1. A compound of formula (II)
wherein
m is an integer from 0 to 3;
R10 is selected from the group consisting of hydroxy, halogen, C1-3alkyl, C1-3alkoxy, cyano, nitro, amino, (C1-4alkylamino) and di(C1-4alkyl)amino;
Y is selected from the group consisting of O and S;
R11 and R12 are each independently selected from the group consisting of hydroxy, C1-4alkyl, \u2014C(\u2014O\u2014C1-4alkyl)2, C1-4alkoxy, halogenated C1-4alkyl, halogenated C1-4alkoxy, phenyl, \u2014O-phenyl, \u2014O-aralkyl, 2-isoxazolidin-3-one and NR15R16
wherein the phenyl, whether alone or as part of a substituent group, is optionally substituted with one or more substituents independently selected from hydroxy, carboxy, halogen, C1-3alkyl, C1-3alkoxy, cyano, nitro, amino, (C1-4alkylamino) and di(C1-4alkyl)amino;
wherein R15 and R16 are each independently selected from the group consisting of hydrogen and C1-4alkyl; alternatively, R15 and R16 are taken together with the nitrogen atom to which they are bound to form a 5- to 7-membered saturated or partially unsaturated nitrogen containing heterocyclyl ring; wherein the nitrogen containing heterocyclyl ring is optionally substituted with one or more substituents independently selected from hydroxy, carboxy, C1-4alkyl, C1-4alkoxy, nitro, cyano, amino, (C1-4alkylamino) and di(C1-4alkyl)amino;
alternatively, R11 and R12 are taken together with the phosphorous atom to which they are bound to form a 5- to 7-membered saturated phosphorous containing heterocyclyl ring; wherein the phosphorous containing heterocyclyl ring is optionally substituted with one or more substituents independently selected from hydroxy, carboxy, C1-4alkyl, C1-4alkoxy, nitro, cyano, amino, (C1-4alkylamino) and di(C1-4alkyl)amino;
R13 is selected from the group consisting of \u2014NR17R18; \u2014O\u2014R19 and \u2014S(O)0-2\u2014R20;
wherein R17 and R18 are each independently selected from the group consisting of hydrogen and C1-4alkyl; alternatively, R17 and R18 are taken together with the nitrogen atom to which they are bound to form a 5- to 7-membered saturated nitrogen containing heterocyclyl ring; wherein the nitrogen containing heterocyclyl ring is optionally substituted with one or more substituents independently selected from the group consisting of hydroxy, carboxy, C1-4alkyl, C1-4alkoxy, nitro, cyano, amino, (C1-4alkylamino) and di(C1-4alkyl)amino;
R19 is selected from the group consisting of C1-4alkyl, \u2014C(O)\u2014C1-4alkyl and \u2014C(O)-phenyl;
R20 is selected from the group consisting of hydrogen and C1-4alkyl;
or a pharmaceutically acceptable salt, ester or prodrug thereof.
2. A compound as in claim 1, wherein
m is an integer from 0 to 1;
R10 is selected from the group consisting of hydroxy, halogen and C1-3alkyl, C1-3alkoxy;
Y is O;
R11 and R12 are each independently selected from the group consisting of C1-4alkyl, C1-4alkoxy, fluorinated C1-4alkyl, fluorinated C1-4alkoxy, phenyl, 2-isoxazolidin-3-one and NR15R16; wherein R15 and R16 are each independently selected from C1-3alkyl;
wherein the phenyl, whether alone or as part of a substituent group, is optionally substituted with one to two substituents independently selected from hydroxy, carboxy, halogen, C1-3alkyl and C1-3alkoxy;
wherein R15 and R16 are each independently selected from the group consisting of hydrogen and C1-4alkyl; alternatively, R15 and R16 are taken together with the nitrogen atom to which they are bound to form a 5- to 6-membered saturated nitrogen containing heterocyclyl ring; wherein the nitrogen containing heterocyclyl ring is optionally substituted with one to two substituents independently selected from hydroxy, C1-4alkyl and C1-4alkoxy;
R13 is selected from the group consisting of \u2014NR17R18, \u2014O\u2014R19 and \u2014S\u2014R20;
wherein R17 and R18 are each independently selected from C1-3alkyl;
wherein R17 and R18 are each independently selected from the group consisting of hydrogen and C1-4alkyl; alternatively, R17 and R11 are taken together with the nitrogen atom to which they are bound to form a 5- to 6-saturated membered nitrogen containing heterocyclyl ring; wherein the nitrogen containing heterocyclyl ring is optionally substituted with one to two substituents independently selected from the group consisting of hydroxy, C1-4alkyl and C1-4alkoxy;
R19 is selected from the group consisting of C1-4alkyl and \u2014C(O)\u2014C1-3alkyl;
R20 is selected from the group consisting of hydrogen and C1-4alkyl;
or a pharmaceutically acceptable salt, ester or prodrug thereof.
