We claim:
1. An optical bus comprising:
an enclosure having at least a first side and a second side each comprising a semiconductor structure, wherein the semiconductor structure comprises:
a monocrystalline silicon substrate;
an amorphous oxide material overlying the monocrystalline substrate;
a monocrystalline perovskite oxide material overlying the amorphous oxide material; and
a monocrystalline compound semiconductor material overlying the monocrystalline perovskite oxide material;
a first source-detector pair formed within the semiconductor structure of the first side, wherein the first source-detector pair comprises a first semiconductor optical source and a first semiconductor optical detector; and
a second source-detector pair formed within the semiconductor structure of the second side, wherein the second source-detector pair comprises a second semiconductor optical source and a second semiconductor optical detector.
2. The optical bus of claim 1, wherein the second semiconductor optical detector is capable of detecting emissions from the first semiconductor optical source.
3. The optical bus of claim 1, wherein one or more inner surfaces of the enclosure are substantially nonreflective to emissions from the first and second semiconductor optical sources.
4. The optical bus of claim 1, wherein the first side has multiple source-detector pairs each having a semiconductor optical source and a semiconductor optical detector formed within the semiconductor structure, and the second side has an inner surface wherein at least a portion of the inner surface is at least partially reflective to emissions from the semiconductor optical sources.
5. The optical bus of claim 4, wherein two or more of the multiple source-detector pairs are electrically interconnected.
6. The optical bus of claim 4, wherein the at least partially reflective portion of the inner surface is shaped to compensate for signal latency.
7. The optical bus of claim 1, wherein at least one semiconductor optical detector is one of a Group IV semiconductor optical device and a compound semiconductor optical device.
8. The optical bus of claim 1, wherein at least one semiconductor optical source is one of a Group IV semiconductor optical device and a compound semiconductor optical device.
9. The optical bus of claim 1 further comprising a emission-dispersing material over at least one of the semiconductor optical sources.
10. The optical bus of claim 9, wherein the emission-dispersing material is one of a transparent, dielectric encapsulate having a high index of refraction, and a transparent, polymeric encapsulate embedded with particles, wherein the particles have an index of refraction different from the polymeric material.
11. The optical bus of claim 1, wherein the first source-pair is coupled to a first device external to the optical bus and the second source-detector pair is coupled to a second device external to the optical bus, wherein the first device transmits information to the second device via the second semiconductor optical detector detecting emissions from the first semiconductor optical source.
12. The optical bus of claim 1 further comprising processing circuitry formed at least partially within the semiconductor structure.
13. An optical bus comprising:
a first side having a first surface, the first side comprising a semiconductor structure, wherein the semiconductor structure comprises:
a monocrystalline silicon substrate;
an amorphous oxide material overlying the monocrystalline substrate;
a monocrystalline perovskite oxide material overlying the amorphous oxide material; and
a monocrystalline compound semiconductor material overlying the monocrystalline perovskite oxide material;
a first and second source-detector pair formed within the semiconductor structure, wherein each source-detector pair comprises a semiconductor optical source and a semiconductor optical detector; and
a second side having a second surface, wherein at least a portion of the second surface is at least partially reflective to emissions from one or more of the semiconductor optical sources;
wherein one or more of the semiconductor optical detectors are capable of detecting the reflected emissions, and wherein the first and second surfaces are closed off to external radiative emissions.
14. The optical bus of claim 13, wherein one or more of the first surface and the second surface comprise an emission-dispersing material.
15. The optical bus of claim 13, wherein the at least partially reflective portion of the second surface is shaped to compensate for signal latency.
16. The optical bus of claim 13, wherein one or more of the first surface and the second surface are partially absorptive to the emissions.
17. The optical bus of claim 13, wherein the second side comprises the semiconductor structure, the optical bus further comprising one or more source-detector pairs formed within the semiconductor structure of the second side.
18. The optical bus of claim 17, wherein at least a portion of the first surface is at least partially reflective to emissions from the one or more of the semiconductor optical sources of the second side.
19. The optical bus of claim 18, wherein the at least partially reflective portion of the first surface is shaped to compensate for signal latency.
20. A process for fabricating an optical bus comprising:
forming one or more source-detector pairs from a semiconductor structure, the step of forming comprising the steps of:
providing a monocrystalline silicon substrate;
depositing a monocrystalline perovskite oxide film overlying the second region of the monocrystalline silicon substrate, the film having a thickness less than a thickness of the material that would result in strain-induced defects;
forming an amorphous oxide interface layer at an interface between the monocrystalline perovskite oxide film and the monocrystalline silicon substrate;
epitaxially forming a monocrystalline compound semiconductor layer overlying the monocrystalline perovskite oxide film; and
forming one or more optical devices within the monocrystalline compound semiconductor layer, wherein each optical device is one of an optical detector and an optical source;
forming an enclosure using the semiconductor structure, wherein the one or more optical devices face an inside of the enclosure; and
sealing the enclosure off from external radiative emissions.
21. The method of claim 20, wherein the step of forming one or more source-detector pairs further comprises the step of forming one or more optical devices at least partially within the monocrystalline silicon substrate in a region wherein each optical device is one of an optical detector and an optical source.
22. The method of claim 20, wherein the step of forming an enclosure comprises joining each edge of the semiconductor structure with an edge of another semiconductor structure to form a polyhedral structure.
23. The method of claim 22, wherein each semiconductor structure comprises one or more optical devices within the monocrystalline compound semiconductor layer, wherein each optical device is one of an optical detector and an optical source.
24. The method of claim 20, wherein the step of forming an enclosure comprises etching the enclosure from the semiconductor structure and exposing the one or more optical devices to the enclosure.
25. The method of claim 20 further comprising the step of providing a surface at least partially reflective to emissions from the optical source, wherein the step of forming an enclosure comprises spacing the surface substantially parallel to and apart from the semiconductor structure with the one or more optical devices facing the surface.
26. The method of claim 25, wherein the at least partially reflective surface is shaped to compensate for signal latency.
27. A method of communication between devices using an optical bus comprising:
generating a signal at a first device;
generating radiative emissions from an optical source in response to the signal, the optical source formed within a semiconductor structure comprising a monocrystalline silicon substrate, an amorphous oxide material overlying the monocrystalline substrate, a monocrystalline perovskite oxide material overlying the amorphous oxide material, and a monocrystalline compound semiconductor material overlying the monocrystalline perovskite oxide material;
detecting the radiative emissions at an optical detector formed within a second semiconductor structure comprising a monocrystalline silicon substrate, an amorphous oxide material overlying the monocrystalline substrate, a monocrystalline perovskite oxide material overlying the amorphous oxide material, and a monocrystalline compound semiconductor material overlying the monocrystalline perovskite oxide material;
re-generating the signal from the radiative emissions; and
transmitting the re-generated signal to a second device.
