Author: claimsbot

1. A copolymer made of alkylene oxides and glycidyl ethers according to formula (I)
in which
R1 is hydrogen or a C1-C4-alkyl radical,
R2 and R4 are hydrogen or a methyl group,
R3 is an alkyl or aryl radical having 1 to 50 carbon atoms which may also contain heteroatoms,
A is an alkylene unit having 2 to 6 carbon atoms,
x is 0 or 1,
y is 0 or 1,
n is a number from 2 to 50,
k is a number from 1 to 100,
R5 is an acid group or hydrogen, and
m is a number from 2 to 100,
with the proviso that (y+n) must be at least 2.
2. The copolymer as claimed in claim 1, in which R5 is the radical of a dibasic or tribasic acid.

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 liquid phase process for the synthesis of mesitylene in the absence of added hydrogen which comprises treating pseudocumene with a catalytic composition comprising a zeolite, in acid or prevalently acid form, selected from ZSM-5 zeolite having a crystal lattice made up of silicon oxide and aluminum oxide, and ZSM-5 modified by the partial or total substitution of Si with a tetravalent element andor the partial or total substitution of Al with other trivalent elements, wherein said process is carried out exclusively in the liquid phase at a temperature of from 250 to 375\xb0 C. and a pressure of between 5 and 50 bar, and wherein said process is conducted in the absence of added hydrogen.
2. The process according to claim 1, wherein the catalytic composition comprises ZSM-5 zeolite having a crystal lattice made up of silicon oxide and aluminum oxide.
3. The process according to claim 2, wherein the molar ratio between silicon oxide and aluminum oxide is higher than 20.
4. The process according to claim 3, wherein the molar ratio between silicon oxide and aluminum oxide ranges from 20 to 1000.
5. The process according to claim 4, wherein the molar ratio between silicon oxide and aluminum oxide ranges from 25 to 300.
6. The process according to claim 1, wherein the catalytic composition comprises the zeolite in a bound form, with a binder selected from alumina, silica, magnesia, zirconia or mixtures thereof.
7. The process according to claim 6, wherein the weight ratio between zeolite and binder ranges from 5:95 to 95:5.
8. The process according to claim 7, wherein the weight ratio ranges from 20:80 to 80:20.
9. The process according to claim 1, wherein the WHSV space velocity is between 0.1 and 10 hours\u22121.
10. The process according to claim 1, carried out continuously, in a fixed bed reactor.
11. The process according to claim 1, wherein the pseudocumene is de-oxygenated before being treated with the catalytic composition.
12. The process according to claim 11, wherein the pseudocumene is de-oxygenated by means of degassing by saturation with an inert gas or by boiling.
13. The process according to claim 1, wherein the pseudocumene used comes directly from distillation, without intermediate storage.
14. The process according to claim 1, wherein said catalytic composition comprises ZSM-5 modified by the partial or total substitution of Si with a tetravalent element andor the partial or total substitution of Al with other trivalent elements.
15. The process according to claim 14, wherein said catalytic composition comprises ZSM-5 modified by the partial or total substitution of Si with Ti or Ge andor the partial or total substitution of Al with Fe, Ga or B.
16. The process according to claim 1, wherein said process consists essentially of contacting said catalytic composition with said pseudocumene.
17. A process for regenerating a catalyst, at least partially exhausted, which comprises treating said catalyst at a temperature ranging from 450 to 550\xb0 C., at a pressure ranging from 1 to 3 bar, with mixtures of oxygen and nitrogen in a ratio ranging from 0.1 to 20% by volume, and with a GHSV space velocity of between 3000 and 6000 hours\u22121, wherein said catalyst is a catalyst previously used in a process for the synthesis of mesitylene which comprises treating pseudocumene with a catalytic composition comprising a zeolite, in acid or prevalently acid form, selected from ZSM-5 zeolite having a crystal lattice made up of silicon oxide and aluminum oxide, and ZSM-5 modified by the partial or total substitution of Si with a tetravalent element andor the partial or total substitution of Al with other trivalent elements.

What is claimed:

1. A compound of the following formula:
113
wherein:
R1 are the same or different and independently selected from the group consisting of:
H;
C1-C6-straight chain alkyl;
C2-C6-straight alkenyl chain;
C3-C6-branched alkyl chain;
C3-C6-branched alkenyl chain;
C3-C7-cycloalkyl;
CH2-(C3-C7-cycloalkyl);
CH2CF3;
CH2CH2CF3; and
CH(CF3)2;

the combination of X, D, and Q are either:
DQN and XCH; or
DXN and QCH; or
QXN and DCH; or
QN and DXCH;

VNH;
O;
S; or
CH2;