3. A compound as in claim 2, wherein
m is 0;
Y is O;
R11 is selected from the group consisting of C1-3alkyl, C1-3alkoxy, phenyl, 2-isoxazolidin-3-one and NR15R16; wherein R15 and R16 are each independently selected from C1-3alkyl;
R12 is selected from the group consisting of C1-3alkyl, C1-3alkoxy, phenyl and NR15R16; wherein R15 and R16 are each independently selected from C1-3alkyl;
R13 is selected from the group consisting of \u2014NR17R17, \u2014O\u2014R19 and \u2014S\u2014R20;
wherein R17 and R18 are each independently selected from C1-3alkyl;
R19 is selected from C1-3alkyl;
R20 is selected from C1-3alkyl;
or a pharmaceutically acceptable salt, ester or prodrug thereof.
4. A compound as in claim 3, wherein
m is 0;
Y is O;
R11 is selected from the group consisting of methyl, methoxy, ethoxy, phenyl, 2-isooxazolidin-3-one and dimethylamino;
R12 is selected from the group consisting of methyl, methoxy, ethoxy, phenyl, 2-isooxazolidin-3-one and dimethylamino;
R13 is selected from the group consisting of \u2014N(CH3)2, \u2014O\u2014CH3 and \u2014S\u2014CH3;
or a pharmaceutically acceptable salt, ester or prodrug thereof.
5. A compound as in claim 4, wherein
m is 0;
Y is O;
R11 is selected from the group consisting of methyl, methoxy, ethoxy and phenyl;
R12 is selected from the group consisting of methyl, methoxy, ethoxy and phenyl;
R13 is selected from the group consisting of \u2014N(CH3)2 and \u2014S\u2014CH3;
or a pharmaceutically acceptable salt thereof.
6. A compound as in claim 4, wherein
m is 0;
Y is O;
R11 is selected from the group consisting of methyl, methoxy, ethoxy, phenyl and 2-isooxazolidin-3-one;
R12 is selected from the group consisting of methyl, methoxy, ethoxy, phenyl and 2-isooxazolidin-3-one;
R13 is selected from the group consisting of \u2014N(CH3)2 and \u2014O\u2014CH3;
or a pharmaceutically acceptable salt thereof.
7. A pharmaceutical composition comprising a pharmaceutically acceptable carrier and a compound of claim 1.
8. A pharmaceutical composition made by mixing a compound of claim 1 and a pharmaceutically acceptable carrier.
9. A process for making a pharmaceutical composition comprising mixing a compound of claim 1 and a pharmaceutically acceptable carrier.
10. A method of treating a disorder mediated by a progesterone or glucocorticoid receptor, comprising administering to a subject in need thereof a therapeutically effective amount of the compound of claim 1.
11. A method of contraception comprising administering to a subject in need thereof a therapeutically effective amount of the compound of claim 1.
12. The method of claim 10, wherein the disorder mediated by the progesterone receptor is selected from the group consisting of secondary amenorrhea; dysfunctional bleeding; uterine leiomyomata; endometriosis; polycystic ovary syndrome; carcinoma of the endometrium, carcinoma of the ovary, carcinoma of the breast, carcinoma of the colon, carcinoma of the prostate, adenocarcinomas of the ovary, adenocarcinomas of the breast, adenocarcinomas of the colon, adenocarcinomas of the prostate and side effects of cyclic menstrual bleeding.