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 compound of structural formula I:
a pharmaceutically acceptable salt or a stereoisomer thereof,
wherein:
X is hydrogen, or halogen;
Z is hydrogen, CF3, carbonyl C1-3 alkyl, C1-4 alkoxy, halogen, C1-3 alkyl, and hydroxymethyl, wherein said alkyl, and alkoxy are optionally substituted with one to seven fluorine atoms;
represents a group chosen from pyridinyl and quinolyl
R1, R2, R3, and R4 are each independently chosen from:
hydrogen,
halogen,
C1-8 alkyl,
amino C0-6alkyl,
C1-6 alkylamino C0-6alkyl,
(C1-6 alkyl)2amino C0-6alkyl,
C1-6 alkoxy C0-6alkyl,
hydroxycarbonyl C0-6alkyl,
C1-6 alkoxycarbonyl C0-6alkyl,
hydroxycarbonyl C1-6 alkyloxy,
hydroxy C0-6alkyl,
cyano,
perfluoroC1-4alkyl,
perfluoroC1-4alkoxy,
C0-6 alkylcarbonyl,
C1-6 alkylcarbonyloxy,
C1-6 alkylcarbonylamino,
C1-6 alkylsulfonylamino,
C1-6 alkoxycarbonylamino,
C1-6alkylaminocarbonylamino,
(C1-6alkyl)2aminocarbonylamino, and
(C1-6alkyl)2aminocarbonyloxy,
wherein
R1 and R2 together with the carbon atom to which they are attached can optionally form a spiro-C3-6 cycloalkyl group, or an oxo group, and
R3 and R4 together with the carbon atom to which they are attached can optionally form a spiro-C3-6 cycloalkyl group, or an oxo group, and
R1, R2, R3, and R4 are each independently optionally substituted with one or more R9;
R5, R6, and R7 are each independently chosen from:
hydrogen,
halogen,
(carbonyl)0-1C1-10 alkyl,
(carbonyl)0-1C2-10 alkenyl,
(carbonyl)0-1C2-10 alkynyl,
(carbonyl)0-1aryl C1-10 alkyl,
C3-8 cycloalkyl C0-10 alkyl(carbonyl)0-1,
(C3-8)heterocyclyl C0-10 alkyl(carbonyl)0-1,
C1-4acylamino C0-10 alkyl,
C0-10 alkylamino C0-10 alkyl,
C0-10 alkylamino C0-10 alkylaminocarbonyl,
di-(C1-10 alkyl)amino C0-10 alkyl,
arylC0-10 alkylamino C0-10 alkyl,
(arylC0-10alkyl)2amino C0-10 alkyl,
C3-8 cycloalkyl C0-10 alkylamino C0-10 alkyl,
C3-8 heterocyclyl C0-10 alkylamino C0-10 alkyl,
(C3-8 cycloalkyl C0-10 alkyl)2amino C0-10 alkyl,
(C3-8 heterocyclyl C0-10 alkyl)2amino C0-10 alkyl,
C3-8 cycloalkyl C0-10 alkyl aminocarbonylamino,
(C1-10 alkyl)2aminocarbonylamino,
(aryl C1-10alkyl)1-2aminocarbonylamino,
C0-10 alkyl aminocarbonylamino,
C3-8 heterocyclyl C0-10 alkyl aminocarbonylamino,
(C1-10alkyl)1-2aminocarbonyl C0-10 alkyl,
(aryl C1-10 alkyl)1-2aminocarbonyl C0-10 alkyl,
C0-10 alkyl aminocarbonyl C0-10 alkyl,
C3-8 cycloalkyl C0-10 alkyl aminocarbonyl C0-10 alkyl,
C3-8 heterocyclyl C0-10 alkyl aminocarbonyl C0-10 alkyl,
aryl C0-10 alkyl aminocarbonyl C0-10 alkyl,
(C1-10 alkyl)2aminocarbonyl,
(aryl C1-10 alkyl)1-2aminocarbonyl,
C1-10 alkoxy (carbonyl)0-1C0-10 alkyl,
C0-10 alkyl carbonylamino(C0-10 alkyl),
C0-10 alkoxy carbonylamino(C0-10 alkyl),
carboxy C0-10 alkylamino,
carboxy C0-10 alkyl,
carboxy aryl,
carboxy C3-8 cycloalkyl,
carboxy C3-8 heterocyclyl,
C1-10 alkoxy,
C1-10alkyloxy C0-10alkyl
C1-10 alkylcarbonyloxy,
C3-8 heterocyclyl C0-10 alkylcarbonyloxy,
C3-8 cycloalkyl C0-10 alkylcarbonyloxy,
aryl C0-10 alkylcarbonyloxy,
C1-10 alkylcarbonyloxy amino,
C3-8 heterocyclyl C0-10 alkylcarbonyloxy amino,
C3-8 cycloalkyl C0-10 alkylcarbonyloxy amino,
aryl C0-10 alkylcarbonyloxy amino,
(C1-10alkyl)2aminocarbonyloxy,
(aryl C0-10alkyl)1-2aminocarbonyloxy,
(C3-8 heterocyclyl C0-10 alkyl)1-2aminocarbonyloxy,
(C3-8 cycloalkyl C0-10alkyl)1-2aminocarbonyloxy,
hydroxy C0-10alkyl,
hydroxycarbonylC0-10alkoxy,
hydroxycarbonylC0-10alkyloxy,
C1-10 alkylthio,
C1-10 alkylsulfinyl,
aryl C0-10 alkylsulfinyl,
C3-8 heterocyclyl C0-10 alkylsulfinyl,
C3-8 cycloalkyl C0-10 alkylsulfinyl,
C1-10 alkylsulfonyl,
aryl C0-10 alkylsulfonyl,
C3-8 heterocyclyl C0-10 alkylsulfonyl,
C3-8 cycloalkyl C0-10 alkylsulfonyl,
C1-10 alkylsulfonylamino,
aryl C1-10 alkylsulfonylamino,
C3-8 heterocyclyl C1-10 alkylsulfonylamino,
C3-8 cycloalkyl C1-10 alkylsulfonylamino,
cyano,
nitro,
perfluoroC1-6alkyl, and
perfluoroC1-6alkoxy,
R5, R6, and R7 are each independently optionally substituted with one or more R9;
R8 is chosen from:
hydrogen,
halogen,
(carbonyl)0-1C1-10 alkyl,
(carbonyl)0-1C2-10 alkenyl,
(carbonyl)0-1C2-10 alkynyl,
(carbonyl)0-1aryl C1-10 alkyl,
C3-8 cycloalkyl C0-10 alkyl(carbonyl)0-1,
C1-4acylamino C0-10 alkyl,
C0-10 alkylamino C0-10 alkyl,
C0-10 alkylamino C0-10 alkylaminocarbonyl,
di-(C1-10 alkyl)amino C0-10 alkyl,
arylC0-10 alkylamino C1-10 alkyl,
(arylC0-10 alkyl)2amino C0-10 alkyl,
C3-8 cycloalkyl C0-10 alkylamino C0-10 alkyl,
C3-8 heterocyclyl C0-10 alkylamino C0-10 alkyl,
(C3-8 cycloalkyl C0-10 alkyl)2amino C0-10 alkyl,
(C3-8 heterocyclyl C0-10 alkyl)2amino C0-10 alkyl,
C3-8 cycloalkyl C0-10 alkyl aminocarbonylamino,
(C1-10 alkyl)2aminocarbonylamino,
(aryl C1-10 alkyl)1-2aminocarbonylamino,
C0-10 alkyl aminocarbonylamino,
C3-8 heterocyclyl C0-10 alkyl aminocarbonylamino,
(C1-10 alkyl)2aminocarbonyl C0-10 alkyl,
(aryl C1-10 alkyl)1-2aminocarbonyl C0-10alkyl,
C0-10 alkyl aminocarbonyl C0-10 alkyl,
C3-8 cycloalkyl C0-10 alkyl aminocarbonyl C0-10 alkyl,
C3-8 heterocyclyl C0-10 alkyl aminocarbonyl C0-10 alkyl,
aryl C0-10 alkyl aminocarbonyl C0-10 alkyl,