R2phenyl;
substituted phenyl, wherein the substituents (1-2 in number) are in any position and are independently selected from the group consisting of R1, OR1, SR1, S(O)R1, S(O2)R1, NHR1, NO2, OC(O)CH3, NHC(O)CH3, F, Cl, Br, CF3, C(O)R1, C(O)NHR1, phenyl, and C(O)NHCHR1CH2OH;
1-naphthyl;
2-naphthyl;
heterocycles selected from the group consisting of:
2-pyridyl;
3-pyridyl;
4-pyridyl;
2-pyrimidyl;
4-pyrimidyl;
5-pyrimidyl;
thiophene-2-yl;
thiophene-3-yl;
2-furanyl;
3-furanyl;
oxazol-2-yl;
oxazol-4-yl;
oxazol-5-yl;
thiazol-2-yl;
thiazol-4-yl;
thiazol-5-yl;
imidazol-2-yl;
imidazol-4-yl;
pyrazol-3-yl;
pyrazol-4-yl;
isoxazol-3-yl;
isoxazol-4-yl;
isoxazol-5-yl;
isothiazol-3-yl;
isothiazol-4-yl;
isothiazol-5-yl;
1,3,4-thiadiazol-2-yl;
benzobfuran-2-yl;
benzobthiophene-2-yl;
2-pyrrolyl;
3-pyrrolyl;
1,3,5-triazin-2-yl;
pyrazin-2-yl;
pyridazin-3-yl;
pyridazin-4-yl;
2-quinolinyl;
3-quinolinyl;
4-quinolinyl;
1-isoquinolinyl;
3-isoquinolinyl; and
4-isoquinolinyl; or

substituted heterocycle, wherein the substituents (1-2 in number) are in any position and are independently selected from the group consisting of Br, Cl, F, R1, and C(O)CH3;

R3 are the same or different and independently selected from the group consisting of:
H;
C1-C4-straight chain alkyl;
C3-C4-branched chain alkyl;
C2-C4-alkenyl chain;
(CH2)nPh; and
(CH2)n-substituted phenyl, wherein the phenyl substituents are as defined above in R2;

R4H;
C1-C4-straight chain alkyl; or
C3-C4-branched chain alkyl;

R3 and R4 can be linked together by a carbon chain to form with intervening atoms a 5-8-membered saturated or unsaturated ring;
n10-3;
n0-3;
ACH2;
(CH2)2;
(CH2)3;
OCH2CH2; or
CHCH3;

YH;
OR1;
N(R1)2;
N(R1)C(O)R3;
N(R1)C(O)R5;
N(R1)C(O)CH(R6)NH2;
N(R1)SO2R3;
N(R1)C(O)NHR3; or
N(R1)C(O)OR6;

R5C3-C7-cycloalkyl;
R6C1-C4-straight chain alkyl;
C3-C4-branched chain alkyl;
C2-C4-alkenyl chain;
(CH2)nPh; or
(CH2)n-substituted phenyl, wherein the phenyl substituents are as defined above in R2;
or a pharmaceutically acceptable salt thereof.
2. A compound according to claim 1, wherein
R3 are the same or different and independently selected from the group consisting of:
H;
C1-C4-straight chain alkyl; and
C3-C4-branched chain alkyl;

YH;
OR1;
N(R1)2;
N(R1)C(O)R3;
N(R1)SO2R3; or
N(R1)C(O)NHR3.
3. A compound according to claim 1, wherein two of X, D, and QN;
R3 are the same or different and independently selected from the group consisting of:
H;
C1-C4-straight chain alkyl; and
C3-C4-branched chain alkyl;

YH;
N(R1)2;
N(R1)C(O)R3;
N(R1)SO2R3; or
N(R1)C(O)NHR3;
or a pharmaceutically acceptable salt thereof.
4. A compound of the following formula:
114
wherein:
R1 are the same or different and independently selected from the group consisting of:
H;
C1-C6-straight chain alkyl;
C2-C6-straight alkenyl chain;
C3-C6-branched alkyl chain;
C3-C6-branched alkenyl chain;
C3-C7-cycloalkyl;
CH2(C3-C7-cycloalkyl);
CH2CF3;
CH2CH2CF3; and
CH(CF3)2;

the combination of X, D, and Q are either:
DQN and XCH; or
DXN and QCH; or
QXN and DCH; or
QN and DXCH;

VNH;
O;
S; or
CH2;

R2phenyl;
substituted phenyl, wherein the substituents (1-2 in number) are in any position and are independently selected from the group consisting of R1, OR1, SR1, S(O)R1, S(O2)R1, NHR1, NO2, OC(O)CH3, NHC(O)CH3, F, Cl, Br, CF3, C(O)R1, C(O)NHR1, phenyl, and C(O)NHCHR1CH2OH;
1-naphthyl;
2-naphthyl;
heterocycles selected from the group consisting of:
2-pyridyl;
3-pyridyl;
4-pyridyl;
2-pyrimidyl;
4-pyrimidyl;
5-pyrimidyl;
thiophene-2-yl;
thiophene-3-yl;
2-furanyl;
3-furanyl;
oxazol-2-yl;
oxazol-4-yl;
oxazol-5-yl;
thiazol-2-yl;
thiazol-4-yl;
thiazol-5-yl;
imidazol-2-yl;
imidazol-4-yl;
pyrazol-3-yl;
pyrazol-4-yl;
isoxazol-3-yl;
isoxazol-4-yl;
isoxazol-5-yl;
isothiazol-3-yl;
isothiazol-4-yl;
isothiazol-5-yl;
1,3,4-thiadiazol-2-yl;
benzobfuran-2-yl;
benzobthiophene-2-yl;
2-pyrrolyl;
3-pyrrolyl;
1,3,5-triazin-2-yl;
pyrazin-2-yl;
pyridazin-3-yl;
pyridazin-4-yl;
2-quinolinyl;
3-quinolinyl;
4-quinolinyl;
1-isoquinolinyl;
3-isoquinolinyl; and
4-isoquinolinyl; or

