公开(公告)号：US06518315B1

公开(公告)日：2003-02-11

申请号：US09509829

申请日：2000-06-23

Applicant: Basil Don Roufogalis ,  Colin Charles Duke ,  Van Hoan Tran

Inventor： Basil Don Roufogalis ,  Colin Charles Duke ,  Van Hoan Tran

IPC: A01N3500

CPC classification number: C07D317/54 ,  C07C43/23 ,  C07C45/30 ,  C07C45/516 ,  C07C45/62 ,  C07C45/673 ,  C07C45/71 ,  C07C45/72 ,  C07C45/73 ,  C07C45/74 ,  C07C49/255 ,  C07C49/84 ,  C07C47/277

Abstract: A compound of formula (I), a pharmaceutically acceptable derivative thereof, wherein Ph is a phenyl radical R1 is H, OH, OC1-4alkyl, NO2; R2 is OH, OC1-4alkyl, OC═OC1-4alkyl or OC═OPh where the Ph can be optionally substituted by halogen, C1-3 alkyl or NO2; R1 and R2 along with the two carbon atoms of the phenyl ring to which they are attached can combine to form a 5 or 6 membered heterocyclic ring comprising 1 or 2 heteroatoms selected from O, S or N; R3 is an optionally substituted hydroycarby radical; R4 is H, CH3, OH or ═O; when R4 is ═O, then the carbon to which R4 is attached is not bonded to H; W is C(═O)—CH2, CH═CH—, CH2CO, CH(OH)—CH2, C(CH3)(OH)CH2, CH2CH(OH), CH2C(CH3)OH, CO, CHOH, C(CH3)(OH), CH2, CH2CH2; X is —CH—OH, C(CH3)OH, CH2, CH(CH3) or —C═O; Y is —CH—OH, C(CH3)OH, CH2, CH(CH3) or —C═O; provided that one of W, X or Y has an OH group.

Abstract translation: 式（I）化合物，其药学上可接受的衍生物，其中Ph是苯基R1是H，OH，OC1-4烷基，NO2; R 2是OH，OC 1-4烷基，OC = OC 1-4烷基或OC = OPh，其中Ph可以任选地被卤素，C 1-3烷基或NO 2取代; R1和R2与它们所连接的苯环的两个碳原子一起可以结合形成包含1或2个选自O，S或N的杂原子的5或6元杂环; R3是任选取代的环烃基; R4是H，CH3，OH或= O; 当R 4为= O时，R 4所连接的碳不与H键合; W是C（= O）-CH 2，CH = CH-，CH 2 CO，CH（OH）-CH 2，C（CH 3）（OH）CH 2，CH 2 CH（OH），CH 2 C（CH 3）OH，CO，CHOH，C（ CH3）（OH），CH2，CH2CH2; X是-CH-OH，C（CH 3）OH，CH 2，CH（CH 3）或-C = O; Y是-CH-OH，C（CH 3）OH，CH 2，CH（CH 3）或-C = O; 条件是W，X或Y中的一个具有OH基团。

公开(公告)号：US20120071524A1

公开(公告)日：2012-03-22

申请号：US13216927

申请日：2011-08-24

Applicant: Yan Lu ,  Chien-Ming Li ,  Zhao Wang ,  Jianjun Chen ,  Wei Li ,  James T. DALTON ,  Duane D. Miller ,  Charles Duke ,  Sunjoo Ahn

Inventor： Yan Lu ,  Chien-Ming Li ,  Zhao Wang ,  Jianjun Chen ,  Wei Li ,  James T. DALTON ,  Duane D. Miller ,  Charles Duke ,  Sunjoo Ahn

IPC: A61K31/427 ,  C07D263/32 ,  C07D413/12 ,  C07D233/22 ,  C07D403/04 ,  A61P35/02 ,  A61K31/426 ,  A61K31/421 ,  A61K31/4178 ,  A61K31/4174 ,  A61P35/00 ,  C07D277/42 ,  C07D403/12

CPC classification number: A61K31/425 ,  A61K45/06 ,  C07D263/32 ,  C07D277/24 ,  C07D277/28 ,  C07D277/56 ,  C07D417/04 ,  A61K2300/00

Abstract: The present invention relates to novel compounds having anti-cancer activity, methods of making these compounds, and their use for treating cancer and drug-resistant tumors, e.g. melanoma, metastatic melanoma, drug resistant melanoma, prostate cancer and drug resistant prostate cancer.

