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1. 发明授权

US07259273B1 Compositions containing lysophosphotidic acids which inhabit apoptosis and uses thereof 失效
标题翻译：含有溶血磷脂酸的组合物，其存在凋亡及其用途
公开(公告)号：US07259273B1
公开(公告)日：2007-08-21
申请号：US11236429
申请日：2005-09-26
申请人： John G. Goddard , Donald H. Picker , Samuil R. Umansky , Steven Price , Jac C. Wijkmans , Edward A. Boyd , Anthony D. Baxter
发明人： John G. Goddard , Donald H. Picker , Samuil R. Umansky , Steven Price , Jac C. Wijkmans , Edward A. Boyd , Anthony D. Baxter
IPC分类号： C07C305/00 , A61K31/66
CPC分类号： C07F9/091
摘要： The invention provides anti-apoptotic compositions containing lysophosphatidic acids and methods for making and using the compositions. Such compositions may also contain LPA potentiating agents, including proteins, lipid membrane structures and polymers such as polyethylene glycols. The compositions can additionally contain other pharmaceutically effective agents such as drugs, antibiotics, wound healing agents and antioxidants.
摘要翻译：本发明提供含有溶血磷脂酸的抗凋亡组合物和制备和使用组合物的方法。此类组合物还可含有LPA增效剂，包括蛋白质，脂质膜结构和聚合物如聚乙二醇。组合物可另外含有其它药学上有效的试剂，例如药物，抗生素，伤口愈合剂和抗氧化剂。

2. 发明授权

US5013733A Lactam derivatives 失效
公开(公告)号：US5013733A
公开(公告)日：1991-05-07
申请号：US485532
申请日：1990-02-27
申请人： Ian H. Coates , Alexander W. Oxford , Peter C. North , Thomas Miller , Anthony D. Baxter , Kevin I. Hammond
发明人： Ian H. Coates , Alexander W. Oxford , Peter C. North , Thomas Miller , Anthony D. Baxter , Kevin I. Hammond
IPC分类号： C07D453/02 , A61K31/435 , A61P1/00 , A61P1/04 , A61P1/08 , A61P25/00 , A61P25/04 , A61P25/18 , A61P25/20 , A61P25/28 , A61P43/00 , C07D519/00
CPC分类号： C07D519/00
摘要： The invention provides lactam derivatives of the general formula (I) ##STR1## wherein R.sup.1 represents a hydrogen atom or a group selected from C.sub.1-6 alkyl, C.sub.3-6 alkenyl, C.sub.3-10 alkynyl, C.sub.3-7 cycloalkyl, C.sub.3-7 cycloalkylC.sub.1-4 alkyl, phenyl, phenylC.sub.1-3 alkyl, phenylmethoxymethyl, phenoxyethyl, phenoxymethyl, --CO.sub.2 R.sup.3, --COR.sup.3, --CONR.sup.3 R.sup.4 or --SO.sub.2 R.sup.3 (wherein R.sup.3 and R.sup.4, which may be the same or different each represents a hydrogen atom, a C.sub.1-6 alkyl or C.sub.3-7 cycloalkyl group, or a phenyl or phenylC.sub.1-4 alkyl group, in which the phenyl group is optionally substituted by one or more C.sub.1-4 alkyl, C.sub.1-4 alkoxy or hydroxy groups or halogen atoms, with the proviso that R.sup.3 does not represent a hydrogen atom when R.sup.1 represents a group --CO.sub.2 R.sup.3 or --SO.sub.2 R.sup.3);and R.sup.2 represents a group of formula (a), (b) or (c): ##STR2## wherein R.sup.5 represents a hydrogen atom or a C.sub.1-6 alkyl, C.sub.3-7 cycloalkyl, C.sub.3-6 alkenyl or phenylC.sub.1-3 alkyl group;n represents 2, 3 or 4;Q represents a hydrogen or a halogen atom, or a hydroxy, C.sub.1-4 alkoxy, phenylC.sub.1-3 alkoxy or C.sub.1-6 alkyl group or a group --NH.sup.6 R.sup.7 or --CONR.sup.6 R.sup.7 wherein R.sup.6 and R.sup.7, which may be the same or different, each represents a hydrogen atom or a C.sub.1-4 alkyl or C.sub.3-4 alkenyl group, or together with the nitrogen atom to which they are attached form a saturated 5 to 7 membered ring); and physiologically acceptable salts and solvates thereof.The compounds of formula (I) are potent and selective antagonists of 5-hydroxytryptamine at 5-HT.sub.3 receptors and are useful, for example in the treatment of psychotic disorders, anxiety and nausea and vomiting.

3. 发明授权

US5100896A Carbocyclic analogues of 7H-1,2,3-triazolo [4,5-d]pyrimidine furanosides 失效
标题翻译： 7H-1,2,3-三唑（4,5-D）吡咯烷酮类的半胱氨酸类似物
公开(公告)号：US5100896A
公开(公告)日：1992-03-31
申请号：US556262
申请日：1990-07-23
申请人： Alan D. Borthwick , Keith Biggadike , Barrie E. Kirk , Richard Storer , Niall G. Weir , Anthony D. Baxter , Chi L. Mo
发明人： Alan D. Borthwick , Keith Biggadike , Barrie E. Kirk , Richard Storer , Niall G. Weir , Anthony D. Baxter , Chi L. Mo
IPC分类号： A61K31/505 , A61P31/12 , C07D487/04
CPC分类号： C07D487/04
摘要： The present invention provides a compound of formula (I) ##STR1## and salts and solvates and pharmaceutically acceptable derivatives thereof, and describes processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of viral diseases, especially those caused by the Herpetoviridae.