substituted heterocycle, wherein the substituents (1-2 in number) are in any position and are independently selected from the group consisting of Br, Cl, F, R1, and C(O)CH3;

n0-3;
ACH2;
(CH2)2;
(CH2)3;
OCH2CH2; or
CHCH3;

YH;
OR1;
N(R1)2;
N(R1)C(O)R3;
N(R1)C(O)R5;
N(R1)C(O)CH(R6)NH2;
N(R1)SO2R3;
N(R1)C(O)NHR3; or
N(R1)C(O)OR6;

R3 are the same or different and independently selected from the group consisting of:
H;
C1-C4-straight chain alkyl;
C3-C4-branched chain alkyl;
C2-C4-alkenyl chain;
(CH2)nPh; and
(CH2)n-substituted phenyl, wherein the phenyl substituents are as defined above in R2;

R5C3-C7-cycloalkyl;
R6C1-C4-straight chain alkyl;
C3-C4-branched chain alkyl; or
C2-C4-alkenyl chain;
or a pharmaceutically acceptable salt thereof.
5. A compound according to claim 4, wherein two of X, D, and QN.
6. A method of treating a mammal with a disorder mediated by elevated levels of cell proliferation compared to a healthy mammal comprising:
administering a therapeutically effective amount of the compound of claim 1 to the mammal under conditions effective to treat the disorder mediated by elevated levels of cell proliferation compared to a healthy mammal.
7. The method of claim 6, wherein the disorder mediated by elevated levels of cell proliferation compared to a healthy mammal is cancer, wherein the cancer is selected from the group consisting of breast cancer, colon cancer, central nervous system cancer, leukemia, melanoma, lung cancer, ovarian cancer, prostate cancer, and renal cancer.
8. The method of claim 7, wherein the disorder mediated by elevated levels of cell proliferation compared to a healthy mammal is restenosis.
9. The method of claim 7, wherein the mammal is human.
10. A pharmaceutical composition of matter comprising the compound of claim 1 and one or more pharmaceutical excipients.
11. A method of treating a mammal with a disorder mediated by elevated levels of cell proliferation compared to a healthy mammal comprising:
administering a therapeutically effective amount of the compound of claim 4 to the mammal under conditions effective to treat the disorder mediated by elevated levels of cell proliferation compared to a healthy mammal.
12. The method of claim 11, wherein the disorder mediated by elevated levels of cell proliferation compared to a healthy mammal is cancer, wherein the cancer is selected from the group consisting of breast cancer, colon cancer, central nervous system cancer, leukemia, melanoma, lung cancer, ovarian cancer, prostate cancer, and renal cancer.
13. The method of claim 11, wherein the disorder mediated by elevated levels of cell proliferation compared to a healthy mammal is restenosis.
14. The method of claim 11, wherein the mammal is human.
15. A pharmaceutical composition of matter comprising the compound of claim 4 and one or more pharmaceutical excipients.
16. A process for preparation of a purine derivative compound of the formula:
115
wherein:
R1 are the same or different and independently selected from the group consisting of:
H;
C1-C6-straight chain alkyl;
C2-C6-straight alkenyl chain;
C3-C6-branched alkyl chain;
C3-C6-branched alkenyl chain;
C3-C7-cycloalkyl;
CH2(C3-C7-cycloalkyl);
CH2CF3;
CH2CH2CF3; and
CH(CF3)2;

the combination of X, D, and Q are either:
DQN, and XCH; or
DXN, and QCH; or
QXN, and DCH; or
QN, and DXCH;

VNH;
O;
S; or
CH2;

