3,4-disubstituted phenols-immunomodulating agents
    51.
    发明授权
    3,4-disubstituted phenols-immunomodulating agents 失效
    3,4-二取代苯酚 - 免疫调节剂

    公开(公告)号:US5466715A

    公开(公告)日:1995-11-14

    申请号:US208396

    申请日:1994-03-08

    摘要: Certain 3,4-disubstituted phenols and pharmaceutically acceptable salts thereof are provided which mimic IL-1 activity by inducing IL-2 synthesis and subsequent IL-2 receptor expression. Specifically, the invention provides compounds of Formula I and acid addition salts thereof: ##STR1## wherein Y is ##STR2## NHSO.sub.2 or SO.sub.2 NH where R.sup.4 is H; Z is --O--, --NH--, --NR--, --S--, or other heteroatoms capable of hydrogen bonding with R.sup.4 to give a preferred conformation;R is alkyl;R.sup.1 is --OH;R.sup.2 is H, alkyl, cycloalkyl, aralkyl, substituted or unsubstituted aryl, or a substituted or unsubstituted nitrogen heterocyclic group having 4 to 5 nuclear carbon atoms; andR.sup.3 is a lipophilic moiety selected from the group consisting of substituted C.sub.1 -C.sub.10 alkyl, C.sub.3 -C.sub.16 cycloalkyl and 2,4-di-t-pentylphenyl.

    摘要翻译: 提供了通过诱导IL-2合成和随后的IL-2受体表达而模拟IL-1活性的某些3,4-二取代的苯酚及其药学上可接受的盐。 具体地,本发明提供式I化合物及其酸加成盐:其中Y为NHSO 2或SO 2 NH,其中R 4为H; Z是-O-,-NH-,-NR-,-S-或能够与R4氢键合的其它杂原子,以产生优选的构象; R是烷基; R1是-OH; R2是H,烷基,环烷基,芳烷基,取代或未取代的芳基或取代或未取代的具有4至5个核碳原子的氮杂环基; 并且R 3是选自取代的C 1 -C 10烷基,C 3 -C 16环烷基和2,4-二 - 叔戊基苯基的亲脂性部分。

    Compositions of iodophenyl esters and iodophenyl sulfonates in
film-forming materials for visualization of the gastrointestinal tract
    52.
    发明授权
    Compositions of iodophenyl esters and iodophenyl sulfonates in film-forming materials for visualization of the gastrointestinal tract 失效
    碘苯基酯和碘苯基磺酸盐在成膜材料中用于胃肠道可视化的组合物

    公开(公告)号:US5372800A

    公开(公告)日:1994-12-13

    申请号:US192234

    申请日:1994-02-04

    摘要: Disclosed are x-ray contrast compositions for oral or retrograde examination of the gastrointestinal tract comprising a polymeric material capable of forming a coating on the gastrointestinal tract and an x-ray producing agent of the formula ##STR1## and methods for their use in diagnostic radiology of the gastrointestinal tract whereinX= ##STR2## Z=H, halo, C.sub.1 -C.sub.20 alkyl, cycloalkyl, lower alkoxy, cyano, where the alkyl and cycloalkyl groups can be substituted with halogen or halo-lower-alkyl groups;R=C.sub.1 -C.sub.25 alkyl, cycloalkyl, aryl or halo-lower-alkyl, optionally substituted with halo, fluoro-lower-alkyl, lower-alkoxy, hydroxy, carboxy or lower-alkoxy carbonyl, lower-alkenyl, lower-alkynyl, lower-alkylene or lower-alkoxy-carbonyloxy,n is 1-5;y is 0-4; andw is 1-4.

    摘要翻译: 公开了用于口腔或逆行检查胃肠道的x射线造影剂组合物,其包含能够在胃肠道上形成涂层的聚合物材料和具有式“IMAGE”的X射线产生剂及其用于诊断放射学的方法 的胃肠道,其中X = Z,H =卤素,C 1 -C 20烷基,环烷基,低级烷氧基,氰基,其中烷基和环烷基可被卤素或卤代低级烷基取代; R = C 1 -C 25烷基,环烷基,芳基或卤代低级烷基,任选被卤素,氟代低级烷基,低级烷氧基,羟基,羧基或低级烷氧基羰基,低级烯基,低级炔基,低级 - 亚烷基或低级 - 烷氧基 - 羰氧基,n为1-5; y为0-4; w为1-4。