(C1-10 alkyl)2aminocarbonyl,
(aryl C1-10 alkyl)1-2aminocarbonyl,
C1-10 alkoxy (carbonyl)0-1C0-10 alkyl,
C0-10 alkyl carbonylamino(C0-10 alkyl),
C0-10 alkoxy carbonylamino(C0-10 alkyl),
carboxy C0-10 alkylamino,
carboxy C0-10 alkyl,
carboxy C3-8 cycloalkyl,
C1-10 alkoxy,
C1-10 alkyloxy C0-10 alkyl
C1-10 alkylcarbonyloxy,
C3-8 heterocyclyl C0-10 alkylcarbonyloxy,
C3-8 cycloalkyl C0-10 alkylcarbonyloxy,
aryl C0-10 alkylcarbonyloxy,
C1-10 alkylcarbonyloxy amino,
C3-8 heterocyclyl C0-10 alkylcarbonyloxy amino,
C3-8 cycloalkyl C0-10 alkylcarbonyloxy amino,
aryl C0-10 alkylcarbonyloxy amino,
(C1-10 alkyl)2aminocarbonyloxy,
(aryl C0-10 alkyl)1-2aminocarbonyloxy,
(C3-8 heterocyclyl C0-10alkyl)1-2aminocarbonyloxy,
(C3-8 cycloalkyl C0-10 alkyl)1-2aminocarbonyloxy,
hydroxy C0-10 alkyl,
hydroxycarbonylC0-10 alkoxy,
hydroxycarbonylC0-10 alkyloxy,
C1-10 alkylthio,
C1-10 alkylsulfinyl,
aryl C0-10 alkylsulfinyl,
C3-8 heterocyclyl C0-10alkylsulfinyl,
C3-8 cycloalkyl C0-10 alkylsulfinyl,
C1-10 alkylsulfonyl,
aryl C0-10 alkylsulfonyl,
C3-8 heterocyclyl C0-10 alkylsulfonyl,
C3-8 cycloalkyl C0-10 alkylsulfonyl,
C1-10 alkylsulfonylamino,
aryl C1-10 alkylsulfonylamino,
C3-8 heterocyclyl C1-10 alkylsulfonylamino,
C3-8 cycloalkyl C1-10 alkylsulfonylamino,
cyano,
nitro,
perfluoroC1-6alkyl, and
perfluoroC1-6alkoxy;
wherein R8 is optionally substituted with one or more R9; and
R9 is chosen from:
hydrogen,
halogen,
(carbonyl)0-1C1-10 alkyl,
(carbonyl)0-1C2-10 alkenyl,
(carbonyl)0-1C2-10 alkynyl,
(carbonyl)0-1aryl C1-10 alkyl,
C3-8 cycloalkyl C0-10 alkyl,
(C3-8)heterocyclyl C0-10 alkyl,
C1-4acylamino C0-10 alkyl,
C0-10 alkylamino C0-10 alkyl,
di-(C1-10 alkyl)amino C0-10 alkyl,
arylC0-10 alkylamino C0-10 alkyl,
(arylC0-10 alkyl)2amino C0-1 alkyl,
C3-8 cycloalkyl C0-10 alkylamino C0-10 alkyl,
C3-8 heterocyclyl C0-10 alkylamino C0-10 alkyl,
(C1-10 alkyl)2aminocarbonyl,
C1-10 alkoxy (carbonyl)0-1C0-10 alkyl,
C1-10alkyloxy C0-10 alkyl,
(C1-10 alkyl)2aminocarbonyloxy,
hydroxycarbonylC0-10alkoxy,
(C1-10 alkyl)2aminocarbonyloxy,
(aryl C0-10 alkyl)1-2aminocarbonyloxy,
hydroxy C0-10alkyl,
C1-10 alkylsulfonyl,
C1-10 alkylsulfonylamino,
aryl C1-10 alkylsulfonylamino,
C3-8 heterocyclyl C1-10 alkylsulfonylamino,
C3-8 cycloalkyl C1-10 alkylsulfonylamino,
cyano,
nitro,
perfluoroC1-6alkyl, and
perfluoroC1-6alkoxy, and
wherein, R9 is optionally substituted with one or more groups selected from hydrogen, OH, (C1-6)alkoxy, halogen, CO2H, CN, O(C\u2550O)C1-C6 alkyl, NO2, trifluoromethoxy, trifluoroethoxy, \u2014Ob(C1-10)perfluoroalkyl, and NH2.
2. A compound according to claim 1, wherein X is halogen and Z is C1-3 alkyl optionally substituted with one to seven fluorine atoms.
3. A compound according to claim 1 having a structural formula II:
a pharmaceutically acceptable salt or a stereoisomer thereof,
wherein:
represents a group chosen from pyridinyl and quinolyl
R1, R2, R3, and R4 are each independently chosen from:
hydrogen,
halogen,
C1-8 alkyl,
amino C0-6alkyl,
C1-6 alkylamino C0-6alkyl,
(C1-6 alkyl)2amino C0-6alkyl,
C1-6 alkoxy C0-6 alkyl,
hydroxycarbonyl C0-6alkyl,
C1-6 alkoxycarbonyl C0-6alkyl,
hydroxycarbonyl C1-6 alkyloxy,
hydroxy C0-6alkyl,
cyano,
perfluoroC1-4alkyl,
perfluoroC1-4alkoxy,
C0-6 alkylcarbonyl,
C1-6 alkylcarbonyloxy,
C1-6 alkylcarbonylamino,
C1-6 alkylsulfonylamino,
C1-6 alkoxycarbonylamino,
C1-6alkylaminocarbonylamino,
(C1-6 alkyl)2aminocarbonylamino, and
(C1-6 alkyl)2aminocarbonyloxy,
and wherein
R1 and R2 together with the carbon atom to which they are attached can optionally form a spiro-C3-6 cycloalkyl group, or an oxo group,
R3 and R4 together with the carbon atom to which they are attached can optionally form a spiro-C3-6 cycloalkyl group, or an oxo group, and
R1, R2, R3, and R4 are each independently optionally substituted with one or more R9;
R5, R6, and R7 are each independently chosen from:
hydrogen,
halogen,
(carbonyl)0-1C1-10 alkyl,
(carbonyl)0-1C2-10 alkenyl,
(carbonyl)0-1C2-10 alkynyl,
(carbonyl)0-1aryl C1-10 alkyl,
C3-8 cycloalkyl C0-10 alkyl(carbonyl)0-1,
(C3-8)heterocyclyl C0-10 alkyl(carbonyl)0-1,
C1-4acylamino C0-10 alkyl,
C0-10 alkylamino C0-10 alkyl,
C0-10 alkylamino C0-10 alkylaminocarbonyl,
di-C1-10 alkyl)amino C0-10 alkyl,
arylC0-10 alkylamino C0-10 alkyl,
(arylC0-10 alkyl)2amino C0-10 alkyl,
C3-8 cycloalkyl C0-10 alkylamino C0-10 alkyl,
C3-8 heterocyclyl C0-10 alkylamino C0-10 alkyl,
(C3-8 cycloalkyl C0-10 alkyl)2amino C0-10 alkyl,
(C3-8 heterocyclyl C0-10 alkyl)2amino C0-10 alkyl,
C3-8 cycloalkyl C0-10 alkyl aminocarbonylamino,
(C1-10 alkyl)2aminocarbonylamino,
(aryl C1-10 alkyl)1-2aminocarbonylamino,
C0-10 alkyl aminocarbonylamino,
C3-8 heterocyclyl C0-10 alkyl aminocarbonylamino,
(C1-10 alkyl)2aminocarbonyl C0-10 alkyl,
(aryl C1-10 alkyl)1-2aminocarbonyl C0-10 alkyl,
C0-10 alkyl aminocarbonyl C0-10 alkyl,
C3-8 cycloalkyl C1-10 alkyl aminocarbonyl C0-10 alkyl,
C3-8 heterocyclyl C0-10 alkyl aminocarbonyl C0-10 alkyl,
aryl C0-10 alkyl aminocarbonyl C1-10 alkyl,
(C1-10 alkyl)2aminocarbonyl,
(aryl C1-10 alkyl)1-2aminocarbonyl,
C1-10 alkoxy (carbonyl)0-1C0-10 alkyl,