R2phenyl;
substituted phenyl, wherein the substituents (1-2 in number) are in any position and are independently selected from the group consisting of R1, OR1, SR1, S(O)R1, S(O2)R1, NHR1, NO2, OC(O)CH3, NHC(O)CH3, F,
Cl, Br, CF3, C(O)R1, C(O)NHR1, phenyl, and C(O)NHCHR1CH2OH;
1-naphthyl;
2-naphthyl;
heterocycles selected from the group consisting of:
2-pyridyl;
3-pyridyl;
4-pyridyl;
2-pyrimidyl;
4-pyrimidyl;
5-pyrimidyl;
thiophene-2-yl;
thiophene-3-yl;
2-furanyl;
3-furanyl;
oxazol-2-yl;
oxazol-4-yl;
oxazol-5-yl;
thiazol-2-yl;
thiazol-4-yl;
thiazol-5-yl;
imidazol-2-yl;
imidazol-4-yl;
pyrazol-3-yl;
pyrazol-4-yl;
isoxazol-3-yl;
isoxazol-4-yl;
isoxazol-5-yl;
isothiazol-3-yl;
isothiazol-4-yl;
isothiazol-5-yl;
1,3,4-thiadiazol-2-yl;
benzobfuran-2-yl;
benzobthiophene-2-yl;
2-pyrrolyl;
3-pyrrolyl;
1,3,5-triazin-2-yl;
pyrazin-2-yl;
pyridazin-3-yl;
pyridazin-4-yl;
2-quinolinyl;
3-quinolinyl;
4-quinolinyl;
1-isoquinolinyl;
3-isoquinolinyl; and
4-isoquinolinyl; or

substituted heterocycle, wherein the substituents (1-2 in number) are in any position and are independently selected from the group consisting of Br, Cl, F, R1, and C(O)CH3;

R3 are the same or different and independently selected from the group consisting of:
H;
C1-C4-straight chain alkyl;
C3-C4-branched chain alkyl;
C2-C4-alkenyl chain;
(CH2)nPh; and
(CH2)n-substituted phenyl, wherein the phenyl substituents are as defined above in R2;

R4H;
C1-C4-straight chain alkyl; or
C3-C4-branched chain alkyl;

R3 and R4 can be linked together by a carbon chain to form with intervening atoms a 5-8-membered saturated or unsaturated ring;
n10-3;
n0-3;
ACH2;
(CH2)2;
(CH2)3;
OCH2CH2; or
CHCH3;

YH;
OR1;
N(R1)2;
N(R1)C(O)R3;
N(R1)C(O)R5;
N(R1)C(O)CH(R6)NH2;
N(R1)SO2R3;
N(R1)C(O)NHR3; or
N(R1)C(O)OR6;

R5C3-C7-cycloalkyl;
R6C1-C4-straight chain alkyl;
C3-C4-branched chain alkyl;
C2-C4-alkenyl chain;
(CH2)nPh; or
(CH2)n-substituted phenyl, wherein the phenyl substituents are as defined above in R2;
or a pharmaceutically acceptable salt thereof;
said process comprising:

reacting a first intermediate compound of the formula:
116
where ZBr or I
with a compound of the formula: R2B(OH)2, R2Sn(n-Bu)3, or R2Sn(Me)3, or mixtures thereof, under conditions effective to form the purine derivative compound.
17. A process according to claim 16, wherein if Y is NHR1, said process further comprises:
reacting the purine derivative compound with R3C(O)Cl or R5C(O)Cl or R3SO2Cl or R3NCO or R6OC(O)Cl under conditions effective to form a final product having the same formula as the purine derivative compound except that Y is NR1C(O)R3 or NR1C(O)R5 or NR1SO2R3 or NR1C(O)NHR3 or NR1C(O)OR6.
18. A process according to claim 16 further comprising:
reacting a second intermediate compound of the formula:
117
with a second compound of the formula:
118
wherein: V1NH2;
OH;
SH;
under conditions effective to form the first intermediate compound.
19. A process according to claim 18 further comprising:
reacting a third intermediate compound of the formula:
119
with a compound of the formula R1-Z under conditions effective to form the second intermediate compound.
20. A process according to claim 16, wherein the purine derivative compound has the formula:
120
21. A process for preparation of a purine derivative compound of the formula:
121
wherein:
R1 are the same or different and independently selected from the group consisting of:
H;
C1-C6-straight chain alkyl;
C2-C6-straight alkenyl chain;
C3-C6-branched alkyl chain;
C3-C6-branched alkenyl chain;
C3-C7-cycloalkyl;
CH2(C3-C7-cycloalkyl);
CH2CF3;
CH2CH2CF3; and
CH(CF3)2;

the combination of X, D, and Q are either:
DQN, and XCH; or
DXN, and QCH; or
QXN, and DCH; or
QN, and DXCH;

VNH;
O;
S; or
CH2;

