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    • 1. 发明授权
    • Phosphate transport inhibitors
    • 磷酸盐转运抑制剂
    • US07754200B2
    • 2010-07-13
    • US11438679
    • 2006-05-22
    • Thomas H. JozefiakCecilia M. BastosChad C. Huval
    • Thomas H. JozefiakCecilia M. BastosChad C. Huval
    • A61K31/74
    • C07F9/65502C07F9/3821C07F9/4012C07F9/5537C08F8/40C08F30/02Y02P20/55
    • Disclosed is a phosphate transport inhibiting compound represented by Structural Formula (I): R1 and R2 are independently —H, an electron withdrawing group or a C1-C10 alkyl group. Y is a covalent bond, a substituted methylene group, an unsubstituted methylene group or —CR1R2P(O)(OH)—. R3 is a hydrocarbyl group optionally comprising one or more amine, ammonium, ether, thioether or phenylene linking groups, a substituted hydrocarbyl group optionally comprising one or more amine, ammonium, ether, thioether or phenylene linking groups, a heteroaryl group, a substituted heteroaryl group or a phenyl group substituted with one or more groups selected from —Cl, —Br, —F, —CN, —NO2, —ORa, —N(Ra)2, —COORa, —CON(Ra)2, —CORa, —S(O)Ra, —S(O)2Ra, —S(O)2N(Ra)2, —NRaS(O)2Ra, —NRaCORa, a halogenated lower alkyl group, an aryl group, a substituted aryl group, or a halogenated alkoxy group. Each Ra is independently —H, lower alkyl, substituted lower alkyl, aryl or substituted aryl.Each Rb is independently —H, a lower alkyl group, or a phosphate protecting group.
    • 公开了由结构式(I)表示的磷酸盐转运抑制化合物:R1和R2独立地为-H,吸电子基团或C1-C10烷基。 Y是共价键,取代亚甲基,未取代的亚甲基或-CR 1 R 2 P(O)(OH) - 。 R3是任选地包含一个或多个胺,铵,醚,硫醚或亚苯基连接基团的烃基,任选地包含一个或多个胺,铵,醚,硫醚或亚苯基连接基团的取代的烃基,杂芳基,取代的杂芳基 被一个或多个选自-Cl,-Br,-F,-CN,-NO 2,-OR a,-N(R a)2,-COOR a,-CON(R a)2,-COR a ,-S(O)R a,-S(O)2 R a,-S(O)2 N(R a)2,-NR a(O)2 R a,-NR a COR a,卤代低级烷基,芳基,取代的芳基 ,或卤代烷氧基。 每个R a独立地为-H,低级烷基,取代的低级烷基,芳基或取代的芳基。 每个R b独立地是-H,低级烷基或磷酸酯保护基。
    • 8. 发明授权
    • Phosphate transport inhibitors
    • 磷酸盐转运抑制剂
    • US07119120B2
    • 2006-10-10
    • US10327627
    • 2002-12-20
    • Thomas H. JozefiakCecilia M. BastosAndrew T. PapoulisStephen Randall Holmes-Farley
    • Thomas H. JozefiakCecilia M. BastosAndrew T. PapoulisStephen Randall Holmes-Farley
    • A61K31/18A61K31/16A61K37/18
    • A61K45/06A61K31/166A61K31/17A61K31/18A61K31/415A61K31/63A61K33/38A61K2300/00
    • Disclosed are compounds which have been identified as inhibitors of phosphate transport. Many of the compounds are represented by Structural Formula (I): Ar1—W—X—Y—Ar2; or a pharmaceutically acceptable salt thereof. Ar1 and Ar2 are independently a substituted or unsubstituted aryl group or an optionally substituted five membered or six membered non-aromatic heterocylic group fused to an optionally substituted monocylic aryl group. W and Y are independently a covalent bond or a C1–C3 substituted or unsubstituted alkylene group. X is a heteroatom-containing functional group, an aromatic heterocyclic group, substituted aromatic heterocyclic group, non-aromatic heterocyclic group, substituted non-aromatic heterocyclic group, an olefin group or a substituted olefin group. Also disclosed are methods of treating a subject with a disease associated with hyperphosphatemia, as well as a disease mediated by phosphate-transport function. The methods comprise the step of administering an effective amount of the one of the compounds described above.
    • 公开了已被鉴定为磷酸盐转运抑制剂的化合物。 许多化合物由结构式(I)表示:<?in-line-formula description =“In-line Formulas”end =“lead”?> Ar -WXY-Ar 2 <?in-line-formula description =“In-line Formulas”end =“tail”?>或其药学上可接受的盐。 Ar 1和Ar 2独立地是与任选取代的单环芳基稠合的取代或未取代的芳基或任选取代的五元或六元非芳族杂环基。 W和Y独立地是共价键或C1-C3取代或未取代的亚烷基。 X为含杂原子的官能团,芳香族杂环基,取代芳香族杂环基,非芳香族杂环基,取代非芳香族杂环基,烯基或取代烯基。 还公开了治疗患有与高磷酸盐血症相关的疾病的受试者以及由磷酸盐转运功能介导的疾病的方法。 所述方法包括施用有效量的上述一种化合物的步骤。
    • 9. 发明授权
    • Photographic element containing a novel cyan dye forming coupler and
process for its use
    • 含有新型青色染料成色剂的摄影元件及其使用方法
    • US5476757A
    • 1995-12-19
    • US359134
    • 1994-12-19
    • Philip T. S. LauThomas H. JozefiakThomas R. Welter
    • Philip T. S. LauThomas H. JozefiakThomas R. Welter
    • G03C7/00G03C7/32G03C7/34
    • G03C7/344G03C7/3212
    • A photographic element comprises a light sensitive silver halide emulsion layer having associated therewith a cyan dye-forming coupler dispersed in an organic solvent, the coupler having the formula: ##STR1## wherein A, B, and C are hydrogen or fluorine;X is selected from the group consisting of halogen, alkoxy and methyl groups;R is a straight chain aliphatic group which is unsubstituted or substituted with one or members selected from the group consisting of --F, --R", --OR", --SO.sub.2 R", --SO.sub.2 NHR", --CONHR", --COOR", --NHCOR", --NHSO.sub.2 R", and --OCOR" where R" is a primary or secondary alkyl group;R' is a substituent group and m is from 0 to 4;COG is hydrogen or a coupling-off group capable of being split-off by an oxidized color developer; andwherein the substituent groups X, R, and R' are selected so as to ballast the coupler and prevent it from wandering within the photographic coatings.The invention also encompasses a process for forming an image in an element as described after it has been exposed.
    • 照相元件包括光敏卤化银乳剂层,其具有分散在有机溶剂中的形成青色染料的成色剂,所述成色剂具有下式:尿素; X选自卤素,烷氧基和甲基; R是未取代的或被选自-F,-R“,-OR”,-SO 2 R“,-SO 2 NHR”,-CONHR“的一个或多个成员取代的直链脂族基团, -COOR“,-NHCOR”,-NHSO 2 R“和-OCOR”,其中R“是伯或仲烷基; R'为取代基,m为0〜4; COG是氢或能够被氧化的显色剂分离的偶合离去基团; 并且其中选择取代基X,R和R',以便使耦合剂镇定并防止其在照相涂层内漂浮。 本发明还包括用于在已经暴露之后描述的元件中形成图像的方法。