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    Inhibition of cell proliferation
    5.
    发明授权
    Inhibition of cell proliferation 有权
    抑制细胞增殖

    公开(公告)号：US08642278B2

    公开(公告)日：2014-02-04

    申请号：US11562903

    申请日：2006-11-22

    申请人： Said M. Sebti ,  Srikumar Chellappan ,  Nicholas James Lawrence

    发明人： Said M. Sebti ,  Srikumar Chellappan ,  Nicholas James Lawrence

    IPC分类号： A61K31/155 ,  A61K31/215 ,  A61K31/34 ,  A61K31/41 ,  A61K31/415 ,  A61K31/425 ,  A61K31/44 ,  A61K31/47 ,  A61K31/675 ,  C07D233/00 ,  C07D249/12

    CPC分类号： C07C323/45 ,  C07C279/06 ,  C07C335/32 ,  C07D213/53 ,  C07D215/12 ,  C07D233/30 ,  C07D233/84 ,  C07D235/28 ,  C07D249/12 ,  C07D249/14 ,  C07D277/40 ,  C07D277/42 ,  C07D317/56 ,  C07D317/58

    摘要： The disclosed modulators of Rb:Raf-1 interactions are potent, selective disruptors of Rb:Raf-1 binding, with IC50 values ranging from 80 nM to 500 nM. Further, these compounds are surprisingly effective in inhibiting a wide variety of cancer cells, including osteosarcoma, epithelial lung carcinoma, non-small cell lung carcinoma, three different pancreatic cancer cell lines, two different glioblastoma cell lines, metastatic breast cancer, melanoma, and prostate cancer. Moreover, the disclosed compounds effectively disrupt angiogenesis and significantly inhibited tumors in nude mice derived from human epithelial lung carcinoma tumors. Accordingly, the disclosed compounds, pharmaceutical compositions comprising the compounds, methods of inhibiting cell proliferation, methods of treating subjects with cancer, and methods of preparing the disclosed compounds are provided.

    摘要翻译： 所公开的Rb：Raf-1相互作用的调节剂是Rb：Raf-1结合的有效的选择性破坏剂，IC 50值范围为80nM至500nM。 此外，这些化合物令人惊奇地有效地抑制多种癌细胞，包括骨肉瘤，上皮性肺癌，非小细胞肺癌，三种不同的胰腺癌细胞系，两种不同的胶质母细胞瘤细胞系，转移性乳腺癌，黑素瘤和 前列腺癌。 此外，所公开的化合物有效地破坏了血管发生，并显着抑制了源自人上皮性肺癌肿瘤的裸鼠中的肿瘤。 因此，提供了所公开的化合物，包含该化合物的药物组合物，抑制细胞增殖的方法，治疗患有癌症的受试者的方法以及制备所公开的化合物的方法。

    Selective neurokinin antagonists
    7.
    发明授权
    Selective neurokinin antagonists 失效
    选择性神经激肽拮抗剂

    公开(公告)号：US06635630B2

    公开(公告)日：2003-10-21

    申请号：US10163663

    申请日：2002-06-06

    申请人： Neng-Yang Shih ,  Ho-Jane Shue ,  Gregory A. Reichard ,  Sunil Paliwal ,  David J. Blythin ,  John J. Piwinski ,  Dong Xiao ,  Xiao Chen

    发明人： Neng-Yang Shih ,  Ho-Jane Shue ,  Gregory A. Reichard ,  Sunil Paliwal ,  David J. Blythin ,  John J. Piwinski ,  Dong Xiao ,  Xiao Chen

    IPC分类号： A61K31330

    CPC分类号： C07D239/10 ,  C07C45/71 ,  C07C217/48 ,  C07D211/58 ,  C07D233/14 ,  C07D233/16 ,  C07D233/22 ,  C07D233/30 ,  C07D233/32 ,  C07D233/42 ,  C07D233/46 ,  C07D233/48 ,  C07D233/78 ,  C07D285/10 ,  C07D401/04 ,  C07D401/12 ,  C07D403/12 ,  C07D409/06 ,  C07D413/04 ,  C07D413/06 ,  C07D413/10 ,  C07F9/6506 ,  C07C47/575

