SK11692002A3 - Purínové deriváty - Google Patents

Purínové deriváty Download PDF

Info

Publication number: SK11692002A3
Authority: SK; Slovakia
Prior art keywords: amino; carbonyl; purine; ethylamino; carboxamide
Prior art date: 2000-02-18

Application number

SK1169-2002A

Other languages

English (en)

Slovak (sk)

Inventor

Simon John Mantell

Sandra Marina Monaghan

Peter Thomas Stephenson

Original Assignee

Pfizer Inc.

Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)

2000-02-18

Filing date

2001-02-09

Publication date

2003-11-04

2001-02-09 Application filed by Pfizer Inc. filed Critical Pfizer Inc.

2003-11-04 Publication of SK11692002A3 publication Critical patent/SK11692002A3/sk

Links

229940083251 peripheral vasodilators purine derivative Drugs 0.000 title description 4
125000000561 purinyl group Chemical class N1=C(N=C2N=CNC2=C1)* 0.000 title 1
150000001875 compounds Chemical class 0.000 claims abstract description 194
238000000034 method Methods 0.000 claims abstract description 101
150000003839 salts Chemical class 0.000 claims abstract description 42
239000012453 solvate Substances 0.000 claims abstract description 27
-1 hydroxy, fluorenyl Chemical group 0.000 claims description 103
239000000203 mixture Substances 0.000 claims description 82
229910052739 hydrogen Inorganic materials 0.000 claims description 43
125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 37
125000004432 carbon atom Chemical group C* 0.000 claims description 33
125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims description 22
125000000217 alkyl group Chemical group 0.000 claims description 21
125000002915 carbonyl group Chemical group [*:2]C([*:1])=O 0.000 claims description 21
125000000579 2,2-diphenylethyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])(C1=C([H])C([H])=C([H])C([H])=C1[H])C([H])([H])* 0.000 claims description 20
125000000031 ethylamino group Chemical group [H]C([H])([H])C([H])([H])N([H])[*] 0.000 claims description 20
IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims description 18
239000001257 hydrogen Substances 0.000 claims description 18
241000124008 Mammalia Species 0.000 claims description 16
125000004093 cyano group Chemical group *C#N 0.000 claims description 14
125000001624 naphthyl group Chemical group 0.000 claims description 14
238000011282 treatment Methods 0.000 claims description 14
208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 13
125000003386 piperidinyl group Chemical group 0.000 claims description 13
229910052799 carbon Inorganic materials 0.000 claims description 12
125000000753 cycloalkyl group Chemical group 0.000 claims description 12
201000010099 disease Diseases 0.000 claims description 12
125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims description 12
238000004519 manufacturing process Methods 0.000 claims description 11
125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 11
UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims description 10
125000001931 aliphatic group Chemical group 0.000 claims description 10
206010006451 bronchitis Diseases 0.000 claims description 10
239000003814 drug Substances 0.000 claims description 10
125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims description 10
229910052757 nitrogen Inorganic materials 0.000 claims description 10
OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims description 9