C0-10 alkyl carbonylamino(CO10 alkyl),
C0-10 alkoxy carbonylamino(C0-10 alkyl),
carboxy C0-10 alkylamino,
carboxy C0-10 alkyl,
carboxy aryl,
carboxy C3-8 cycloalkyl,
carboxy C3-8 heterocyclyl,
C1-10 alkoxy,
C1-10alkyloxy C0-10alkyl
C1-10 alkylcarbonyloxy,
C3-8 heterocyclyl C0-10 alkylcarbonyloxy,
C3-8 cycloalkyl C0-10 alkylcarbonyloxy,
aryl C0-10 alkylcarbonyloxy,
C1-10 alkylcarbonyloxy amino,
C3-8 heterocyclyl C0-10 alkylcarbonyloxy amino,
C3-8 cycloalkyl C0-10 alkylcarbonyloxy amino,
aryl C0-10 alkylcarbonyloxy amino,
(C1-10 alkyl)2aminocarbonyloxy,
(aryl C0-10 alkyl)1-2aminocarbonyloxy,
(C3-8 heterocyclyl C0-10 alkyl)1-2aminocarbonyloxy,
(C3-8 cycloalkyl C0-10 alkyl)1-2aminocarbonyloxy,
hydroxy C0-10 alkyl,
hydroxycarbonylC0-10alkoxy,
hydroxycarbonylC0-10alkyloxy,
C1-10 alkylthio,
C1-10 alkylsulfinyl,
aryl C0-10 alkylsulfinyl,
C3-8 heterocyclyl C0-10 alkylsulfinyl,
C3-8 cycloalkyl C0-10 alkylsulfinyl,
C1-10 alkylsulfonyl,
aryl C0-10 alkylsulfonyl,
C3-8 heterocyclyl C0-10 alkylsulfonyl,
C3-8 cycloalkyl C0-10 alkylsulfonyl,
C1-10 alkylsulfonylamino,
aryl C1-10 alkylsulfonylamino,
C3-8 heterocyclyl C1-10 alkylsulfonylamino,
C3-8 cycloalkyl C1-10 alkylsulfonylamino,
cyano,
nitro,
perfluoroC1-6 alkyl, and
perfluoroC1-6 alkoxy, and
R5, R6, and R7 are each independently optionally substituted with one or more R9;
R8 is chosen from:
hydrogen,
halogen,
(carbonyl)0-1C1-10 alkyl,
(carbonyl)0-1C2-10 alkenyl,
(carbonyl)0-1C2-10 alkynyl,
(carbonyl)0-1aryl C1-10 alkyl,
C3-8 cycloalkyl C0-10 alkyl(carbonyl)0-1,
C1-4acylamino C0-10 alkyl,
C0-10 alkylamino C0-10 alkyl,
C0-10 alkylamino C0-10 alkylaminocarbonyl,
di-(C1-10 alkyl)amino C0-10 alkyl,
arylC0-10 alkylamino C0-10 alkyl,
(arylC0-10 alkyl)2amino C0-10 alkyl,
C3-8 cycloalkyl C0-10 alkylamino C0-10 alkyl,
C3-8 heterocyclyl C0-10 alkylamino C0-10 alkyl,
(C3-8 cycloalkyl C0-10 alkyl)2amino C0-10 alkyl,
(C3-8 heterocyclyl C0-10 alkyl)2amino C0-10 alkyl,
C3-8 cycloalkyl C0-1 alkyl aminocarbonylamino,
(C1-10 alkyl)2aminocarbonylamino,
(aryl C1-10 alkyl)1-2aminocarbonylamino,
C0-10 alkyl aminocarbonylamino,
C3-8 heterocyclyl C0-10 alkyl aminocarbonylamino,
(C1-10 alkyl)2aminocarbonyl C0-10 alkyl,
(aryl C1-10 alkyl)1-2aminocarbonyl C1-10 alkyl,
C0-10 alkyl aminocarbonyl C0-10 alkyl,
C3-8 cycloalkyl C0-10 alkyl aminocarbonyl C0-10 alkyl,
C3-8 heterocyclyl C0-10 alkyl aminocarbonyl C0-10 alkyl,
aryl C0-10 alkyl aminocarbonyl C0-10 alkyl,
(C1-10 alkyl)2aminocarbonyl,
(aryl C1-10 alkyl)1-2aminocarbonyl,
C1-10 alkoxy (carbonyl)0-1C0-10 alkyl,
C0-10 alkyl carbonylamino(C0-10 alkyl),
C0-10 alkoxy carbonylamino(C0-10 alkyl),
carboxy C0-10 alkylamino,
carboxy C0-10 alkyl,
carboxy C3-8 cycloalkyl,
C1-10 alkoxy,
C1-10 alkyloxy C0-10 alkyl
C1-10 alkylcarbonyloxy,
C3-8 heterocyclyl C0-10 alkylcarbonyloxy,
C3-8 cycloalkyl C0-10 alkylcarbonyloxy,
aryl C0-10 alkylcarbonyloxy,
C1-10 alkylcarbonyloxy amino,
C3-8 heterocyclyl C0-10 alkylcarbonyloxy amino,
C3-8 cycloalkyl C0-10 alkylcarbonyloxy amino,
aryl C0-10 alkylcarbonyloxy amino,
(C1-10 alkyl)2aminocarbonyloxy,
(aryl C0-10 alkyl)1-2aminocarbonyloxy,
(C3-8 heterocyclyl C0-10 alkyl)1-2aminocarbonyloxy,
(C3-8 cycloalkyl C0-10 alkyl)1-2aminocarbonyloxy,
hydroxy C0-10alkyl,
hydroxycarbonylC0-10alkoxy,
hydroxycarbonylC0-10alkyloxy,
C1-10 alkylthio,
C1-10 alkylsulfinyl,
aryl C0-10 alkylsulfinyl,
C3-8 heterocyclyl C0-10 alkylsulfinyl,
C3-8 cycloalkyl C0-10 alkylsulfinyl,
C1-10 alkylsulfonyl,
aryl C0-10 alkylsulfonyl,
C3-8 heterocyclyl C0-10 alkylsulfonyl,
C3-8 cycloalkyl C0-10 alkylsulfonyl,
C1-10 alkylsulfonylamino,
aryl C1-10 alkylsulfonylamino,
C3-8 heterocyclyl C1-10 alkylsulfonylamino,
C3-8 cycloalkyl C1-10 alkylsulfonylamino,
cyano,
nitro,
perfluoroC1-6 alkyl, and
perfluoroC1-6 alkoxy, and
R8 is optionally substituted with one or more R9; and
wherein R9 is chosen from:
hydrogen,
halogen,
(carbonyl)0-1C1-10 alkyl,
(carbonyl)0-1C2-10 alkenyl,
(carbonyl)0-1C2-10 alkynyl,
(carbonyl)0-1aryl C1-10 alkyl,
C3-8 cycloalkyl C0-10 alkyl,
(C3-8)heterocyclyl C0-10 alkyl,
C1-4acylamino C0-10 alkyl,
C0-10 alkylamino C0-10 alkyl,
di-(C1-10 alkyl)amino C0-10 alkyl,
arylC0-10 alkylamino C1-10 alkyl,
(arylC0-10 alkyl)2amino C0-10 alkyl,
C3-8 cycloalkyl C0-10 alkylamino C0-10 alkyl,
C3-8 heterocyclyl C0-10 alkylamino C0-10 alkyl,
(C1-10 alkyl)2aminocarbonyl,
C1-10 alkoxy (carbonyl)0-1C0-10 alkyl,
C1-10alkyloxy C0-10alkyl,
(C1-10 alkyl)2aminocarbonyloxy,
hydroxycarbonylC0-10alkoxy,
(C1-10 alkyl)2aminocarbonyloxy,
(aryl C0-10 alkyl)1-2aminocarbonyloxy,
hydroxy C0-10alkyl,
C1-10 alkylsulfonyl,
C1-10 alkylsulfonylamino,
aryl C1-10 alkylsulfonylamino,
C3-8 heterocyclyl C1-10 alkylsulfonylamino,
C3-8 cycloalkyl C1-10 alkylsulfonylamino,
cyano,
nitro,
perfluoroC1-6 alkyl, and
perfluoroC1-6 alkoxy, and
wherein, R9 is optionally substituted with one or more groups selected from hydrogen, OH, (C1-6)alkoxy, halogen, CO2H, CN, O(C\u2550O)C1-C6 alkyl, NO2, trifluoromethoxy, trifluoroethoxy, \u2014Ob(C1-10)perfluoroalkyl, and NH2.
4. A compound according to claim 3, wherein
is pyridinyl.