R2phenyl;
substituted phenyl, wherein the substituents (1-2 in number) are in any position and are independently selected from the group consisting of R1, OR1, SR1, S(O)R1, S(O2)R1, NHR1, NO2, OC(O)CH3, NHC(O)CH3, F, Cl, Br, CF3, C(O)R1, C(O)NHR1, phenyl, and C(O)NHCHR1CH2OH;
1-naphthyl;
2-naphthyl;
heterocycles selected from the group consisting of:
2-pyridyl;
3-pyridyl;
4-pyridyl;
2-pyrimidyl;
4-pyrimidyl;
5-pyrimidyl;
thiophene-2-yl;
thiophene-3-yl;
2-furanyl;
3-furanyl;
oxazol-2-yl;
oxazol-4-yl;
oxazol-5-yl;
thiazol-2-yl;
thiazol-4-yl;
thiazol-5-yl;
imidazol-2-yl;
imidazol-4-yl;
pyrazol-3-yl;
pyrazol-4-yl;
isoxazol-3-yl;
isoxazol-4-yl;
isoxazol-5-yl;
isothiazol-3-yl;
isothiazol-4-yl;
isothiazol-5-yl;
1,3,4-thiadiazol-2-yl;
benzobfuran-2-yl;
benzobthiophene-2-yl;
2-pyrrolyl;
3-pyrrolyl;
1,3,5-triazin-2-yl;
pyrazin-2-yl;
pyridazin-3-yl;
pyridazin-4-yl;
2-quinolinyl;
3-quinolinyl;
4-quinolinyl;
1-isoquinolinyl;
3-isoquinolinyl; and
4-isoquinolinyl; or

substituted heterocycle, wherein the substituents (1-2 in number) are in any position and are independently selected from the group consisting of Br, Cl, F, R1, and C(O)CH3;

R3 are the same or different and independently selected from the group consisting of:
H;
C1-C4-straight chain alkyl;
C3-C4-branched chain alkyl;
C2-C4-alkenyl chain;
(CH2)nPh; and
(CH2)n-substituted phenyl, wherein the phenyl substituents are as defined above in R2;

R4H;
C1-C4-straight chain alkyl; or
C3-C4-branched chain alkyl;

R3 and R4 can be linked together by a carbon chain to form with intervening atoms a 5-8-membered saturated or unsaturated ring;
n10-3;
n0-3;
ACH2;
(CH2)2;
(CH2)3;
OCH2CH2;
CHCH3;

YH;
OR1;
N(R1)2;
N(R1)C(O)R3;
N(R1)C(O)R5;
N(R1)C(O)CH(R6)NH2;
N(R1)SO2R3;
N(R1)C(O)NHR3; or
N(R1)C(O)OR6;

R5C3-C7-cycloalkyl;
R6C1-C4-straight chain alkyl;
C3-C4-branched chain alkyl;
C2-C4-alkenyl chain;
(CH2)nPh; or
(CH2)n-substituted phenyl, wherein the phenyl substituents are as defined above in R2;
or a pharmaceutically acceptable salt thereof, said process comprising:

reacting a first intermediate compound of the formula:
122
under reductive or hydrogenation conditions effective to form the purine derivative compound.
22. A process according to claim 21 further comprising:
reacting a second intermediate compound of the formula:
123
with a second compound of the formula:
124
under conditions effective to form the first intermediate compound.
23. A process according to claim 22 further comprising:
reacting a third intermediate compound of the formula:
125
with a compound of the formula: R2B(OH)2, R2Sn(n-Bu)3, or R2Sn(Me)3, or mixtures thereof, under conditions effective to form the second intermediate compound.
24. A process according to claim 21 further comprising:
reacting a fourth intermediate compound of the formula:
126
with a compound of the formula: R2B(OH)2, R2Sn(n-Bu)3, or R2Sn(Me)3, or mixtures thereof, under conditions effective to form the first intermediate compound.
25. A process according to claim 24 further comprising:
reacting a fifth intermediate compound of the formula:
127
with a compound of the formula:
128
under conditions effective to form the fourth intermediate compound.
26. A process according to claim 21, wherein the purine derivative compound has the formula:
129
27. A process for preparation of a purine derivative compound of the formula:
130
wherein:
R1 are the same or different and independently selected from the group consisting of:
H;
C1-C6-straight chain alkyl;
C2-C6-straight alkenyl chain;
C3-C6-branched alkyl chain;
C3-C6-branched alkenyl chain;
C3-C7-cycloalkyl;
CH2(C3-C7-cycloalkyl);
CH2CF3;
CH2CH2CF3; and
CH(CF3)2;

the combination of X, D, and Q are either:
DQN, and XCH; or
DXN, and QCH; or
QXN, and DCH; or
QN, and DXCH;

VNH;
O;
S; or
CH2;

R2phenyl;
substituted phenyl, wherein the substituents (1-2 in number) are in any position and are independently selected from the group consisting of R1, OR1, SR1, S(O)R1, S(O2)R1, NHR1, NO2, OC(O)CH3, NHC(O)CH3, F, Cl, Br, CF3, C(O)R1, C(O)NHR1, phenyl, and C(O)NHCHR1CH2OH;
1-naphthyl;
2-naphthyl;
heterocycles selected from the group consisting of:
2-pyridyl;
3-pyridyl;
4-pyridyl;
2-pyrimidyl;
4-pyrimidyl;
5-pyrimidyl;
thiophene-2-yl;
thiophene-3-yl;
2-furanyl;
3-furanyl;
oxazol-2-yl;
oxazol-4-yl;
oxazol-5-yl;
thiazol-2-yl;
thiazol-4-yl;
thiazol-5-yl;
imidazol-2-yl;
imidazol-4-yl;
pyrazol-3-yl;
pyrazol-4-yl;
isoxazol-3-yl;
isoxazol-4-yl;
isoxazol-5-yl;
isothiazol-3-yl;
isothiazol-4-yl;
isothiazol-5-yl;
1,3,4-thiadiazol-2-yl;
benzobfuran-2-yl;
benzobthiophene-2-yl;
2-pyrrolyl;
3-pyrrolyl;
1,3,5-triazin-2-yl;
pyrazin-2-yl;
pyridazin-3-yl;
pyridazin-4-yl;
2-quinolinyl;
3-quinolinyl;
4-quinolinyl;
1-isoquinolinyl;
3-isoquinolinyl; and
4-isoquinolinyl; or

