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    Use of heterocyclic amides to inhibit tumor metastasis
    3.
    发明授权
    Use of heterocyclic amides to inhibit tumor metastasis 失效
    使用杂环酰胺抑制肿瘤转移

    公开(公告)号：US5010080A

    公开(公告)日：1991-04-23

    申请号：US279584

    申请日：1988-12-02

    申请人： George C. Fuller ,  George R. Martin ,  Richard A. Mueller ,  Reuven Reich

    发明人： George C. Fuller ,  George R. Martin ,  Richard A. Mueller ,  Reuven Reich

    IPC分类号： C07D295/18 ,  A61K31/495 ,  A61P43/00 ,  C07D241/04

    CPC分类号： A61K31/495

    摘要： A method of inhibiting tumor metastasis in an animal without treating the tumor cells by administering to said animal a metastasis inhibiting effective amount of a heterocyclic amide represented by the formula: ##STR1## wherein: R.sub.1 and R.sub.2 are the same or different members of the group consisting of halo, phenyl, substituted phenyl and a ##STR2## group wherein q, r and t are independently an integer of from 1 to 8 provided that q+r+t is equal to or less than 10; Y is thio or sulfinyl; alk is straight or branched chain lower alkylene, and R.sub.3 is a heterocyclic amine represented by the formula: ##STR3## wherein R.sub.4 is selected from the group consisting of hydrogen, lower alkyl, phenyl, substituted phenyl, benzyl, or substituted benzyl; p is 0 to 2; or a pharmaceutically acceptable salt thereof.

    Carbamoyl-and thiocarbamoyl-phosphonates and pharmaceutical compositions comprising them
    4.
    发明授权
    Carbamoyl-and thiocarbamoyl-phosphonates and pharmaceutical compositions comprising them 失效
    氨基甲酰基 - 和硫代氨基甲酰基 - 膦酸酯和包含它们的药物组合物

    公开(公告)号：US07345033B2

    公开(公告)日：2008-03-18

    申请号：US11244405

    申请日：2005-10-06

    申请人： Eli Breuer ,  Reuven Reich ,  Gershon Golomb ,  Yiffat Katz

    发明人： Eli Breuer ,  Reuven Reich ,  Gershon Golomb ,  Yiffat Katz

    IPC分类号： A61K31/66 ,  C07F9/22

    CPC分类号： C07F9/4065 ,  C07F9/3891

    摘要： The present invention provides a compound of the following formula I: R3—NH—C(═X)—P(═O)OR1OR2 including pharmaceutically acceptable salts, solvates, hydrates and polymorphs of the compounds of formula I, as well as geometrical isomers and optically active forms of the compounds of formula I and pharmaceutically acceptable salts, solvates, hydrates and polymorphs of said isomers and forms, wherein R1 and R2 may be the same or different and are each selected from hydrogen, acyloxyalkyl and aryl or R1 and R2 may form together with the oxygen and phosphorus atoms a dioxaphosphacycloalkane ring; X is O or S; and R3 is selected, when X is O, from bicycloalkyl, cycloalkylalkyl and substituted cycloalkyl by at least one of alkyl, amino, amidino and guanidino; and R3 is selected, when X is S, from bicycloalkyl, cycloalkylalkyl and cycloalkyl optionally substituted by at least one of alkyl, amino, amidino and guanidino; with the proviso that: when X is O, R3 is not cyclohexylmethyl, and when X is S, R3 is not cyclohexyl. The invention further provides pharmaceutical compositions comprising the above compounds and their use in medicine.

    摘要翻译： 本发明提供下式I的化合物：<？在线式描述=“In-line formula”end =“lead”→R 3 -NH-C（-X ）-P（-O）OR 1或/或2“-in-line-formula description =”In-line Formulas“end =”tail“？>包括药学上可接受的 式I化合物的盐，溶剂合物，水合物和多晶型物，以及式I化合物的几何异构体和光学活性形式以及所述异构体和形式的药学上可接受的盐，溶剂合物，水合物和多晶型物，其中R 1和R 2可以相同或不同，并且各自选自氢，酰氧基烷基和芳基或R 1和R 2 >可与氧和磷原子一起形成二氧杂环磷杂环烷环; X是O或S; 当X为O时，R 3选自烷基，氨基，脒基和胍基中的至少一个来自双环烷基，环烷基烷基和取代环烷基; 当X为S时，选自二烷基，环烷基烷基和任选被烷基，氨基，脒基和胍基中的至少一个取代的环烷基; 条件是：当X是O时，R 3不是环己基甲基，当X是S时，R 3不是环己基。 本发明还提供了包含上述化合物及其在药物中的用途的药物组合物。

    Carbamoyl-and thiocarbamoyl-phosphonates and pharmaceutical compositions comprising them
    7.
    发明申请
    Carbamoyl-and thiocarbamoyl-phosphonates and pharmaceutical compositions comprising them 失效
    氨基甲酰基 - 和硫代氨基甲酰基 - 膦酸酯和包含它们的药物组合物