5. A compound according to claim 1 having structural formula III:
a pharmaceutically acceptable salt or a stereoisomer thereof,
wherein:
represents a group chosen from: and pyridinyl;
R2, R3, and R4 are each independently chosen from:
hydrogen,
halogen,
C1-8 alkyl,
amino C0-6alkyl,
C1-6 alkylamino C0-6alkyl,
(C1-6 alkyl)2amino C0-6alkyl,
(C0-6alkyl)amino,
(C0-6alkyl)carbonylamino,
C1-6 alkoxy C0-6alkyl,
hydroxycarbonyl C0-6alkyl,
C1-6 alkoxycarbonyl C0-6alkyl,
hydroxycarbonyl C1-6 alkyloxy,
hydroxy C0-6alkyl,
cyano,
perfluoroC1-4 alkyl, and
perfluoroC1-4 alkoxy,
wherein
R3 and R4 together with the carbon atom to which they are attached can optionally form a spiro-C3-6 cycloalkyl group, or an oxo group and
R2, R3, and R4 are each independently optionally substituted with one or more R9; R5, R6, and R7 are each independently chosen from:
hydrogen,
halogen,
(carbonyl)0-1C1-10 alkyl,
(carbonyl)0-1C2-10 alkenyl,
(carbonyl)0-1C2-10 alkynyl,
(carbonyl)0-1aryl C1-10 alkyl,
C3-8 cycloalkyl C0-10 alkyl(carbonyl)0-1,
(C3-8)heterocyclyl C0-10 alkyl(carbonyl)0-1,
C1-4acylamino C0-10 alkyl,
C0-10 alkylamino C0-10 alkyl,
C0-10 alkylamino C0-10 alkylaminocarbonyl,
di-(C1-10 alkyl)amino C0-10 alkyl,
arylC0-10 alkylamino C0-10 alkyl,
(arylC0-10 alkyl)2amino C0-10 alkyl,
C3-8 cycloalkyl C0-10 alkylamino C0-10 alkyl,
C3-8 heterocyclyl C0-10 alkylamino C0-10 alkyl,
(C3-8 cycloalkyl C0-10 alkyl)2amino C0-10 alkyl,
(C3-8 heterocyclyl C0-10 alkyl)2amino C0-10 alkyl,
C3-8 cycloalkyl C0-10 alkyl aminocarbonylamino,
(C1-10 alkyl)2aminocarbonylamino,
(aryl C1-10 alkyl)1-2aminocarbonylamino,
C0-10 alkyl aminocarbonylamino,
C3-8 heterocyclyl C0-10 alkyl aminocarbonylamino,
(C1-10 alkyl)2aminocarbonyl C0-10 alkyl,
(aryl C1-10 alkyl)1-2aminocarbonyl C0-10 alkyl,
C0-10 alkyl aminocarbonyl C0-10 alkyl,
C3-8 cycloalkyl C0-10 alkyl aminocarbonyl C0-10 alkyl,
C3-8 heterocyclyl C0-10 alkyl aminocarbonyl C0-10 alkyl,
aryl C0-10 alkyl aminocarbonyl C0-10 alkyl,
(C1-10 alkyl)2aminocarbonyl,
(aryl C1-10 alkyl)1-2aminocarbonyl,
C1-10 alkoxy (carbonyl)0-1C0-10 alkyl,
C0-10 alkyl carbonylamino(C0-10 alkyl),
C0-10 alkoxy carbonylamino(C0-10 alkyl),
carboxy C0-10 alkylamino,
carboxy C0-10 alkyl,
carboxy aryl,
carboxy C3-8 cycloalkyl,
carboxy C3-8 heterocyclyl,
C1-10 alkoxy,
C1-10alkyloxy C0-10alkyl
C1-10 alkylcarbonyloxy,
C3-8 heterocyclyl C0-10 alkylcarbonyloxy,
C3-8 cycloalkyl C0-10 alkylcarbonyloxy,
aryl C0-10 alkylcarbonyloxy,
C1-10 alkylcarbonyloxy amino,
C3-8 heterocyclyl C0-10 alkylcarbonyloxy amino,
C3-8 cycloalkyl C1-10 alkylcarbonyloxy amino,
aryl C0-10 alkylcarbonyloxy amino,
(C1-10 alkyl)2aminocarbonyloxy,
(aryl C0-10 alkyl)1-2aminocarbonyloxy,
(C3-8 heterocyclyl C0-10 alkyl)1-2aminocarbonyloxy,
(C3-8 cycloalkyl C0-10 alkyl)1-2aminocarbonyloxy,
hydroxy C0-10alkyl,
hydroxycarbonylC0-10alkoxy,
hydroxycarbonylC0-10alkyloxy,
C1-10 alkylthio,
C1-10 alkylsulfinyl,
aryl C0-10 alkylsulfinyl,
C3-8 heterocyclyl C0-10 alkylsulfinyl,
C3-8 cycloalkyl C0-10 alkylsulfinyl,
C1-10 alkylsulfonyl,
aryl C0-10 alkylsulfonyl,
C3-8 heterocyclyl C0-10 alkylsulfonyl,
C3-8 cycloalkyl C0-10 alkylsulfonyl,
C1-10 alkylsulfonylamino,
aryl C1-10 alkylsulfonylamino,
C3-8 heterocyclyl C1-10 alkylsulfonylamino,
C3-8 cycloalkyl C1-10 alkylsulfonylamino,
cyano,
nitro,
perfluoroC1-6alkyl, and
perfluoroC1-6alkoxy; and
R5, R6, and R7 are each independently optionally substituted with one or more R9;
R8 is chosen from:
hydrogen,
halogen,
(carbonyl)0-1C1-10 alkyl,
(carbonyl)0-1C2-10 alkenyl,
(carbonyl)0-1C2-10 alkynyl,
(carbonyl)0-1aryl C1-10 alkyl,
C3-8 cycloalkyl C0-10 alkyl(carbonyl)0-1,
C1-4acylamino C0-10 alkyl,
C0-10 alkylamino C0-10 alkyl,
C0-10 alkylamino C0-10 alkylaminocarbonyl,
di-C1-10 alkyl)amino C0-10 alkyl,
arylC0-10 alkylamino C0-10 alkyl,
(arylC0-10 alkyl)2amino C0-10 alkyl,
C3-8 cycloalkyl C0-10 alkylamino C0-10 alkyl,
C3-8 heterocyclyl C0-10 alkylamino C0-10 alkyl,
(C3-8 cycloalkyl C0-10 alkyl)2amino C0-10 alkyl,
(C3-8 heterocyclyl C0-10 alkyl)2amino C0-10 alkyl,
C3-8 cycloalkyl C0-10 alkyl aminocarbonylamino,
(C1-10 alkyl)2aminocarbonylamino,
(aryl C1-10 alkyl)1-2aminocarbonylamino,
C0-10 alkyl aminocarbonylamino,
C3-8 heterocyclyl C0-10 alkyl aminocarbonylamino,
(C1-10 alkyl)2aminocarbonyl C0-10 alkyl,
(aryl C1-10 alkyl)1-2aminocarbonyl C0-10 alkyl,
C0-10 alkyl aminocarbonyl C0-10 alkyl,
C3-8 cycloalkyl C0-10 alkyl aminocarbonyl C0-10 alkyl,
C3-8 heterocyclyl C0-10 alkyl aminocarbonyl C0-10 alkyl,
aryl C0-10 alkyl aminocarbonyl C0-10 alkyl,
(C1-10 alkyl)2aminocarbonyl,
(aryl C1-10 alkyl)1-2aminocarbonyl,
C1-10 alkoxy (carbonyl)0-1C0-10 alkyl,
C0-10 alkyl carbonylamino(C0-10 alkyl),
C0-10 alkoxy carbonylamino(C0-10 alkyl),
carboxy C0-10 alkylamino,
carboxy C0-10 alkyl,
carboxy C3-8 cycloalkyl,
C1-10 alkoxy,
C1-10alkyloxy C0-10alkyl
C1-10 alkylcarbonyloxy,
C3-8 heterocyclyl C0-10 alkylcarbonyloxy,
C3-8 cycloalkyl C0-10 alkylcarbonyloxy,
aryl C0-10 alkylcarbonyloxy,
C1-10 alkylcarbonyloxy amino,