substituted heterocycle, wherein the substituents (1-2 in number) are in any position and are independently selected from the group consisting of Br, Cl, F, R1, and C(O)CH3;

R3 are the same or different and independently selected from the group consisting of:
H;
C1-C4-straight chain alkyl;
C3-C4-branched chain alkyl;
C2-C4-alkenyl chain;
(CH2)nPh; and
(CH2)n-substituted phenyl, wherein the phenyl substituents are as defined above in R2;

R4H;
C1-C4-straight chain alkyl; or
C3-C4-branched chain alkyl;

R3 and R4 can be linked together by a carbon chain to form with intervening atoms a 5-8-membered saturated or unsaturated ring;
n10-3;
n0-3;
ACH2;
(CH2)2;
(CH2)3;
OCH2CH2; or
CHCH3;

YH;
OR1;
N(R1)2;
N(R1)C(O)R3;
N(R1)C(O)R5;
N(R1)C(O)CH(R6)NH2;
N(R1)SO2R3;
N(R1)C(O)NHR3; or
N(R1)C(O)OR6;

R5C3-C7-cycloalkyl;
R6C1-C4-straight chain alkyl;
C3-C4-branched chain alkyl;
C2-C4-alkenyl chain;
(CH2)nPh; or
(CH2)n-substituted phenyl, wherein the phenyl substituents are as defined above in R2; or a pharmaceutically acceptable salt thereof; said process comprising:
reacting a first intermediate compound of the formula:
131
with a compound of the formula:
132
where V1NH2;
OH; or
SH;
under conditions effective to form the purine derivative compound.
28. A process according to claim 27, wherein if Y is NHR1, said process further comprises:
reacting the purine derivative compound with R3C(O)Cl or R5C(O)Cl or R3SO2Cl or R3NCO or R6OC(O)Cl under conditions effective to form a final product having the same formula as the purine derivative compound except that Y is NR1C(O)R3 or NR1C(O)R5 or NR1SO2R3 or NR1C(O)NHR3 or NR1C(O)OR6.
29. A process according to claim 27 further comprising:
reacting a second intermediate compound of the formula:
133
with a compound of the formula R1-Z under conditions effective to form the first intermediate compound.
30. A process according to claim 29 further comprising:
reacting a third intermediate compound of the formula:
134
with a compound of the formula 2,6-dichloropurine (Formula IV) under conditions effective to form the second intermediate compound.
31. A process according to claim 30 further comprising:
reacting a fourth intermediate compound of the formula:
135
with a compound of the formula: R2B(OH)2, R2Sn(n-Bu)3, or R2Sn(Me)3, or mixtures thereof, under conditions effective to form the third intermediate compound.
32. A process according to claim 28, wherein the purine derivative compound has the formula:
136
33. A process for preparation of a purine derivative compound of the formula:
137
wherein:
R1 are the same or different and independently selected from the group consisting of:
H;
C1-C6-straight chain alkyl;
C2-C6-straight alkenyl chain;
C3-C6-branched alkyl chain;
C3-C6-branched alkenyl chain;
C3-C7-cycloalkyl;
CH2(C3-C7-cycloalkyl);
CH2CF3;
CH2CH2CF3; and
CH(CF3)2;

the combination of X, D, and Q are either:
DQN and XCH; or
DXN and QCH; or
QXN and DCH; or
QN and DXCH;

VNH;
O;
S; or
CH2;