208000007882 Gastritis Diseases 0.000 claims description 9
125000002947 alkylene group Chemical group 0.000 claims description 9
125000004169 (C1-C6) alkyl group Chemical group 0.000 claims description 8
125000002733 (C1-C6) fluoroalkyl group Chemical group 0.000 claims description 8
206010001052 Acute respiratory distress syndrome Diseases 0.000 claims description 8
101150051188 Adora2a gene Proteins 0.000 claims description 8
208000013616 Respiratory Distress Syndrome Diseases 0.000 claims description 8
201000000028 adult respiratory distress syndrome Diseases 0.000 claims description 8
229910052736 halogen Inorganic materials 0.000 claims description 8
150000002367 halogens Chemical class 0.000 claims description 8
229940044601 receptor agonist Drugs 0.000 claims description 8
239000000018 receptor agonist Substances 0.000 claims description 8
201000004624 Dermatitis Diseases 0.000 claims description 7
241000590002 Helicobacter pylori Species 0.000 claims description 7
208000006673 asthma Diseases 0.000 claims description 7
229940037467 helicobacter pylori Drugs 0.000 claims description 7
150000002431 hydrogen Chemical class 0.000 claims description 7
125000001436 propyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])[H] 0.000 claims description 7
125000006272 (C3-C7) cycloalkyl group Chemical group 0.000 claims description 6
201000004681 Psoriasis Diseases 0.000 claims description 6
230000001154 acute effect Effects 0.000 claims description 6
208000011341 adult acute respiratory distress syndrome Diseases 0.000 claims description 6
125000004193 piperazinyl group Chemical group 0.000 claims description 6
125000004482 piperidin-4-yl group Chemical group N1CCC(CC1)* 0.000 claims description 6
125000004076 pyridyl group Chemical group 0.000 claims description 6
208000011231 Crohn disease Diseases 0.000 claims description 5
206010014561 Emphysema Diseases 0.000 claims description 5
206010020772 Hypertension Diseases 0.000 claims description 5
208000028017 Psychotic disease Diseases 0.000 claims description 5
206010063837 Reperfusion injury Diseases 0.000 claims description 5
206010040070 Septic Shock Diseases 0.000 claims description 5
208000006011 Stroke Diseases 0.000 claims description 5
229940121363 anti-inflammatory agent Drugs 0.000 claims description 5
239000002260 anti-inflammatory agent Substances 0.000 claims description 5
208000010668 atopic eczema Diseases 0.000 claims description 5
125000001589 carboacyl group Chemical group 0.000 claims description 5
125000000113 cyclohexyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])C1([H])[H] 0.000 claims description 5
230000006378 damage Effects 0.000 claims description 5
206010012601 diabetes mellitus Diseases 0.000 claims description 5
206010015037 epilepsy Diseases 0.000 claims description 5
201000006417 multiple sclerosis Diseases 0.000 claims description 5
125000004433 nitrogen atom Chemical group N* 0.000 claims description 5
230000002093 peripheral effect Effects 0.000 claims description 5
239000000546 pharmaceutical excipient Substances 0.000 claims description 5
206010039083 rhinitis Diseases 0.000 claims description 5
230000036303 septic shock Effects 0.000 claims description 5
230000029663 wound healing Effects 0.000 claims description 5
201000006474 Brain Ischemia Diseases 0.000 claims description 4
206010006458 Bronchitis chronic Diseases 0.000 claims description 4