    摘要： Compound represented by the structural formula or a pharmaceutically acceptable salt thereof, wherein Ar1 and Ar2 are optionally substituted heteroaryl or optionally substituted phenyl; X1 is —O—, —S—, —SO—, —SO2—, —NR12—, —NCOR12— or —NR12SO2R15;  is selected from the group consisting of X2 is —O—, —S— or —NR5—; Y is ═O, ═S or ═NR11; Y1 is H, C1-C6 alkyl, —NR17R13, —SCH3, R19-aryl(CH2)n6—, R19-heteroaryl-(CH2)n6—, —(CH2)n6—heterocycloalkyl, —(C1-C3)alkyl-NH—C(O)O(C1-C6)alkyl or —NHC(O)R15; R5 is H or —(CH2)n1—G, wherein n1 is 0-5, G is H, —CF3, —CHF2, —CH2F, —OH, —O—(C1-C6 alkyl), —SO2R13, —O—(C3-C8 cycloalkyl), —NR13R14, —SO2NR13R14, —NR13SO2R15, —NR13COR12, —NR12(CONR13R14), —CONR13R14, —COOR12, C3-C8 cycloalkyl, R19-aryl, R19-heteroaryl, and provided when n1=0, G is not H; R1, R2, R3 and R7 are H, alkyl, cycloalkyl, —CHF2, —CH2F or —CF3; or R1 and R2, together with the carbon to which they are attached, form an alkylene ring; or R1 and R2 together are ═O; R6 is R7 or —OH; and the remaining variables are as defined in the specification, methods of treating diseases susceptible to treatment with neurokinin antagonists with said compounds, and pharmaceutical compositions comprising said compounds are disclosed. Also disclosed are pharmaceutical compositions comprising an effective amount of a compound of claim 1, at least one pharmaceutically acceptable carrier, and in combination with an effective amount of a selective serotonin reuptake inhibitor.

    摘要翻译： 由结构式表示的化合物或其药学上可接受的盐，其中Ar 1和Ar 2是任选取代的杂芳基或任选取代的苯基; X 1是-O - ， - S - ， - SO-，-SO 2 - ，-NR 12 - ， - NR C 12 - 或-NR 12 SO 2 R 15选自X 2是-O - ， - S-或-NR 5 - ; Y是= O，= S或= NR 11; Y 1是H，C 1 -C 6烷基，-NR 17 R 13，-SCH 3，R 19 - 芳基（CH 2）n6 - （CH 2）n6 - ， - （CH 2）n 6-杂环烷基， - （C 1 -C 3）烷基-NH-C（O）O（C 1 -C 6）烷基或-NHC（O） R 15; R 5是H或 - （CH 2）n1-G，其中n1是0-5，G是H，-CF 3，-CHF 2，-CH 2 F，-OH，-O-（C 1 -C 6 烷基），-SO 2 R 13，-O-（C 3 -C 8环烷基），-NR 13 R 14，-SO 2 NR 13 R 14，-NR 13 SO 2 R 15， NR 13 R 12，-NR 12（CONR 13 R 14），-CONR 13 R 14，-COOR 12，C 3 -C 8环烷基，R 19 芳基，R 19 - 杂芳基，并且当n 1 = 0时，G不为H; R 1，R 2，R 3和R 7为H，烷基，环烷基，-CHF 2 ，-CH2F或-CF3; 或R 1和R 2与它们所连接的碳一起形成亚烷基环; 或R 1和R 2一起为= O; R 6为R 7或-OH;其余变量如本说明书中所定义，治疗易受神经激肽拮抗剂治疗的疾病的方法， 所述化合物和包含所述化合物的药物组合物。还公开了药物组合物，其包含有效量的权利要求1的化合物，至少一种药学上可接受的载体，并与有效量的选择性5-羟色胺再摄取抑制剂组合。

    Shaving composition and method of using same
    9.
    发明授权
    Shaving composition and method of using same 失效

    公开(公告)号：US3190802A

    公开(公告)日：1965-06-22

    申请号：US22752862

    申请日：1962-10-01

    申请人： BOEHRINGER SOHN INGELHEIM

    发明人： KARL ZEILE ,  HELMUT STAHLE

    IPC分类号： A61K8/49 ,  A61K31/00 ,  A61L15/44 ,  A61Q9/02 ,  C07D233/30 ,  C07D233/42 ,  C07D233/50 ,  C07F9/6506

    CPC分类号： A61K8/4946 ,  A61K31/00 ,  A61K2800/70 ,  A61Q9/02 ,  C07D233/30 ,  C07D233/42 ,  C07D233/50 ,  C07F9/65061 ,  Y10S514/93