    公开(公告)号：US20060111328A1

    公开(公告)日：2006-05-25

    申请号：US11244405

    申请日：2005-10-06

    申请人： Eli Breuer ,  Reuven Reich ,  Gershon Golomb ,  Yiffat Katz

    发明人： Eli Breuer ,  Reuven Reich ,  Gershon Golomb ,  Yiffat Katz

    IPC分类号： A61K31/66 ,  C07F9/22

    CPC分类号： C07F9/4065 ,  C07F9/3891

    摘要： The present invention provides a compound of the following formula I: R3—NH—C(═X)—P(═O)OR1OR2 including pharmaceutically acceptable salts, solvates, hydrates and polymorphs of the compounds of formula I, as well as geometrical isomers and optically active forms of the compounds of formula I and pharmaceutically acceptable salts, solvates, hydrates and polymorphs of said isomers and forms, wherein R1 and R2 may be the same or different and are each selected from hydrogen, acyloxyalkyl and aryl or R1 and R2 may form together with the oxygen and phosphorus atoms a dioxaphosphacycloalkane ring; X is O or S; and R3 is selected, when X is O, from bicycloalkyl, cycloalkylalkyl and substituted cycloalkyl by at least one of alkyl, amino, amidino and guanidino; and R3 is selected, when X is S, from bicycloalkyl, cycloalkylalkyl and cycloalkyl optionally substituted by at least one of alkyl, amino, amidino and guanidino; with the proviso that: when X is O, R3 is not cyclohexylmethyl, and when X is S, R3 is not cyclohexyl. The invention further provides pharmaceutical compositions comprising the above compounds and their use in medicine.

    摘要翻译： 本发明提供下式I的化合物：<？在线式描述=“In-line formula”end =“lead”→R 3 -NH-C（-X ）-P（-O）OR 1或/或2“-in-line-formula description =”In-line Formulas“end =”tail“？>包括药学上可接受的 式I化合物的盐，溶剂合物，水合物和多晶型物，以及式I化合物的几何异构体和光学活性形式以及所述异构体和形式的药学上可接受的盐，溶剂合物，水合物和多晶型物，其中R 1和R 2可以相同或不同，并且各自选自氢，酰氧基烷基和芳基或R 1和R 2 >可与氧和磷原子一起形成二氧杂环磷杂环烷环; X是O或S; 当X为O时，R 3选自烷基，氨基，脒基和胍基中的至少一个来自双环烷基，环烷基烷基和取代环烷基; 当X为S时，选自二烷基，环烷基烷基和任选被烷基，氨基，脒基和胍基中的至少一个取代的环烷基; 条件是：当X是O时，R 3不是环己基甲基，当X是S时，R 3不是环己基。 本发明还提供了包含上述化合物及其在药物中的用途的药物组合物。

    Use of lipid conjugates in the treatment of disease
    9.
    发明授权
    Use of lipid conjugates in the treatment of disease 有权

    公开(公告)号：US07034006B2

    公开(公告)日：2006-04-25

    申请号：US09756765

    申请日：2001-01-10

    申请人： Saul Yedgar ,  David Shuseyov ,  Gershon Golomb ,  Reuven Reich ,  Isaac Ginsburg ,  Abd-al-Roof Higazi ,  Moshe Ligumski ,  Miron Krimsky ,  David Ojcius ,  Benito Antonio Yard ,  Fokko Johannes van der Woude ,  Edit Schnitzer

    发明人： Saul Yedgar ,  David Shuseyov ,  Gershon Golomb ,  Reuven Reich ,  Isaac Ginsburg ,  Abd-al-Roof Higazi ,  Moshe Ligumski ,  Miron Krimsky ,  David Ojcius ,  Benito Antonio Yard ,  Fokko Johannes van der Woude ,  Edit Schnitzer

    IPC分类号： A61K31/70 ,  A61K31/715 ,  C08B37/08 ,  C08B37/10 ,  C07H5/06

    CPC分类号： A61K47/544

    摘要： The invention provides novel methods for treating disease based upon the medicinal use of lipids and phospholipids covalently bound to physiologically acceptable monomers or polymers. Phosphatidylethanolamine moieties conjugated to physiologically acceptable monomers and polymers (PE conjugates) manifest an unexpectedly wide range of pharmacological effects, including stabilizing cell membranes; limiting oxidative damage to cell and blood components; limiting cell proliferation, cell extravasation and (tumor) cell migratory behavior; suppressing immune responses; and attenuating physiological reactions to stress, as expressed in elevated chemokine levels. The surprisingly manifold pharmacological properties of the PL-conjugates allow for the invention, disclosed herein, of novel methods for the treatment of a diverse range of disease states, including obstructive respiratory disease, including asthma; colitis and Crohn's disease; central nervous system insult, including blood brain barrier compromise, ischemic stroke, and multiple sclerosis; contact dermatitis; psoriasis; cardiovascular disease, including ischemic conditions and prophylaxis for invasive vascular procedures; cellular proliferative disorders, including anti-tumor vasculogenesis, invasiveness, and metastases; anti-oxidant therapy; hemolytic syndromes; sepsis; acute respiratory distress syndrome; tissue transplant rejection syndromes; autoimmune disease; viral infection; and hypersensitivity conjunctivitis. The therapeutic methods of the invention include administration of phosphatidylethanolamine bound to carboxymethylcellulose, heparin, hyaluronic acid, polyethylene glycol, and hemaccel. Disclosed herein are also new compounds comprised of phospholipid moieties bound to low molecular weight monomers and dimers, including mono- and disaccharides, carboxylated disaccharides, mono- and dicarboxylic acids, salicylates, bile acids, and fatty acids.