4. 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。

5. 发明授权

US5466677A Dinucleoside phosphinates and their pharmaceutical compositions 失效
标题翻译：二核苷次膦酸盐及其药物组合物
公开(公告)号：US5466677A
公开(公告)日：1995-11-14
申请号：US204020
申请日：1994-02-28
申请人： Anthony D. Baxter , Eric K. Baylis , Stephen P. Collingwood , Roger J. Taylor , Alain De Mesmaeker , Chantal Schmit
发明人： Anthony D. Baxter , Eric K. Baylis , Stephen P. Collingwood , Roger J. Taylor , Alain De Mesmaeker , Chantal Schmit
IPC分类号： G01N33/569 , A61K31/665 , A61K31/70 , A61K31/7042 , A61K31/7052 , A61K31/7064 , A61K31/7072 , A61K31/7076 , A61P31/12 , A61P31/16 , C07F9/6512 , C07F9/655 , C07F9/6561 , C07H19/04 , C07H19/06 , C07H19/16 , C07H21/00 , C07H21/02 , C07H21/04
CPC分类号： C07H21/00 , C07H19/04
摘要： A dinucleotide analogue of formula ##STR1## where B.sup.1 and B.sup.2 are each independently a monovalent nucleoside base radical;R.sup.1 is R.sup.1.sub.a or Z;R.sup.1.sub.a, R.sup.2, R.sup.3 and R.sup.4 are each independently hydrogen, halogen or hydroxy;R.sup.5 is R.sup.5.sub.a or Z;R.sup.6 is hydrogen or R.sup.6.sub.a ;R.sup.7 is hydrogen, alkyl-N,N-dialkylphosphoramidyl or R.sup.7.sub.a, R.sup.8 is R.sup.8.sub.a or Z, or the indicated R.sup.7 O and R.sup.8 together denote an isopropylidenedioxy group;R.sup.5.sub.a and R.sup.8.sub.a are each independently hydrogen, halogen, hydroxy, --OR.sup.10, --OCOR.sup.10 or silyloxy substituted by three C.sub.1 -C.sub.15 hydrocarbyl groups;R.sup.6.sub.a and R.sup.7.sub.a are each independently a C.sub.1 -C.sub.10 aliphatic radical, a C.sub.6 -C.sub.15 aromatic radical, a C.sub.7 -C.sub.30 araliphatic radical, --COR.sup.11, --SO.sub.2 R.sup.11 or silyl substituted by three C.sub.1 -C.sub.15 hydrocarbyl groups;R.sup.9 is hydrogen, a C.sub.1 -C.sub.8 aliphatic radical, a C.sub.3 -C.sub.8 cycloaliphatic radical, a C.sub.6 -C.sub.15 aromatic radical, a C.sub.7 -C.sub.13 araliphatic radical, an alkali metal ion or an ammonium ion;R.sup.10 and R.sup.11 are each 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;R.sup.x and R.sup.y are independently hydrogen, halogen, hydroxy, a C.sub.1 -C.sub.10 alkyl, C.sub.2 -C.sub.10 alkenyl, C.sub.3 -C.sub.8 cycloalkyl, C.sub.6 -C.sub.15 aryl, C.sub.7 -C.sub.16 aralkyl, C.sub.1 -C.sub.10 alkoxy, C.sub.2 -C.sub.10 alkenoxy, C.sub.6 -C.sub.10 aryloxy or C.sub.7 -C.sub.16 aralkyloxy group, which is substituted or unsubstituted, or --OCOR.sup.z ;R.sup.z is a substituted or unsubstituted C.sub.1 -C.sub.10 alkyl, C.sub.2 -C.sub.10 alkenyl, C.sub.3 -C.sub.8 cycloalkyl, C.sub.6 -C.sub.15 aryl or C.sub.7 -C.sub.16 aralkyl group; andZ is C.sub.6 -C.sub.10 aryloxythiocarbonyloxy, the C.sub.6 -C.sub.10 aryl group being substituted or unsubstituted.
摘要翻译：式Ⅰ的二核苷酸类似物，其中B1和B2各自独立地是一价核苷碱基; R1为R1a或Z; R1a，R2，R3和R4各自独立地为氢，卤素或羟基; R5为R5a或Z; R6是氢或R6a; R7是氢，烷基-N，N-二烷基磷酰胺基或R7a，R8是R8a或Z，或者所指示的R7O和R8一起表示异丙烯二氧基; R5a和R8a各自独立地为氢，卤素，羟基，-OR10，-OCOR10或被三个C1-C15烃基取代的甲硅烷氧基; R6a和R7a各自独立地为C1-C10脂族基团，C6-C15芳族基团，C7-C30芳脂族基团，-COR11，-SO2R11或被三个C1-C15烃基取代的甲硅烷基基团; R9是氢，C1-C8脂族基团，C3-C8脂环族基团，C6-C15芳族基团，C7-C13芳脂族基团，碱金属离子或铵离子; R 10和R 11各自独立地为C 1 -C 10脂族基团，C 3 -C 8脂环族基团，C 6 -C 15芳族基团或C 7 -C 16芳脂族基团; Rx和Ry独立地是氢，卤素，羟基，C1-C10烷基，C2-C10烯基，C3-C8环烷基，C6-C15芳基，C7-C16芳烷基，C1-C10烷氧基，C2-C10链烯氧基，C6-C10芳氧基或取代或未取代的C 7 -C 16芳烷氧基或-OCOR z; Rz是取代或未取代的C1-C10烷基，C2-C10烯基，C3-C8环烷基，C6-C15芳基或C7-C16芳烷基; Z为C6-C10芳氧基硫代羰氧基，C6-C10芳基为取代或未取代的。

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