C3-8 heterocyclyl C0-10 alkylcarbonyloxy amino,
C3-8 cycloalkyl C0-10 alkylcarbonyloxy amino,
aryl C0-10 alkylcarbonyloxy amino,
(C1-10 alkyl)2aminocarbonyloxy,
(aryl C0-10 alkyl)1-2aminocarbonyloxy,
(C3-8 heterocyclyl C0-10 alkyl)1-2aminocarbonyloxy,
(C3-8 cycloalkyl C0-10 alkyl)1-2aminocarbonyloxy,
hydroxy C0-10alkyl,
hydroxycarbonylC0-10alkoxy,
hydroxycarbonylC0-10alkyloxy,
C1-10 alkylthio,
C1-10 alkylsulfinyl,
aryl C0-10 alkylsulfinyl,
C3-8 heterocyclyl C0-10 alkylsulfinyl,
C3-8 cycloalkyl C0-10 alkylsulfinyl,
C1-10 alkylsulfonyl,
aryl C0-10 alkylsulfonyl,
C3-8 heterocyclyl C0-10 alkylsulfonyl,
C3-8 cycloalkyl C0-10 alkylsulfonyl,
C1-10 alkylsulfonylamino,
aryl C1-10 alkylsulfonylamino,
C3-8 heterocyclyl C1-10 alkylsulfonylamino,
C3-8 cycloalkyl C1-10 alkylsulfonylamino,
cyano,
nitro,
perfluoroC1-6alkyl, and
perfluoroC1-6alkoxy; and
wherein R8 is optionally substituted with one or more R9; and
R9 is chosen from:
hydrogen,
halogen,
(carbonyl)0-1C1-10 alkyl,
(carbonyl)0-1C2-10 alkenyl,
(carbonyl)0-1C2-10 alkynyl,
(carbonyl)0-1aryl C1-10 alkyl,
C3-8 cycloalkyl C0-10 alkyl,
(C3-8)heterocyclyl C0-10 alkyl,
C1-4acylamino C0-10 alkyl,
C0-10 alkylamino C0-10 alkyl,
di-(C1-10 alkyl)amino C0-10 alkyl,
arylC0-10 alkylamino C0-10 alkyl,
(arylC0-10 alkyl)2amino C0-10 alkyl,
C3-8 cycloalkyl C0-10 alkylamino C0-10 alkyl,
C3-8 heterocyclyl C0-10 alkylamino C0-10 alkyl,
(C1-10 alkyl)2aminocarbonyl,
C1-10 alkoxy (carbonyl)0-1C0-10 alkyl,
C1-10 alkyloxy C0-10 alkyl,
(C1-10 alkyl)2aminocarbonyloxy,
hydroxycarbonylC0-10alkoxy,
(C1-10 alkyl)2aminocarbonyloxy,
(aryl C0-10 alkyl)1-2aminocarbonyloxy,
hydroxy C0-10alkyl,
C1-10 alkylsulfonyl,
C1-10 alkylsulfonylamino,
aryl C1-10 alkylsulfonylamino,
C3-8 heterocyclyl C1-10 alkylsulfonylamino,
C3-8 cycloalkyl C1-10 alkylsulfonylamino,
cyano,
nitro,
perfluoroC1-6 alkyl, and
perfluoroC1-6 alkoxy; and
wherein, R9 is optionally substituted with one or more groups selected from hydrogen, OH, (C1-6)alkoxy, halogen, CO2H CN, O(C\u2014O)C1-C6 alkyl, NO2, trifluoromethoxy, trifluoroethoxy, \u2014Ob(C1-10)perfluoroalkyl, and NH2.
6. A compound of claim 5 and formula III, or a pharmaceutically acceptable salt or a stereoisomer thereof, wherein:
represents a group chosen from: pyridinyl;
R2, R3, and R4 are each independently chosen from:
hydrogen,
halogen,
C1-8 alkyl,
(C0-6alkyl)amino,
(C0-6alkyl)carbonylamino,
amino C0-6alkyl,
C1-6 alkylamino C0-6alkyl,
(C1-6 alkyl)2amino C0-6alkyl,
C1-6 alkoxy C0-6alkyl,
C1-6 alkoxycarbonyl C0-6alkyl,
hydroxy C0-6alkyl,
cyano,
perfluoroC1-4alkyl, and
perfluoroC1-4alkoxy,
wherein
R3 and R4 together with the carbon atom to which they are attached can optionally form a spiro-C3-6 cycloalkyl group, or an oxo group, and
R2, R3, and R4 are each independently optionally substituted with one or more R9;
R5, R6, and R7 are each independently chosen from:
hydrogen,
halogen,
(carbonyl)0-1C1-10 alkyl,
(carbonyl)0-1C2-10 alkenyl,
(carbonyl)0-1aryl C1-10 alkyl,
C3-8 cycloalkyl C0-10 alkyl(carbonyl)0-1,
(C3-8)heterocyclyl C0-10 alkyl(carbonyl)0-1,
C1-4acylamino C0-10 alkyl,
C0-10alkylamino C0-10 alkyl,
C0-10 alkylamino C0-10 alkylaminocarbonyl,
di-C1-10 alkyl)amino C0-10 alkyl,
arylC0-10 alkylamino C0-10 alkyl,
C3-8 cycloalkyl C0-10 alkylamino C0-10 alkyl,
C3-8 heterocyclyl C0-10 alkylamino C0-10 alkyl,
(C3-8 cycloalkyl C0-10 alkyl)2amino C0-10 alkyl,
(C3-8 heterocyclyl C0-10 alkyl)2amino C0-10 alkyl,
C3-8 cycloalkyl C0-10 alkyl aminocarbonylamino,
(C1-10 alkyl)2aminocarbonylamino,
(aryl C1-10 alkyl)1-2aminocarbonylamino,
C0-10 alkyl aminocarbonylamino,
C3-8 heterocyclyl C0-10 alkyl aminocarbonylamino,
(C1-10 alkyl)2aminocarbonyl C0-10 alkyl,
(aryl C1-10 alkyl)1-2aminocarbonyl C0-10 alkyl,
C0-10 alkyl aminocarbonyl C0-10 alkyl,
C3-8 cycloalkyl C0-10 alkyl aminocarbonyl C0-10 alkyl,
C3-8 heterocyclyl C0-10 alkyl aminocarbonyl C0-10 alkyl,
aryl C0-10 alkyl aminocarbonyl C0-10 alkyl,
(C1-10 alkyl)2aminocarbonyl,
(aryl C1-10 alkyl)1-2aminocarbonyl,
C1-10 alkoxy (carbonyl)0-1C0-10 alkyl,
C0-10 alkyl carbonylamino(C0-10 alkyl),
C0-10 alkoxy carbonylamino(C0-10 alkyl),
carboxy C0-10 alkylamino,
carboxy C0-10 alkyl,
carboxy aryl,
carboxy C3-8 cycloalkyl,
carboxy C3-8 heterocyclyl,
C1-10 alkoxy,
C1-10alkyloxy C0-10alkyl
C1-10 alkylcarbonyloxy,
C3-8 heterocyclyl C0-10 alkylcarbonyloxy,
C3-8 cycloalkyl C0-10 alkylcarbonyloxy,
aryl C0-10 alkylcarbonyloxy,
C1-10 alkylcarbonyloxy amino,
C3-8 heterocyclyl C0-10 alkylcarbonyloxy amino,
C3-8 cycloalkyl C0-10 alkylcarbonyloxy amino,
aryl C0-10 alkylcarbonyloxy amino,
(C1-10 alkyl)2aminocarbonyloxy,
(aryl C0-10 alkyl)1-2aminocarbonyloxy,
(C3-8 heterocyclyl C0-10 alkyl)1-2aminocarbonyloxy,
(C3-8 cycloalkyl C0-10 alkyl)1-2aminocarbonyloxy,
hydroxy C0-10alkyl,
hydroxycarbonylC0-10alkoxy,
hydroxycarbonylC0-10alkoxy,
C1-10 alkylthio,
C1-10 alkylsulfonyl,
aryl C0-10 alkylsulfonyl,
C3-8 heterocyclyl C0-10 alkylsulfonyl,
C3-8 cycloalkyl C0-10 alkylsulfonyl,
C1-10 alkylsulfonylamino,
aryl C1-10 alkylsulfonylamino,