    Compositions of alkylbenzenes in film-forming materials for
visualization of the gastrointestinal tract
    53.
    发明授权
    Compositions of alkylbenzenes in film-forming materials for visualization of the gastrointestinal tract 失效
    用于胃肠道可视化的成膜材料中烷基苯的组成

    公开(公告)号:US5334370A

    公开(公告)日:1994-08-02

    申请号:US13459

    申请日:1993-02-04

    摘要: Disclosed are x-ray contrast compositions for oral or retrograde examination of the gastrointestinal tract comprising a polymeric material capable of forming a coating on the gastrointestinal tract and an x-ray producing agent of the formula ##STR1## and methods for their use in diagnostic radiology of the gastrointestinal tract whereinR=C.sub.1 -C.sub.25 alkyl, cycloalkyl, unsaturated allyl or halo-lower-alkyl, optionally substituted with halo, fluoro-lower-alkyl, aryl, lower-alkoxy, hydroxy, carboxy, lower-alkoxy carbonyl or lower-alkoxy-carbonyloxy, (CR.sub.1 R.sub.2).sub.p --(CR.sub.3 .dbd.CR.sub.4).sub.m Q, or (CR.sub.1 R.sub.2).sub.p --C.tbd.C--Q;R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are independently H, lower-alkyl, optionally substituted with halo;n is 1-5;m is 1-5;p is 1-10; andQ is H, lower-alkyl, lower-alkenyl, lower-alkynyl, lower-alkylene, aryl, or aryl-lower alkyl.

    摘要翻译: 公开了用于口腔或逆行检查胃肠道的x射线造影剂组合物,其包含能够在胃肠道上形成涂层的聚合物材料和具有式“IMAGE”的X射线产生剂及其用于诊断放射学的方法 的胃肠道,其中R = C 1 -C 25烷基,环烷基,不饱和烯丙基或卤代低级烷基,任选被卤素,氟 - 低级 - 烷基,芳基,低级 - 烷氧基,羟基,羧基,低级 - 烷氧基羰基或低级 (CR 1 R 2)p - (CR 3 = CR 4)m Q或(CR 1 R 2)p C 3 B 3 CQ; R 1,R 2,R 3和R 4独立地为H,低级烷基,任选被卤素取代; n为1-5; m为1-5; p为1-10; 并且Q是H,低级烷基,低级烯基,低级炔基,低级亚烷基,芳基或芳基 - 低级烷基。

    Inhibitors of c-fms kinase
    54.
    发明授权
    Inhibitors of c-fms kinase 有权
    c-fms激酶抑制剂

    公开(公告)号:US08815867B2

    公开(公告)日:2014-08-26

    申请号:US11736653

    申请日:2007-04-18

    IPC分类号: A61K31/496 C07D403/10

    摘要: The invention is directed to compounds of Formula I: wherein Z, X, J, R2 and W are set forth in the specification, as well as solvates, hydrates, tautomers and pharmaceutically acceptable salts thereof, that inhibit protein tyrosine kinases, especially c-fms kinase. Methods of treating autoimmune diseases; and diseases with an inflammatory component; treating metastasis from ovarian cancer, uterine cancer, breast cancer, prostate cancer, lung cancer, colon cancer, stomach cancer, hairy cell leukemia; and treating pain, including skeletal pain caused by tumor metastasis or osteoarthritis, or visceral, inflammatory, and neurogenic pain; as well as osteoporosis, Paget's disease, and other diseases in which bone resorption mediates morbidity including rheumatoid arthritis, and other forms of inflammatory arthritis, osteoarthritis, prosthesis failure, osteolytic sarcoma, myeloma, and tumor metastasis to bone with the compounds of Formula I, are also provided.

    摘要翻译: 本发明涉及式I化合物:其中Z,X,J,R 2和W在本说明书中列出,以及其抑制蛋白酪氨酸激酶,特别是c-型的溶剂化物,水合物,互变异构体和药学上可接受的盐, fms激酶。 治疗自身免疫性疾病的方法 和具有炎症成分的疾病; 治疗卵巢癌,子宫癌,乳腺癌,前列腺癌,肺癌,结肠癌,胃癌,毛细胞白血病的转移; 并治疗疼痛,包括由肿瘤转移或骨关节炎引起的骨骼疼痛,或内脏,炎症和神经源性疼痛; 骨质疏松症,佩吉特氏病和其他疾病,其中骨吸收介导包括类风湿性关节炎和其它形式的炎症性关节炎,骨关节炎,假体衰竭,溶骨性肉瘤,骨髓瘤和肿瘤转移至骨骼的发病率与式I化合物, 也提供。