13. The method of claim 10, wherein the disorder mediated by the glucocorticoid receptor is selected from the group consisting of Type II diabetes mellitus, impaired oral glucose tolerance, elevated blood glucose levels and Syndrome X.
14. A method of treating a disorder mediated by a progesterone or glucocorticoid receptor comprising administering to a subject in need thereof a therapeutically effective amount of the composition of claim 7.
15. The use of a compound as in claim 1 for the preparation of a medicament for treating: (a) secondary amenorrhea; (b) dysfunctional bleeding; (c) uterine leiomyomata; (d) endometriosis; (e) polycystic ovary syndrome; (f) carcinoma of the endometrium, (g) carcinoma of the ovary, (h) carcinoma of the breast, (i) carcinoma of the colon, (j) carcinoma of the prostate, (k) adenocarcinomas of the ovary, (l) adenocarcinomas of the breast, (m) adenocarcinomas of the colon, (n) adenocarcinomas of the prostate, (O) side effects of cyclic menstrual bleeding, (p) Type II diabetes mellitus, (q) impaired oral glucose tolerance, (r) elevated blood glucose levels, (s) Syndrome X or (t) for contraception, in a subject in need thereof.
16. The compound formula (III)
or a pharmaceutically acceptable salt, ester or prodrug thereof.
The claims below are in addition to those above.
All refrences to claim(s) which appear below refer to the numbering after this setence.
1. A light source module comprising:(a) two lighting seat bodies each equipped with light-emitting diode, the light-emitting diode being connected with a lighting circuit; and (b) a light guide medium, at least one face of the light guide medium being defined as an incident face right facing light-projecting faces of the light-emitting diode, a back face of the light guide medium being printed with ink to form multiple reflective sections, whereby the light coming into the light guide medium and going to the reflective sections is reflected by the reflective sections to a front face of the light guide medium and goes out from the front face, and wherein the lighting circuit, arranged in each of the two lighting seat bodies, includes a pair of electrodes protruding from the lighting circuit with a specification of a common fluorescent lamp.
2. The light source module as claimed in claim 1, further comprising a reflective shade attached to all faces of the light guide medium except the front face and the incident face.
3. The light source module as claimed in claim 1, wherein the two lighting seat bodies tightly fitted on two opposite ends of the light guide medium.
4. The light source module as claimed in claim 3, wherein an outer cover is fitted between the two lighting seat bodies to enclose the light guide medium, the outer cover being a transparent circular tube.
5. The light source module as claimed in claim 1, wherein one end of said each of the two lighting seat bodies is formed with a socket in which one end of the light guide medium is inserted.
6. The light source module as claimed in claim 1, wherein a fitting section is formed on outer circumference of said each of the two lighting seat bodies, two ends of a transparent outer cover being fitted on the corresponding fitting sections of said each of the two lighting seal bodies to enclose the light guide medium.
7. The light source module as claimed in claim 1, wherein the front face of the light guide medium is aligned with and faces a glass layer of a display.
8. A light source module comprising:(a) two lighting seat bodies each equipped with a light-emitting diode, the light-emitting diode being connected with a lighting circuit; and (b) a light guide medium, at least one face of the light guide medium being defined as an incident face right facing light-projecting faces of the light-emitting diode, a back face of the light guide medium being printed with ink to form multiple reflective sections, whereby the light coming into the light guide medium and going to the reflective sections is reflected by the reflective sections to a front face of the light guide medium and goes out from the front face, and wherein an outer cover is fitted between the two lighting seat bodies to enclose the light guide medium, the outer cover being a tubular body with C-shaped cross-section, the outer cover having a longitudinal split corresponding to the front face of the light guide medium.
9. The light source module as claimed in claim 8, wherein the two lighting seat bodies tightly fitted on two opposite ends of the light guide medium.
10. The light source module as claimed in claim 8, wherein one end of each of the two lighting seat bodies is formed with a socket in which one end of the light guide medium is inserted.