C3-8 heterocyclyl C1-10 alkylsulfonylamino,
C3-8 cycloalkyl C1-10 alkylsulfonylamino,
cyano,
nitro,
perfluoroC1-6 alkyl, and
perfluoroC1-6 alkoxy, and
R5, R6, and R7 are each independently optionally substituted with one or more R9;
R8 is chosen from:
hydrogen,
(carbonyl)0-1C1-10 alkyl,
(carbonyl)0-1aryl C1-10 alkyl,
C3-8 cycloalkyl C0-10 alkyl(carbonyl)0-1,
C0-10 alkylamino C0-10 alkyl,
carboxy C0-10 alkyl,
carboxy C3-8 heterocyclyl,
C1-10alkyloxy C0-10alkyl,
hydroxy C0-10alkyl, and
perfluoroC1-6 alkyl,
wherein R8 is optionally substituted with one or more R9;
R9 is chosen from:
hydrogen,
halogen,
(carbonyl)0-1C1-10 alkyl,
(carbonyl)0-1C2-10 alkenyl,
(carbonyl)0-1aryl C1-10 alkyl,
C3-8 cycloalkyl C0-10 alkyl,
(C3-8)heterocyclyl C0-10 alkyl,
C1-4acylamino C0-10 alkyl,
C0-10 alkylamino C0-10 alkyl,
di-C1-10 alkyl)amino C0-10 alkyl,
arylC0-10 alkylamino C0-10 alkyl,
(arylC0-10 alkyl)2amino C0-10 alkyl,
C3-8 cycloalkyl C0-10 alkylamino C0-10 alkyl,
C3-8 heterocyclyl C0-10 alkylamino C0-10 alkyl,
(C1-10 alkyl)2aminocarbonyl,
C1-10 alkoxy (carbonyl)0-1C0-10 alkyl,
C1-10alkyloxy C0-10alkyl,
(C1-10 alkyl)2aminocarbonyloxy,
hydroxycarbonylC0-10alkoxy,
(C1-10 alkyl)2aminocarbonyloxy,
hydroxy C0-10alkyl,
C1-10 alkylsulfonyl,
C1-10 alkylsulfonylamino,
aryl C1-10 alkylsulfonylamino,
C3-8 heterocyclyl C1-10 alkylsulfonylamino,
C3-8 cycloalkyl C1-10 alkylsulfonylamino,
cyano,
nitro,
perfluoroC1-6alkyl, and
perfluoroC1-6alkoxy; and
wherein, R9 is optionally substituted with one or more groups selected from hydrogen, OH, (C1-6)alkoxy, halogen, CO2H, CN, O(C\u2550O)C1-C6 alkyl, NO2, trifluoromethoxy, trifluoroethoxy, \u2014Ob(C1-10)perfluoroalkyl, and NH2.
7. A compound according to claim 6, wherein R2 is chosen from hydrogen, halogen, C1-8alkyl, and perfluoroC1-6alkyl.
8. A compound according to claim 6, wherein R3 and R4 are each independently chosen from hydrogen, halogen, C1-8alkyl, C1-10alkoxyl, and perfluoroC1-6alkyl.
9. A compound according to claim 6, wherein R8 is chosen from:
hydrogen,
(carbonyl)0-1C1-10 alkyl,
(carbonyl)0-1aryl C1-10 alkyl,
C3-8 cycloalkyl C0-10 alkyl(carbonyl)0-1,
C0-10 alkylamino C0-10 alkyl,
hydroxy C0-10alkyl, and
perfluoroC1-6alkyl,
wherein R8 is optionally substituted with at least one substituent, R9, chosen from:
hydrogen,
halogen,
(carbonyl)0-1C1-10 alkyl,
(carbonyl)0-1C2-10 alkenyl,
(carbonyl)0-1aryl C1-10 alkyl,
C3-8 cycloalkyl C0-10 alkyl,
(C3-8)heterocyclyl C0-10 alkyl,
C1-4acylamino C0-10 alkyl,
C0-10 alkylamino C0-10 alkyl,
di-(C1-10 alkyl)amino C0-10 alkyl,
arylC0-10 alkylamino C0-10 alkyl,
(arylC1-10 alkyl)2amino C0-10 alkyl,
C3-8 cycloalkyl C0-10 alkylamino C0-10 alkyl,
C3-8 heterocyclyl C0-10 alkylamino C0-10 alkyl,
(C1-10 alkyl)2aminocarbonyl,
C1-10 alkoxy (carbonyl)0-1C0-10alkyl,
C1-10 alkyloxy C0-10alkyl,
(C1-10 alkyl)2aminocarbonyloxy,
hydroxycarbonylC0-10alkoxy,
(C1-1 alkyl)2aminocarbonyloxy,
hydroxy C0-10alkyl,
C1-10 alkylsulfonyl,
C1-10 alkylsulfonylamino,
aryl C1-10 alkylsulfonylamino,
C3-8 heterocyclyl C1-10 alkylsulfonylamino,
C3-8 cycloalkyl C1-10 alkylsulfonylamino,
cyano,
nitro,
perfluoroC1-6alkyl, and
perfluoroC1-6alkoxy, and
wherein, R9 is optionally substituted with one or more groups selected from hydrogen, OH, (C1-6)alkoxy, halogen, CO2H, CN, O(C\u2550O)C1-C6 alkyl, NO2, trifluoromethoxy, trifluoroethoxy, \u2014Ob(C1-10)perfluoroalkyl, and NH2.
10. A compound selected from:
N-(pyridin-2-ylmethyl)-4-methyl-3-oxo-4-aza-5\u03b1-androst-1-en-17\u03b2-acetamide;
N-(pyridin-3-ylmethyl)-4-methyl-3-oxo-4-aza-5\u03b1-androst-1-en-17\u03b2-acetamide;
N-(pyridin-4-ylmethyl)-4-methyl-3-oxo-4-aza-5\u03b1-androst-1-en-17\u03b2-acetamide;
N-(6-methylpyridin-2-yl)methyl-4-methyl-3-oxo-4-aza-5\u03b1-androst-1-en-17\u03b2-acetamide;
N-(1-oxidopyridin-2-yl)methyl-4-methyl-3-oxo-4-aza-5\u03b1-androst-1-en-17\u03b2-acetamide;
N-3-(methylthio)pyridin-2-ylmethyl-4-methyl-3-oxo-4-aza-5\u03b1-androst-1-en-17\u03b2-acetamide;
N-{1H-trifluoromethyl)pyridin-3-ylmethyl}-4-methyl-3-oxo-4-aza-5\u03b1-androst-1-en-17\u03b2-acetamide;
N-N-methyl(pyridin-2-ylmethyl-4-methyl-3-oxo-4-aza-5\u03b1-androst-1-en-17\u03b2-acetamide;
N-(1-pyridin-2-ylethyl)-4-methyl-3-oxo-4-aza-5\u03b1-androst-1-en-17\u03b2-acetamide;
N-(2,2,2-trifluoro-1-pyridin-2-ylethyl)-4-methyl-3-oxo-4-aza-5\u03b1-androst-1-en-17\u03b2-acetamide;
N-(3-hydroxy-methylpyridin-2-yl)methyl-4-methyl-3-oxo-4-aza-5\u03b1-androst-1-en-17\u03b2-acetamide;
N-{tert-butyl6-aminomethyl)pyridin-2-ylmethylcarbamate}-4-methyl-3-oxo-4-aza-5\u03b1-androst-1-en-17\u03b2-acetamide;
N-(3-fluoropyridin-2-yl)methyl-4-methyl-3-oxo-4-aza-5\u03b1-androst-1-en-17\u03b2-acetamide;
N-(4-tert-butylpyridin-2-yl)methyl-4-methyl-3-oxo-4-aza-5\u03b1-androst-1-en-17\u03b2-acetamide;
N-(3-chloropyridin-2-yl)methyl-4-methyl-3-oxo-4-aza-5\u03b1-androst-1-en-17\u03b2-acetamide;
N-(3-methylpyridin-2-yl)methyl-4-methyl-3-oxo-4-aza-5\u03b1-androst-1-en-17\u03b2-acetamide;
and pharmaceutically acceptable salts and stereoisomers thereof.
