1. A compound having formula:
wherein:
ring A is an optionally substituted 5 membered heterocyclic ring;
Rx is H, aliphatic, OH, \u2014C(O)\u2014O-(cycloaliphatic or aliphatic or \u2014C(O)-(cycloaliphatic or aliphatic);
Ar is an optionally substituted aryl or heteroaryl;
X is O, S, NRx, \u2014CH\u2550, \u2014C\u2261 or CH2;
R1 is C2-C8 alkynyl, optionally substituted with up to 4 substituents selected from halo, Ar, cycloaliphatic, heterocyclyl, NH2, NH(cycloaliphatic or aliphatic), N(cycloaliphatic or aliphatic)2, halogen, \u2014OH, \u2014O(cycloaliphatic or aliphatic), NO2, \u2014CN, \u2014CO2H, \u2014CO2(cycloaliphatic or aliphatic), \u2014O(halo-cycloaliphatic or aliphatic), or halo-(cycloaliphatic or aliphatic); and
wherein up to 2 \u2014CH2\u2014 in said alkynyl, cycloaliphatic or aliphatic may be replaced with O, S, or \u2014NRx\u2014.
2. The compound according to claim 1, wherein ring A, including the nitrogen atom attached to \u2014S(O)2\u2014 is pyrrolidinyl ring.
3. The compound according to claim 1, wherein ring A, including the nitrogen atom is:
4. The compound according to claim 1, wherein ring A optionally comprises up to 3 substituents, wherein:
the first of said substituents, if present, is selected from Rx, R2, R4 or R5,
the second of said substituents, if present, is selected from Rx or R4, and
the third of said substituents, if present, is Rx; wherein:
each RX is independently selected from 1,2-methylenedioxy, 1,2-ethylenedioxy, R6 or (CH2)n\u2014Y;
wherein n is 0, 1 or 2; and
Y is selected from halogen, CN, NO2, CF3, OCF3, OH, SR6, S(O)R6, SO2R6, NH2, NHR6, N(R6)2, NR6R8, COOH, COOR6 or OR6;
each R2 is independently selected from (C1-C6)-straight or branched alkyl, or (C2-C6)-straight or branched alkenyl or alkynyl; and each R2 optionally comprises up to 2 substituents, wherein:
the first of said substituents, if present, is selected from Rx, R4 and R5, and
the second of said substituents, if present, is Rx;
each R4 is independently selected from OR5, OC(O)R6, OC(O)R5, OC(O)OR6, OC(O)OR5, OC(O)N(R6)2, OP(O)(OR6)2, SR6, SR5, S(O)R6, S(O)R5, SO2R6, SO2R5 , SO2N(R6)2, SO2NR5R6, SO3R6, C(O)R5, C(O)OR5, C(O)R6, C(O)OR6, NC(O)C(O)R6, NC(O)C(O)R5, NC(O)C(O)OR6, NC(O)C(O)N(R6)2, C(O)N(R6)2, C(O)N(OR6)R6, C(O)N(OR6)R5, C(NOR6)R6, C(NOR6)R5, N(R6)2, NR6C(O)R1, NR6C(O)R6, NR6C(O)R5, NR6C(O)OR6, NR6C(O)OR5, NR6C(O)N(R6)2, NR6C(O)NR5R6, NR6SO2R6, NR6SO2R5, NR6SO2N(R6)2, NR6SO2NR5R6, N(OR6)R6, N(OR6)R5, P(O)(OR6)N(R6)2, and P(O)(OR6)2;
each R5 is a cycloaliphatic, aryl, heterocyclyl, or heteroaromatic; and each R5 optionally comprises up to 3 substituents, each of which, if present, is R1;
each R6 is independently selected from H, (C1-C6)-straight or branched alkyl, or (C2-C6) straight or branched alkenyl; and each R6 optionally comprises a substituent that is R7;
R7 is a cycloaliphatic, aryl, heterocyclyl, or heteroaromatic; and each R7 optionally comprises up to 2 substituents independently chosen from H, (C1-C6)-straight or branched alkyl, (C2-C6) straight or branched alkenyl, 1,2-methylenedioxy, 1,2-ethylenedioxy, or (CH2)n-Z;
wherein n is 0, 1 or 2; and
Z is selected from halogen, CN, NO2, CF3, OCF3, OH, S(C1-C6)-alkyl, SO(C1-C6)-alkyl, SO2(C1-C6)-alkyl, NH2, NH(C1-C6)-alkyl, N((C1-C6)-alkyl)2, N((C1-C6)-alkyl)R8, COOH, C(O)O(C1-C6)-alkyl or O(C1-C6)-alkyl; and
R8 is an amino protecting group.