206010008120 Cerebral ischaemia Diseases 0.000 claims description 4
208000006545 Chronic Obstructive Pulmonary Disease Diseases 0.000 claims description 4
201000003883 Cystic fibrosis Diseases 0.000 claims description 4
206010012434 Dermatitis allergic Diseases 0.000 claims description 4
208000010228 Erectile Dysfunction Diseases 0.000 claims description 4
208000022559 Inflammatory bowel disease Diseases 0.000 claims description 4
125000003545 alkoxy group Chemical group 0.000 claims description 4
125000004103 aminoalkyl group Chemical group 0.000 claims description 4
206010008118 cerebral infarction Diseases 0.000 claims description 4
208000007451 chronic bronchitis Diseases 0.000 claims description 4
239000003085 diluting agent Substances 0.000 claims description 4
210000001035 gastrointestinal tract Anatomy 0.000 claims description 4
201000001881 impotence Diseases 0.000 claims description 4
208000023504 respiratory system disease Diseases 0.000 claims description 4
206010039073 rheumatoid arthritis Diseases 0.000 claims description 4
125000001424 substituent group Chemical group 0.000 claims description 4
208000019553 vascular disease Diseases 0.000 claims description 4
DUWOYHMJSXRWJX-RBANDXJHSA-N 6-(2,2-diphenylethylamino)-9-[(2r,3r,4s,5s)-5-(ethylcarbamoyl)-3,4-dihydroxyoxolan-2-yl]-n-[2-(4-propan-2-ylpiperidin-1-yl)ethyl]purine-2-carboxamide Chemical compound O[C@@H]1[C@H](O)[C@@H](C(=O)NCC)O[C@H]1N1C2=NC(C(=O)NCCN3CCC(CC3)C(C)C)=NC(NCC(C=3C=CC=CC=3)C=3C=CC=CC=3)=C2N=C1 DUWOYHMJSXRWJX-RBANDXJHSA-N 0.000 claims description 3
206010009137 Chronic sinusitis Diseases 0.000 claims description 3
206010009900 Colitis ulcerative Diseases 0.000 claims description 3
201000006704 Ulcerative Colitis Diseases 0.000 claims description 3
125000004183 alkoxy alkyl group Chemical group 0.000 claims description 3
201000008937 atopic dermatitis Diseases 0.000 claims description 3
201000009267 bronchiectasis Diseases 0.000 claims description 3
201000009151 chronic rhinitis Diseases 0.000 claims description 3
208000027157 chronic rhinosinusitis Diseases 0.000 claims description 3
125000004428 fluoroalkoxy group Chemical group 0.000 claims description 3
230000002757 inflammatory effect Effects 0.000 claims description 3
125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims description 3
125000004573 morpholin-4-yl group Chemical group N1(CCOCC1)* 0.000 claims description 3
125000000587 piperidin-1-yl group Chemical group [H]C1([H])N(*)C([H])([H])C([H])([H])C([H])([H])C1([H])[H] 0.000 claims description 3
125000006559 (C1-C3) alkylamino group Chemical group 0.000 claims description 2
125000004214 1-pyrrolidinyl group Chemical group [H]C1([H])N(*)C([H])([H])C([H])([H])C1([H])[H] 0.000 claims description 2
125000004105 2-pyridyl group Chemical group N1=C([*])C([H])=C([H])C([H])=C1[H] 0.000 claims description 2
JYZISXDTPDDOTM-LQHHRKQYSA-N 6-(1,3-diphenylpropan-2-ylamino)-9-[(2r,3r,4s,5s)-5-(ethylcarbamoyl)-3,4-dihydroxyoxolan-2-yl]-n-(2-piperidin-1-ylethyl)purine-2-carboxamide Chemical compound O[C@@H]1[C@H](O)[C@@H](C(=O)NCC)O[C@H]1N1C2=NC(C(=O)NCCN3CCCCC3)=NC(NC(CC=3C=CC=CC=3)CC=3C=CC=CC=3)=C2N=C1 JYZISXDTPDDOTM-LQHHRKQYSA-N 0.000 claims description 2