11. A compound according to claim 10, selected from:
N-(3-fluoropyridin-2-yl)methyl-20-fluoro-4-methyl-3-oxo-4-aza-5\u03b1-androst-1-en-17\u03b2-acetamide;
and pharmaceutically acceptable salts and stereoisomers thereof.
12. A compound according to claim 10, selected from:
N-(pyridin-2-ylmethyl)-4-methyl-3-oxo-aza-5\u03b1-androst-1-en-17\u03b2-acetamide;
N-(pyridin-3-ylmethyl)-4-methyl-3-oxo-4-aza-5\u03b1-androst-1-en-17\u03b2-acetamide;
N-(pyridin-4-ylmethyl)-4-methyl-3-oxo-4-aza-5\u03b1-androst-1-en-17\u03b2-acetamide;
N-(6-methylpyridin-2-yl)methyl-4-methyl-3-oxo-4-aza-5\u03b1-androst-1-en-17\u03b2-acetamide;
N-(1-oxidopyridin-2-yl)methyl-4-methyl-3-oxo-4-aza-5\u03b1-androst-1-en-17\u03b2-acetamide;
N-3-methylthio)pyridin-2-ylmethyl-4-methyl-3-oxo-4-aza-5\u03b1-androst-1-en-17\u03b2-acetamide;
N-{6-(trifluoromethyl)pyridin-3-ylmethyl}methyl-3-oxo-4-aza-5\u03b1-androst-1-en-17\u03b2-acetamide;
N-N-methyl(pyridin-2-ylmethyl)-4-methyl-3-oxo-4-aza-5\u03b1-androst-1-en-17\u03b2-acetamide;
N-(1-pyridin-2-ylethyl)-4-methyl-3-oxo-4-aza-5\u03b1-androst-1-en-17\u03b2-acetamide;
N-(2,2,2-trifluoro-1-pyridin-2-ylethyl)-4-methyl-3-oxo-4-aza-5\u03b1-androst-1-en-17\u03b2-acetamide;
N-(3-hydroxy-6-methylpyridin-2-yl)methyl)-4-methyl-3-oxo-4-aza-5\u03b1-androst-1-en-17\u03b2-acetamide;
N-{tert-butyl6-aminomethyl)pyridin-2-ylmethylcarbamate}-4-methyl-3-oxo-4-aza-5\u03b1-androst-1-en-17\u03b2-acetamide;
N-(3-fluoropyridin-2-yl)methyl-4-methyl-3-oxo-4-aza-5\u03b1-androst-1-en-17\u03b2-acetamide;
N-(4-tert-butylpyridin-2-yl)methyl-4-methyl-3-oxo-4-aza-5\u03b1-androst-1-en-17\u03b2-acetamide;
N-(3-chloropyridin-2-yl)methyl-4-methyl-3-oxo-4-aza-5\u03b1-androst-1-en-17\u03b2-acetamide;
N-(3-methylpyridin-2-yl)methylmethyl-3-oxo-4-aza-5\u03b1-androst-1-en-17\u03b2-acetamide;
N-(3-fluoropyridin-2-yl)methyl-20-fluoro-4-methyl-3-oxo-4-aza-5\u03b1-androst-1-en-17\u03b2-acetamide;
and pharmaceutically acceptable salts and stereoisomers thereof.
13. A compound according to claim 12 selected from:
N-(pyridin-2-ylmethyl)-4-methyl-3-oxo-4-aza-5\u03b1-androst-1-en-17\u03b2-acetamide;
N-(pyridin-3-ylmethyl)-4-methyl-3-oxo-4-aza-5\u03b1-androst-1-en-17\u03b2-acetamide;
N-(pyridin-4-ylmethyl)-4-methyl-3-oxo-4-aza-5\u03b1-androst-1-en-17\u03b2-acetamide;
N-(6-methylpyridin-2-yl)methyl-4-methyl-3-oxo-4-aza-5\u03b1-androst-1-en-17\u03b2-acetamide;
N-(1-oxidopyridin-2-yl)methyl-4-methyl-3-oxo-4-aza-5\u03b1-androst-1-en-17\u03b2-acetamide;
N-3-methylthio)pyridin-2-ylmethyl-4-methyl-3-oxo-4-aza-5\u03b1-androst-1-en-17\u03b2-acetamide;
N-{6-trifluoromethyl)pyridin-3-ylmethyl)}-4-methyl-3-oxo-4-aza-5\u03b1-androst-1-en-17\u03b2-acetamide;
N-N-methyl(pyridin-2-ylmethyl)-4-methyl-3-oxo-4-aza-5\u03b1-androst-1-en-17\u03b2-acetamide;
N-(1-pyridin-2-ylethyl)-4-methyl-3-oxo-4-aza-5\u03b1-androst-1-en-17\u03b2-acetamide;
N-(2,2,2-trifluoro-1-pyridin-2-ylethyl)-4-methyl-3-oxo-4-aza-5\u03b1-androst-1-en-17\u03b2-acetamide;
N-(3-hydroxy-6-methylpyridin-2-yl)methyl-4-methyl-3-oxo-4-aza-5\u03b1-androst-1-en-17\u03b2-acetamide;
N-{tert-butyl6-aminomethyl)pyridin-2-ylmethylcarbamate}methyl-3-oxo-4-aza-5\u03b1-androst-1-en-17\u03b2-acetamide;
N-(3-fluoropyridin-2-yl)methyl-4-methyl-3-oxo-4-aza-5\u03b1-androst-1-en-17\u03b2-acetamide;
N-(4-tert-butylpyridin-2-yl)methyl-4-methyl-3-oxo-4-aza-5\u03b1-androst-1-en-17\u03b2-acetamide;
N-(3-chloropyridin-2-yl)methyl-4-methyl-3-oxo-4-aza-5\u03b1-androst-1-en-17\u03b2-acetamide;
N-(3-methylpyridin-2-yl)methylmethyl-3-oxo-4-aza-5\u03b1-androst-1-en-17\u03b2-acetamide;
N-(3-fluoropyridin-2-yl)methyl-20-fluoro-4-methyl-3-oxo-4-aza-5\u03b1-androst-1-en-17\u03b2-acetamide;
and pharmaceutically acceptable salts and stereoisomers thereof.
14. A pharmaceutical composition comprising a therapeutically effective amount of a compound of claim 1 and a pharmaceutically acceptable carrier.
15. A process for making a pharmaceutical composition comprising combining a compound according to claim 1 and a pharmaceutically acceptable carrier.
16. A compound which is N-(pyridin-2-ylmethyl)-4-methyl-3-oxo-4-aza-5\u03b1-androst-1-en-17\u03b2-acetamide or a pharmaceutically acceptable salt or stereoisomer thereof.
17. A pharmaceutical composition according to claim 16 comprising a compound which is N-(pyridin-2-ylmethyl)-4-methyl-3 -oxo-4-aza-5\u03b1-androst-1-en-17\u03b2-acetamide or a pharmaceutically acceptable salt or stereoisomer thereof and a pharmaceutically acceptable carrier.