5. The compound according to claim 4, wherein ring A has up to three substituents selected from aliphatic, cyano, halo, hydroxy, \u2014NOH, carboxy, oxo, amido, cyanoaliphatic, hydroxyaliphatic, thioaliphatic, carboxyaliphatic, aliphatic-oxycarbonyl, aliphatic-carbonylaliphatic, aliphatic-cycloaliphatic, aliphatic-cycloaliphatic-aliphatic, aliphatiesulfonyl, aryl, aryl-aliphatic, aryl-aliphatic-oxyaliphatic, aryl(aliphatic-carbonyl)aliphatic, arylcarbamoylaliphatic, heterocyclylcarbamoylaliphatic, aliphatic-carbamoylaliphatic, cycloaliphatic-carbamoylaliphatic, diaryl-aliphatic, aryl(carboxyaliphatic)amide, arylamino, arylcarbonyl, arylsulfonyl, cycloaliphatic, cycloaliphatic-carbonyl, cycloaliphatic-alkyl, heteroaryl, heteroaryl-aliphatic, heterocyclyl, or heterocyclyl-aliphatic.
6. The compound according to claim 1, wherein R1 is C2-C8 alkynyl, optionally substituted with up to 3 substituents selected from halo, Ar, cycloalkyl, heterocyclyl, heteroaromatic, NH2, NH(C1-C4 aliphatic), N(C1-C4 aliphatic)2, halogen, OH, O(C1-C4 aliphatic), NO2, CN, CO2H, CO2(C1-C4 aliphatic), O(halo-C1-C4 aliphatic), or halo-C1-C4 aliphatic.
7. The compound according to claim 6, wherein R1 is C2-C8 alkynyl.
8. The compound according to claim 7, wherein R1 is 2-butynyl.
9. The compound according to claim 1, wherein Ar is an optionally substituted monocyclic aryl ring or a monocyclic heteroaryl ring.
10. The compound according to claim 9, wherein Ar is an aromatic ring system with substituents that enhance the ability of said ring system to engage in a \u03c0-stacking interaction.
11. The compound according to claim 10, wherein Ar is an optionally substituted phenyl or a 5-6 membered heteroaromatic ring.
12. The compound according to claim 11, wherein Ar is phenyl.
13. The compound according to claim 11, wherein Ar is triazinyl, pyrazinyl, pyrimidinyl, pyridazinyl, pyridinyl, thiadiazolyl, triazolyl, oxadiazolyl, isothiazolyl, pyrazolyl, imidazolyl, thiazolyl, oxazolyl, pyrrolyl, thiophenyl, furanyl, indolizinyl, indolyl, isoindolyl, benzofuranyl, benzo bthiophenyl, 1H-indazolyl, benzimidazolyl, benzthiazolyl, purinyl, quinolinyl, isoquinolinyl, cinnolinyl, phthazinyl, quinazolinyl, quinoxalinyl, 1,8-naphthyridinyl, pteridinyl, carbazolyl, acridinyl, phenazinyl, phenothiazinyl, phenoxazinyl, indenyl, naphthyl, azulinyl, or anthracenyl.