R2phenyl;
substituted phenyl, wherein the substituents (1-2 in number) are in any position and are independently selected from the group consisting of R1, OR1, SR1, S(O)R1, S(O2)R1, NHR1, NO2, OC(O)CH3, NHC(O)CH3, F, Cl, Br, CF3, C(O)R1, C(O)NHR1, phenyl, and C(O)NHCHR1CH2OH;
1-naphthyl;
2-naphthyl;
heterocycles selected from the group consisting of:
2-pyridyl;
3-pyridyl;
4-pyridyl;
2-pyrimidyl;
4-pyrimidyl;
5-pyrimidyl;
thiophene-2-yl;
thiophene-3-yl;
2-furanyl;
3-furanyl;
oxazol-2-yl;
oxazol-4-yl;
oxazol-5-yl;
thiazol-2-yl;
thiazol-4-yl;
thiazol-5-yl;
imidazol-2-yl;
imidazol-4-yl;
pyrazol-3-yl;
pyrazol-4-yl;
isoxazol-3-yl;
isoxazol-4-yl;
isoxazol-5-yl;
isothiazol-3-yl;
isothiazol-4-yl;
isothiazol-5-yl;
1,3,4-thiadiazol-2-yl;
benzobfuran-2-yl;
benzobthiophene-2-yl;
2-pyrrolyl;
3-pyrrolyl;
1,3,5-triazin-2-yl;
pyrazin-2-yl;
pyridazin-3-yl;
pyridazin-4-yl;
2-quinolinyl;
3-quinolinyl;
4-quinolinyl;
1-isoquinolinyl;
3-isoquinolinyl; and
4-isoquinolinyl; or

substituted heterocycle, wherein the substituents (1-2 in number) are in any position and are independently selected from the group consisting of Br, Cl, F, R1, and C(O)CH3;

R3 are the same or different and independently selected from the group consisting of:
H;
C1-C4-straight chain alkyl;
C3-C4-branched chain alkyl;
C2-C4-alkenyl chain;
(CH2)nPh; and
(CH2)n-substituted phenyl, wherein the phenyl substituents are as defined above in R2;

R4H;
C1-C4-straight chain alkyl; or
C3-C4-branched chain alkyl;

R3 and R4 can be linked together by a carbon chain to form with intervening atoms a 5-8-membered saturated or unsaturated ring;
n10-3;
n0-3;
ACH2;
(CH2)2;
(CH2)3;
OCH2CH2; or
CHCH3;

YNR1C(O)R3;
NR1SO2R3;
NR1C(O)NHR3;or
NR1C(O)OR6

R5C3-C7-cycloalkyl;
R6C1-C4-straight chain alkyl;
C3-C4-branched chain alkyl;
C2-C4-alkenyl chain;
(CH2)nPh; or
(CH2)n-substituted phenyl, wherein the phenyl substituents are as defined above in R2;
or a pharmaceutically acceptable salt thereof;
said process comprising:

reacting a first intermediate compound having the same formula as the purine derivative compound except that YNHR1, with R3COCl or R5COCl or R3SO2Cl or R3NCO or R6OC(O)Cl under conditions effective to form the purine derivative compound.
34. A process according to claim 33 further comprising:
reacting a second intermediate compound having the same formula as the first intermediate compound except that Y is NH2, with R8CH2Z or R8CHO under conditions effective to form the first intermediate compound where YNHR1 or N(R1)2, wherein Z is Br or I and R8C1-C5-straight chain alkyl; C2-C5-straight alkenyl chain; C3-C5-branched alkyl chain; C3-C5-branched alkenyl chain; C3-C7-cycloalkyl; CF3; CH2CF3.
35. A process for preparation of a purine derivative compound of the formula:
138
wherein:
R1 are the same or different and independently selected from the group consisting of:
H;
C1-C6-straight chain alkyl;
C2-C6-straight alkenyl chain;
C3-C6-branched alkyl chain;
C3-C6-branched alkenyl chain;
C3-C7-cycloalkyl;
CH2(C3-C7-cycloalkyl);
CH2CF3;
CH2CH2CF3; and
CH(CF3)2;

the combination of X, D, and Q are either:
DQN and XCH; or
DXN and QCH; or
QXN and DCH; or
QN and DXCH;

VNH;
O;
S; or
CH2;

R2phenyl;
substituted phenyl, wherein the substituents (1-2 in number) are in any position and are independently selected from the group consisting of R1, OR1, SR1, S(O)R1, S(O2)R1, NHR1, NO2, OC(O)CH3, NHC(O)CH3, F, Cl, Br, CF3, C(O)R1, C(O)NHR1, phenyl, and C(O)NHCHR1CH2OH;
1-naphthyl;
2-naphthyl;
heterocycles selected from the group consisting of:
2-pyridyl;
3-pyridyl;
4-pyridyl;
2-pyrimidyl;
4-pyrimidyl;
5-pyrimidyl;
thiophene-2-yl;
thiophene-3-yl;
2-furanyl;
3-furanyl;
oxazol-2-yl;
oxazol-4-yl;
oxazol-5-yl;
thiazol-2-yl;
thiazol-4-yl;
thiazol-5-yl;
imidazol-2-yl;
imidazol-4-yl;
pyrazol-3-yl;
pyrazol-4-yl;
isoxazol-3-yl;
isoxazol-4-yl;
isoxazol-5-yl;
isothiazol-3-yl;
isothiazol-4-yl;
isothiazol-5-yl;
1,3,4-thiadiazol-2-yl;
benzobfuran-2-yl;
benzobthiophene-2-yl;
2-pyrrolyl;
3-pyrrolyl;
1,3,5-triazin-2-yl;
pyrazin-2-yl;
pyridazin-3-yl;
pyridazin-4-yl;
2-quinolinyl;
3-quinolinyl;
4-quinolinyl;
1-isoquinolinyl;
3-isoquinolinyl; and
4-isoquinolinyl; or

substituted heterocycle, wherein the substituents (1-2 in number) are in any position and are independently selected from the group consisting of Br, Cl, F, R1, and C(O)CH3;