    INHIBITORS OF C-FMS KINASE
    58.
    发明申请
    INHIBITORS OF C-FMS KINASE 有权
    C-FMS激酶抑制剂

    公开(公告)号:US20090105296A1

    公开(公告)日:2009-04-23

    申请号:US12252439

    申请日:2008-10-16

    摘要: The invention is directed to compounds of Formula I: wherein Z, X, J, R2 and W are set forth in the specification, as well as solvates, hydrates, tautomers and pharmaceutically acceptable salts thereof, that inhibit protein tyrosine kinases, especially c-fms kinase. Methods of treating autoimmune diseases; and diseases with an inflammatory component; treating metastasis from ovarian cancer, uterine cancer, breast cancer, prostate cancer, lung cancer, colon cancer, stomach cancer, hairy cell leukemia; and treating pain, including skeletal pain caused by tumor metastasis or osteoarthritis, or visceral, inflammatory, and neurogenic pain; as well as osteoporosis, Paget's disease, and other diseases in which bone resorption mediates morbidity including rheumatoid arthritis, and other forms of inflammatory arthritis, osteoarthritis, prosthesis failure, osteolytic sarcoma, myeloma, and tumor metastasis to bone with the compounds of Formula I, are also provided.

    摘要翻译: 本发明涉及式I化合物:其中Z,X,J,R 2和W在本说明书中列出,以及其抑制蛋白酪氨酸激酶,特别是c-型的溶剂化物,水合物,互变异构体和药学上可接受的盐, fms激酶。 治疗自身免疫性疾病的方法 和具有炎症成分的疾病; 治疗卵巢癌,子宫癌,乳腺癌,前列腺癌,肺癌,结肠癌,胃癌,毛细胞白血病的转移; 并治疗疼痛,包括由肿瘤转移或骨关节炎引起的骨骼疼痛,或内脏,炎症和神经源性疼痛; 骨质疏松症,佩吉特氏病和其他疾病,其中骨吸收介导包括类风湿性关节炎和其它形式的炎症性关节炎,骨关节炎,假体衰竭,溶骨性肉瘤,骨髓瘤和肿瘤转移至骨骼的发病率与式I化合物, 也提供。

    INHIBITORS OF C-FMS KINASE
    60.
    发明申请
    INHIBITORS OF C-FMS KINASE 有权
    C-FMS激酶抑制剂

    公开(公告)号:US20070249649A1

    公开(公告)日:2007-10-25

    申请号:US11736635

    申请日:2007-04-18

    摘要: The invention is directed to compounds of Formula I: wherein Z, X, J, R2 and W are set forth in the specification, as well as solvates, hydrates, tautomers and pharmaceutically acceptable salts thereof, that inhibit protein tyrosine kinases, especially c-fms kinase. Methods of treating autoimmune diseases; and diseases with an inflammatory component; treating metastasis from ovarian cancer, uterine cancer, breast cancer, colon cancer, stomach cancer, hairy cell leukemia and non-small lung carcinoma; and treating pain, including skeletal pain caused by tumor metastasis or osteoarthritis, or visceral, inflammatory, and neurogenic pain; as well as osteoporosis, Paget's disease, and other diseases in which bone resorption mediates morbidity including arthritis, prosthesis failure, osteolytic sarcoma, myeloma, and tumor metastasis to bone with the compounds of Formula I, are also provided.

    摘要翻译: 本发明涉及式I化合物:其中Z,X,J,R 2和W在本说明书中列出,以及溶剂合物,水合物,互变异构体及其药学上可接受的盐,其中 抑制蛋白酪氨酸激酶,特别是c-fms激酶。 治疗自身免疫性疾病的方法 和具有炎症成分的疾病; 治疗卵巢癌,子宫癌,乳腺癌,结肠癌,胃癌,毛细胞白血病和非小细胞肺癌的转移; 并治疗疼痛,包括由肿瘤转移或骨关节炎引起的骨骼疼痛,或内脏,炎症和神经源性疼痛; 还提供了骨质疏松症,佩吉特氏病和其它骨吸收介导包括关节炎,假体失败,溶骨性骨肉瘤,骨髓瘤以及与式I化合物对骨的肿瘤转移的其它疾病。