14. The compound according to claim 13, wherein Ar is triazinyl, pyrazinyl, pyrimidinyl, pyridazinyl, pyridinyl, thiadiazolyl, triazolyl, oxadiazolyl, isothiazolyl, pyrazolyl, imidazolyl, thiazolyl, oxazolyl, pyrrolyl, thiophenyl or furanyl.
15. The compound according to claim 14, wherein Ar is pyridinyl.
16. The compound according to claim 1, wherein X is \u2014CH2\u2014, O, S, or NRx.
17. A compound having formula (I\u2032):
wherein:
Y is CH2;
one of X1, X2, X3, and X4 is \u2550CH\u2014, and each of the other three of X1, X2, X3, and X4 is independently selected from \u2550N\u2014 or \u2550CH\u2014;
X\u2032 is selected from O or NRx;
Rx is H, aliphatic, OH, \u2014C(O)\u2014O-(cycloaliphatic or aliphatic or \u2014C(O)-(cycloaliphatic or aliphatic);
R1 is C2-C8 alkynyl, optionally substituted with up to 4 substituents selected from halo, aryl, heteroaryl, cycloaliphatic, heterocyclyl, NH2, NH(cycloaliphatic or aliphatic), N(cycloaliphatic or aliphatic)2, halogen, \u2014OH, \u2014O(cycloaliphatic or aliphatic), NO2, \u2014CN, \u2014CO2H, \u2014CO2(cycloaliphatic or aliphatic), \u2014O(halo-cycloaliphatic or aliphatic), or halo-(cycloaliphatic or aliphatic); and
wherein up to 2 \u2014CH2\u2014 in said alkynyl, cycloaliphatic or aliphatic may be replaced with O, S, or \u2014NRx\u2014.
18. The compound according to claim 17, wherein said compound has formula:
19. The compound according to claim 17, wherein said compound has formula:
20. The compound according to claim 17, wherein said compound is selected from:
Compd
No.
Structure
2
3
4
5
6
7
21. The compound according to claim 1, wherein ring A in formula (I) together with the sulfonyl group attached thereto is selected from:
wherein R is hydrogen.
22. A pharmaceutical composition comprising a compound according to claim 1 or claim 17, and a pharmaceutical carrier.
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 hot water heating system with a burner and operating components associated with said burner, said burner and said operating components being located within a housing, said operating components being located at and accessible form one end of said heating system upon removal of a portion of said housing.
2. A hot water heating system as in claim 1 wherein said operating components include a burner assembly, a compressor, a combustion fan and a fuel pump.
3. A hot water heating system as in claim 2 and further comprising a hot water outlet and a cold water inlet located at said one end of said heating system.
4. A hot water heating system as in claim 3 which utilises a coolant and further comprising a coolant level sensor which produces a signal when said coolant within said heater is beneath a predetermined level, said signal being operable to terminate operation of said burner.
5. A hot water heating system as in claim 4 wherein coolant replaces said water, said heater circulating said heated coolant through a boat, vehicle or other living area, said heater comprising a coolant stack carrying gases from a burner, said coolant stack being located within a coolant jacket and said coolant stack terminating in an exhaust stack releasing said hot gases to the atmosphere, said coolant stack being in a configuration that allows said exhaust stack to exit said water heater at least two exhaust stack exit locations.
6. A coolant level sensor in a heated coolant and diesel powered heater, said coolant level sensor producing a signal when said coolant within said heater is beneath a predetermined level, said signal being operable to terminate operation of said heater.
7. A coolant level sensor as in claim 6 wherein said coolant is water.
8. Coolant heater for heating coolant and circulating said heated coolant through a boat, vehicle or other living area, said coolant heater comprising a coolant stack carrying gases from a burner, said coolant stack being located within a coolant jacket and said coolant stack terminating in an exhaust stack releasing said hot gases to the atmosphere, said coolant stack being in a configuration that allows said exhaust stack to exit said water heater at at least two exhaust stack exit locations.