R3 are the same or different and independently selected from the group consisting of:
H;
C1-C4-straight chain alkyl;
C3-C4-branched chain alkyl;
C2-C4-alkenyl chain;
(CH2)nPh; and
(CH2)n-substituted phenyl, wherein the phenyl substituents are as defined above in R2;

R4H;
C1-C4-straight chain alkyl; or
C3-C4-branched chain alkyl;

R3 and R4 can be linked together by a carbon chain to form with intervening atoms a 5-8-membered saturated or unsaturated ring;
n10-3;
n0-3;
ACH2;
(CH2)2;
(CH2)3;
OCH2CH2; or
CHCH3;

YNHC(O)CH(R6)NH2;
R5C3-C7-cycloalkyl;
R6C1-C4-straight chain alkyl;
C3-C4-branched chain alkyl;
C2-C4-alkenyl chain;
(CH2)nPh; or
(CH2)n-substituted phenyl, wherein the phenyl substituents are as defined above in R2;
or a pharmaceutically acceptable salt thereof;
said process comprising:

reacting a first intermediate compound having the same formula as the purine derivative compound except that Y is NH2, with a compound of the formula: PNHCH(R6)CO2H under conditions effective to form the purine derivative compound after a suitable deprotection strategy,
wherein
PC(O)OtBu;
C(O)OCH2Ph;
Fmoc
Benzyl; or
Alloc.

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. An earplug comprising:
an earplug body of elastomeric material with a body front portion of a size to enter a human ear canal and block sound, said body front portion having a body front end;
a core that is elongated in a front-to-rear direction, that lies in said body, and that is stiffer than said body;
said core is bonded to said body, and said core has a front end that lies rearward of said body front end.
2. The earplug described in claim 1 wherein:
said body front portion includes a quantity of said elastomeric material which lies forward of said front end of said core.
3. The earplug described in claim 1 wherein:
said front end of said core which lies rearward of said body front end, is exposed at the end of a passage, so material of said body does not lie directly in front of most of the area of said core front end.
4. The earplug described in claim 3 wherein:
said body front end has at least one crosscut that extends across the diameter of said body front end.
5. The earplug described in claim 3 wherein:
said body front end has a bore formed in it where said elastomeric material of said body was removed, to leave said core front end exposed.
6. The earplug described in claim 1 wherein:
said body has a body rear portion with a body rear end, and said core has a rear end that lies forward of said body rear end.
7. The earplug described in claim 6 wherein:
the material of said body lies directly behind said core rear end.
8. The earplug described in claim 6 wherein:
said rear end of said core which lies forward of said body rear end, is exposed so material of said body does not lie directly behind most of the area of said core rear end.
9. The earplug described in claim 1 wherein:
said core front end lies a distance A rearward of said body front end, and the distance (B) between a rear end of said body and a rear end of said core is less than said distance A.
10. An earplug comprising:
an earplug body that is formed of resilient foam elastomeric material, said body having front and rear body ends and an axis extending between said ends, and said body having a front portion for entering a person’s ear canal;
a core that is elongated in front-to-rear directions and at least twice as resistant to column compression collapse than said body, said core having front and rear ends and lying in said body and extending along said axis, and said core being bonded to the material of said body;
at least said front end of said core lying a plurality of millimeters rearward of said front end of said body.
11. The earplug described in claim 10 wherein:
said front end of said core is covered by said elastomeric material of said body.
12. The earplug described in claim 10 wherein:
said front end of said core is exposed, said body forming an empty passage of a length of a plurality of millimeters extending from said body front end to said core front end.
13. A method for manufacturing an earplug which includes the extrusion of elastomeric earplug bodies through an extrusion head and around cores of material that are stiffer than said body, while the cores moves rearward through the extrusion head, and cutting said extrusion into lengths on the order of magnitude of one inch, comprising:
cutting a core device into lengths that forms said cores, with each core having front and rear ends, prior to moving said cores through the extrusion head, and controlling the movement of the cores with respect to said step of cutting, so the extrusion is cut at locations that are each more than one millimeter forward of the front end of each core, whereby to produce earplugs with the front end of the core lying rearward of the front end of the body.
14. The method described in claim 13 wherein:
said step of cutting the core device into core lengths includes cutting the core device into cores that are each of a length that is sufficiently less than the length of said extrusion between subsequent cuts of the extrusion, so rear ends of the core lengths do not protrude from rear ends of the earplug bodies.
15. The method described in claim 14 wherein:
said step of cutting said extrusion includes cutting it into earplugs where the cores each have rear ends that lie forward of rear end of the corresponding body.