Abstract translation: 本发明涉及具有抗癌活性的新化合物，制备这些化合物的方法及其用于治疗癌症和药物抗性肿瘤的用途，例如， 黑素瘤，转移性黑素瘤，耐药性黑素瘤，前列腺癌和耐药前列腺癌。

公开(公告)号：US5741821A

公开(公告)日：1998-04-21

申请号：US553714

申请日：1995-11-30

Applicant: Basil Don Roufogalis ,  Colin Charles Duke ,  Qian Li

Inventor： Basil Don Roufogalis ,  Colin Charles Duke ,  Qian Li

IPC: C07D311/18 ,  A61K31/047 ,  A61K31/05 ,  A61K31/055 ,  A61K31/065 ,  A61K31/11 ,  A61K31/12 ,  A61K31/215 ,  A61K31/235 ,  A61K31/35 ,  A61K31/352 ,  A61K31/365 ,  A61K31/37 ,  A61P9/00 ,  A61P9/04 ,  A61P43/00 ,  B01J27/10 ,  C07B61/00 ,  C07C37/01 ,  C07C37/14 ,  C07C39/14 ,  C07C39/15 ,  C07C39/16 ,  C07C39/19 ,  C07C39/21 ,  C07C39/23 ,  C07C205/22 ,  C07C205/26 ,  C07D311/16 ,  C07D311/32 ,  C07C39/04

CPC classification number: C07C39/16 ,  A61K31/05 ,  A61K31/235 ,  A61K31/35 ,  A61K31/365 ,  A61K31/37 ,  C07C39/14 ,  C07D311/16

Abstract: Use of a compound of formula (I), wherein Ar is an aromatic ring system comprising one or more optionally substituted phenyl rings optionally linked to or fused with one or more other optionally substituted phenyl rings or one or more 5 or 6-membered, optionally substituted heterocyclic rings wherein the heteroatom is oxygen; and wherein the ring system comprises 1-4 phenyl rings and wherein Ar can be linked to another Ar via a group X wherein the Ar is independently selected; where X is optionally substituted C.sub.1-20 alkylene, C.sub.2-20 alkenylene or C.sub.2-20 alkynylene; R is hydrogen; C.sub.1-20 alkenyl, C.sub.2-20 alkynyl, C.sub.2-20 alkanoyl, C.sub.2-20 alkynoyl, each of which can be optionally substituted; R.sub.1 is independently selected and is hydrogen; optionally substituted C.sub.1-12 alkyl, C.sub.2-12 alkenyl, C.sub.2-20 alkynyl; --COOR'--NR'R', halogen, --OR', --COR', --CONR'R', .dbd.O, --SR', --SO.sub.3 R', --SO.sub.2 NR'R', --SOR', --SO.sub.2 R', --NO.sub.2, --CN, glycoside, silyl; where R' is independently hydrogen; alkyl, alkenyl or alkynyl each optionally substituted; and where two groups R.sub.1 can be joined; wherein the optional substituents are one or more independently selected from C.sub.1-10 alkyl, C.sub.2-10 alkenyl, C.sub.2-10 alkynyl; --COOR"--NR"R", halogen, OR", --COR", --CONR"R", --SR", .dbd.O, --SO.sub.3 R", --SO.sub.2 NR"R", --SOR", --S.sub.2 ", --NO.sub.2, --CN: wherein R" is independently hydrogen, alkyl, alkenyl, or alkynyl; n=1, 2 or 3; m=1, 2, 3 or 4; or a pharmaceutically acceptable derivative thereof in the manufacture of a medicament for inhibiting the action of Ca.sup.2+ -ATPase enzymes. Certain compounds of formula (I) and 8-lavandulyl flavone pharmaceutical formulations are new. ##STR1##