    摘要： Compounds of the formula: wherein R represents a hydrogen atom or a C1- 4 alkyl group, Ar represents a phenyl group which is at least di-substituted, the substituents being halogen atoms and/or C1- 4 alkyl groups, and Y represents an ethylene group either unsubstituted or substituted by a methyl group, or acid-addition salts thereof, may be incorporated in pre-shave soaps.ALSO:The invention comprises compounds of the formula wherein R1 and R2, which may be the same or different, each represents a halogen atom or a C1-2 alkyl group, and non-toxic, acid-addition salts thereof, and a process for preparing compounds of the formula wherein R represents a hydrogen atom or a C1-4 alkyl group, Ar represents a phenyl group which is at least disubstituted, the substituents being halogen atoms and/or C1-4 alkyl groups, and Y represents an ethylene group either unsubstituted or substituted by a methyl group, and acid-addition salts thereof, by heating at a temperature of 100 DEG C. to 200 DEG C. for 10 to 120 minutes in the absence of a solvent, an isothiouronium salt of the formula in which R1 represents a C1-4 alkyl and X represents a chlorine, bromine or iodine atom, with an alkylene diamine of the formula H2N-Y-NH2 When the compounds of Formula II are obtained in the form of their acid-addition salts, these salts may be converted into the free bases or other acid-addition salts in known manner. 2,6 - Diethylphenyl - S - ethyl isothiouronium bromide is prepared by reacting 2,6-diethylaniline with ammonium thiocyanate to form 2,6-diethylphenyl-thiourea and heating this compound with ethyl bromide. 2,6-Dichloro-S-methyl isothiouronium iodide is prepared by reacting 2,6-dichloroaniline with ammonium thiocyanate to form 2,6-dichlorophenyl-thiourea and treating this with methyl iodide.ALSO:Pharmaceutical and cosmetic compositions comprise a compound of the formula: wherein R represents a hydrogen atom or a C1-4 alkyl group, Ar represents a phenyl group which is at least disubstituted, the substituents being halogen atoms and / or C1-4 alkyl groups and Y represents an ethylene group either unsubstituted or substituted by a methyl group, or an acid addition salt thereof, in association with an inert carrier or excipient. The pharmaceutical compositions possess vasoconstrictive activity and may be adapted for topical administration, e.g. they may be in the form of nasal drops, sprays and ointments. They may contain one or more suspending agents and, in the case of compositions for administration into the nose, also a germicide, e.g. phenyl mercury borate. The cosmetic compositions possess pilo-erecting properties and may be presented as pre-shave preparations, for example as lotions or creams. They may include one or more perfumes, preservatives, wetting agents, dispersing agents, humectants, powder bases, colouring agents or oils.

    INHIBITION OF CELL PROLIFERATION
    10.
    发明申请
    INHIBITION OF CELL PROLIFERATION 有权
    抑制细胞增殖

    公开(公告)号：US20070254318A1

    公开(公告)日：2007-11-01

    申请号：US11562903

    申请日：2006-11-22

    申请人： Said Sebti ,  Srikumar Chellappan ,  Nicholas Lawrence

    发明人： Said Sebti ,  Srikumar Chellappan ,  Nicholas Lawrence

    IPC分类号： A61K31/155 ,  A61K31/215 ,  A61K31/34 ,  A61K31/41 ,  A61K31/415 ,  A61K31/425 ,  A61K31/44 ,  A61K31/47 ,  A61K31/675 ,  C07D233/00 ,  C07D249/12 ,  C12N5/08 ,  G01N33/50

    CPC分类号： C07C323/45 ,  C07C279/06 ,  C07C335/32 ,  C07D213/53 ,  C07D215/12 ,  C07D233/30 ,  C07D233/84 ,  C07D235/28 ,  C07D249/12 ,  C07D249/14 ,  C07D277/40 ,  C07D277/42 ,  C07D317/56 ,  C07D317/58

    摘要： The disclosed modulators of Rb:Raf-1 interactions are potent, selective disruptors of Rb:Raf-1 binding, with IC50 values ranging from 80 nM to 500 nM. Further, these compounds are surprisingly effective in inhibiting a wide variety of cancer cells, including osteosarcoma, epithelial lung carcinoma, non-small cell lung carcinoma, three different pancreatic cancer cell lines, two different glioblastoma cell lines, metastatic breast cancer, melanoma, and prostate cancer. Moreover, the disclosed compounds effectively disrupt angiogenesis and significantly inhibited tumors in nude mice derived from human epithelial lung carcinoma tumors. Accordingly, the disclosed compounds, pharmaceutical compositions comprising the compounds, methods of inhibiting cell proliferation, methods of treating subjects with cancer, and methods of preparing the disclosed compounds are provided.

    摘要翻译： 所公开的Rb：Raf-1相互作用的调节剂是Rb：Raf-1结合的有效的选择性破坏剂，其中80nM至500nM的IC 50 N值。 此外，这些化合物令人惊奇地有效地抑制多种癌细胞，包括骨肉瘤，上皮性肺癌，非小细胞肺癌，三种不同的胰腺癌细胞系，两种不同的胶质母细胞瘤细胞系，转移性乳腺癌，黑素瘤和 前列腺癌。 此外，所公开的化合物有效地破坏了血管发生，并显着抑制了源自人上皮性肺癌肿瘤的裸鼠中的肿瘤。 因此，提供了所公开的化合物，包含该化合物的药物组合物，抑制细胞增殖的方法，治疗患有癌症的受试者的方法以及制备所公开的化合物的方法。