，至少一种下式的化合物：其中R是氢，烷基具有1 至5原子，其为未取代的或被羟基取代的盐，其与强一元或多元酸的盐或与无机或有机碱或其光学异构体作为活性组分。

9. 发明授权

US4331591A Chemical process for the production of .alpha.-aminophosphonic acids and peptide derivatives 失效
标题翻译：用于生产α-氨基膦酸和肽衍生物的化学方法
公开(公告)号：US4331591A
公开(公告)日：1982-05-25
申请号：US080763
申请日：1979-10-01
申请人： Eric K. Baylis
发明人： Eric K. Baylis
IPC分类号： A01N57/18 , A61K31/66 , A61P31/04 , C07F9/38 , C07F9/547 , C07K5/04 , C07K5/08 , C07C103/52 , C07C9/02 , C07G7/00
CPC分类号： C07F9/3808 , C07K5/0827 , Y02P20/55
摘要： The present invention provides a process for the production of physiologically-useful .alpha.-aminophosphonic acids and peptide derivatives of the formula: ##STR1## wherein R and R.sub.1 may be the same or different and each can be hydrogen, deuterium or an optionally substituted lower alkyl group, lower alkenyl, lower alkynyl, cycloalkyl, aryl or heterocyclic radical containing one or more oxygen, nitrogen or sulphur atoms and which may be fused to an aromatic ring, a lower alkyl group substituted by a cycloalkyl radical, a lower alkyl group substituted by an aryl radical, a lower alkyl group substituted by a heterocyclic radical as defined above or R and R.sub.1 together form a polymethylene chain optionally interrupted by an oxygen, nitrogen or sulphur atom, or R.sub.1 represents, together with the C(R)--N
摘要翻译：本发明提供了一种制备下式的生理有用的α-氨基膦酸和肽衍生物的方法：其中R和R 1可以相同或不同，并且各自可以是氢，氘或任选取代的低级烷基，低级烯基，低级炔基，环烷基，芳基或杂环基，其含有一个或多个氧，氮或硫原子，并且可以与芳环稠合，被环烷基取代的低级烷基，低级烷基取代通过芳基，被如上定义的杂环基取代的低级烷基或R和R 1一起形成任选被氧，氮或硫原子间隔的聚亚甲基链，或者R 1与C（R）-N 它所连接的残基，完成杂环基团所需的原子; 并且R 2可以是氢，任选取代的被环烷基取代的低级烷基，环烷基，芳基或低级烷基，被含有一个或多个氮原子的杂环基取代的低级烷基; 通过含有一个或多个氮原子的杂环基团，或其与连接的C（H）-N残基一起可以表示完成杂环基团所需的原子; 且n为0,1,2,3或4; 包括使用氧化剂氧化具有下式的化合物：其中R，R 1，R 2和n具有其先前的含义，Z是H或通常用于氨基的保护基; 然后移除任何保护基团。

10. 发明授权

US5508270A Nucleoside phosphinate compounds and compositions 失效
标题翻译：核苷次膦酸盐化合物和组合物
公开(公告)号：US5508270A
公开(公告)日：1996-04-16
申请号：US203962
申请日：1994-02-28
申请人： Anthony D. Baxter , Eric K. Baylis , Stephen P. Collingwood , Roger J. Taylor , Alain Mesmaeker , Chantal Schmit
发明人： Anthony D. Baxter , Eric K. Baylis , Stephen P. Collingwood , Roger J. Taylor , Alain Mesmaeker , Chantal Schmit
IPC分类号： C07H9/04 , C07F9/30 , C07H13/06 , C07H19/06 , C07H19/10 , C07H19/16 , C07H19/20 , C07H21/00 , A61K31/70
CPC分类号： C07H19/10 , C07H19/20 , C07H21/00 , Y02P20/55
摘要： A compound of formula ##STR1## where R.sup.1 is hydrogen or a protecting group Q;R.sup.2 is hydrogen, a C.sub.1 -C.sub.8 aliphatic radical, a C.sub.6 -C.sub.15 aromatic radical, a C.sub.3 -C.sub.8 cycloaliphatic radical, a C.sub.7 -C.sub.13 araliphatic radical, an alkali metal ion or an ammonium ion;R.sup.3 and R.sup.4 are independently hydrogen, halogen or hydroxy;R.sup.5 is C.sub.6 -C.sub.10 aryloxythiocarbonyloxy, the C.sub.6 -C.sub.10 aryl group being unsubstituted or substituted, or R.sup.5.sub.a ;R.sup.5.sub.a is hydrogen, fluorine, chlorine, hydroxy, --OR.sup.8, --OCOR.sup.8 or silyloxy substituted by three C.sub.1 -C.sub.15 hydrocarbyl groups;R.sup.6 is hydrogen, a C.sub.1 -C.sub.10 aliphatic radical, a C.sub.6 -C.sub.15 aromatic radical, a C.sub.7 -C.sub.16 araliphatic radical, --COR.sup.9, --SO.sub.2 R.sup.9 or silyl substituted by three C.sub.1 -C.sub.15 hydrocarbyl groups;R.sup.7 is a monovalent nucleoside base radical, hydroxyl, --OR.sup.8 or --OCOR.sup.8, andR.sup.9 are independently a C.sub.1 -C.sub.10 aliphatic radical, a C.sub.3 -C.sub.8 cycloaliphatic radical, a C.sub.6 -C.sub.15 aromatic radical or a C.sub.7 -C.sub.16 araliphatic radical; orR.sup.5 and the indicated R.sup.6 O-together denote an isopropylidenedioxy group or R.sup.5 and R.sup.7 together denote an isopropylidenedioxy group, provided that when R.sup.5 and R.sup.7 together denote isopropylidenedioxy, R.sup.1 R.sup.2, R.sup.3 R.sup.4 and R.sup.6 are not all hydrogen. The disclosure further relates to a method of preparing the compounds of formula I by reacting a olefinic acetonide with a phosphinate compound and to the use of the compounds of formula I as pharmaceutical agents.
摘要翻译：式Ⅰ的化合物，其中R 1是氢或保护基团Q; R2是氢，C1-C8脂族基团，C6-C15芳族基团，C3-C8脂环族基团，C7-C13芳脂族基团，碱金属离子或铵离子; R3和R4独立地是氢，卤素或羟基; R5是C6-C10芳氧基硫代羰氧基，C6-C10芳基是未取代或取代的，或R5a; R5a是氢，氟，氯，羟基，-OR8，-OCOR8或被三个C1-C15烃基取代的甲硅烷氧基; R 6是氢，C 1 -C 10脂族基，C 6 -C 15芳基，C 7 -C 16芳脂基，-COR 9，-SO 2 R 9或被三个C 1 -C 15烃基取代的甲硅烷基; R7是单价核苷碱基，羟基-OR8或-OCOR8，R9独立地是C1-C10脂族基团，C3-C8脂环族基团，C6-C15芳族基团或C7-C16芳脂族基团; 或R5和所示的R6O一起表示异丙烯二氧基，或者R 5和R 7一起表示异亚丙二氧基，条件是当R 5和R 7一起表示异亚丙二氧基时，R 1 R 2，R 3 R 4和R 6不全为氢。本公开还涉及通过使烯属丙烯腈与次膦酸盐化合物反应制备式I化合物的方法，以及式I化合物作为药剂的用途。

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