FUGODAJIZQBSCD-LIHQSLCGSA-N 6-(2,2-diphenylethylamino)-9-[(2r,3r,4s,5s)-5-(ethylcarbamoyl)-3,4-dihydroxyoxolan-2-yl]-n-(2-morpholin-4-ylethyl)purine-2-carboxamide Chemical compound O[C@@H]1[C@H](O)[C@@H](C(=O)NCC)O[C@H]1N1C2=NC(C(=O)NCCN3CCOCC3)=NC(NCC(C=3C=CC=CC=3)C=3C=CC=CC=3)=C2N=C1 FUGODAJIZQBSCD-LIHQSLCGSA-N 0.000 claims description 2
VUQSUSMHWKJISC-CWFKBQJKSA-N 6-(2,2-diphenylethylamino)-9-[(2r,3r,4s,5s)-5-(ethylcarbamoyl)-3,4-dihydroxyoxolan-2-yl]-n-(2-pyridin-2-ylethyl)purine-2-carboxamide Chemical compound O[C@@H]1[C@H](O)[C@@H](C(=O)NCC)O[C@H]1N1C2=NC(C(=O)NCCC=3N=CC=CC=3)=NC(NCC(C=3C=CC=CC=3)C=3C=CC=CC=3)=C2N=C1 VUQSUSMHWKJISC-CWFKBQJKSA-N 0.000 claims description 2
SXFLBSDOSKMUEX-CWFKBQJKSA-N 6-(2,2-diphenylethylamino)-9-[(2r,3r,4s,5s)-5-(ethylcarbamoyl)-3,4-dihydroxyoxolan-2-yl]-n-(3-pyrrolidin-1-ylpropyl)purine-2-carboxamide Chemical compound O[C@@H]1[C@H](O)[C@@H](C(=O)NCC)O[C@H]1N1C2=NC(C(=O)NCCCN3CCCC3)=NC(NCC(C=3C=CC=CC=3)C=3C=CC=CC=3)=C2N=C1 SXFLBSDOSKMUEX-CWFKBQJKSA-N 0.000 claims description 2
LPDBKAZOIXZACQ-BBJOTMRQSA-N 6-(2,2-diphenylethylamino)-9-[(2r,3r,4s,5s)-5-(ethylcarbamoyl)-3,4-dihydroxyoxolan-2-yl]-n-(4-piperidin-1-ylbutyl)purine-2-carboxamide Chemical compound O[C@@H]1[C@H](O)[C@@H](C(=O)NCC)O[C@H]1N1C2=NC(C(=O)NCCCCN3CCCCC3)=NC(NCC(C=3C=CC=CC=3)C=3C=CC=CC=3)=C2N=C1 LPDBKAZOIXZACQ-BBJOTMRQSA-N 0.000 claims description 2
ZNAJCQBHOPNWID-LIHQSLCGSA-N 6-(2,2-diphenylethylamino)-9-[(2r,3r,4s,5s)-5-(ethylcarbamoyl)-3,4-dihydroxyoxolan-2-yl]-n-(piperidin-4-ylmethyl)purine-2-carboxamide Chemical compound O[C@@H]1[C@H](O)[C@@H](C(=O)NCC)O[C@H]1N1C2=NC(C(=O)NCC3CCNCC3)=NC(NCC(C=3C=CC=CC=3)C=3C=CC=CC=3)=C2N=C1 ZNAJCQBHOPNWID-LIHQSLCGSA-N 0.000 claims description 2
XJOCHMTXNBMQKN-RBANDXJHSA-N 6-(2,2-diphenylethylamino)-9-[(2r,3r,4s,5s)-5-(ethylcarbamoyl)-3,4-dihydroxyoxolan-2-yl]-n-[2-(1-propan-2-ylpiperidin-4-yl)ethyl]purine-2-carboxamide Chemical compound O[C@@H]1[C@H](O)[C@@H](C(=O)NCC)O[C@H]1N1C2=NC(C(=O)NCCC3CCN(CC3)C(C)C)=NC(NCC(C=3C=CC=CC=3)C=3C=CC=CC=3)=C2N=C1 XJOCHMTXNBMQKN-RBANDXJHSA-N 0.000 claims description 2
ANGJTPXTEDBIRI-LQHHRKQYSA-N 6-(2,2-diphenylethylamino)-9-[(2r,3r,4s,5s)-5-(ethylcarbamoyl)-3,4-dihydroxyoxolan-2-yl]-n-[2-(4-methylpiperidin-1-yl)ethyl]purine-2-carboxamide Chemical compound O[C@@H]1[C@H](O)[C@@H](C(=O)NCC)O[C@H]1N1C2=NC(C(=O)NCCN3CCC(C)CC3)=NC(NCC(C=3C=CC=CC=3)C=3C=CC=CC=3)=C2N=C1 ANGJTPXTEDBIRI-LQHHRKQYSA-N 0.000 claims description 2
HMGGMKCLHLSIFH-LIHQSLCGSA-N 6-(2,2-diphenylethylamino)-9-[(2r,3r,4s,5s)-5-(ethylcarbamoyl)-3,4-dihydroxyoxolan-2-yl]-n-[2-(5-methyl-1h-imidazol-4-yl)ethyl]purine-2-carboxamide Chemical compound O[C@@H]1[C@H](O)[C@@H](C(=O)NCC)O[C@H]1N1C2=NC(C(=O)NCCC3=C(NC=N3)C)=NC(NCC(C=3C=CC=CC=3)C=3C=CC=CC=3)=C2N=C1 HMGGMKCLHLSIFH-LIHQSLCGSA-N 0.000 claims description 2
UXQNOIHCPQBXSW-LIHQSLCGSA-N 6-(2,2-diphenylethylamino)-9-[(2r,3r,4s,5s)-5-(ethylcarbamoyl)-3,4-dihydroxyoxolan-2-yl]-n-[3-(propan-2-ylamino)propyl]purine-2-carboxamide Chemical compound O[C@@H]1[C@H](O)[C@@H](C(=O)NCC)O[C@H]1N1C2=NC(C(=O)NCCCNC(C)C)=NC(NCC(C=3C=CC=CC=3)C=3C=CC=CC=3)=C2N=C1 UXQNOIHCPQBXSW-LIHQSLCGSA-N 0.000 claims description 2
CSWKLOGHYJISOL-ZVJSOJQNSA-N 6-(2,2-diphenylethylamino)-9-[(2r,3r,4s,5s)-5-(ethylcarbamoyl)-3,4-dihydroxyoxolan-2-yl]-n-[3-[methyl(methylsulfonyl)amino]propyl]purine-2-carboxamide Chemical compound O[C@@H]1[C@H](O)[C@@H](C(=O)NCC)O[C@H]1N1C2=NC(C(=O)NCCCN(C)S(C)(=O)=O)=NC(NCC(C=3C=CC=CC=3)C=3C=CC=CC=3)=C2N=C1 CSWKLOGHYJISOL-ZVJSOJQNSA-N 0.000 claims description 2
125000004541 benzoxazolyl group Chemical group O1C(=NC2=C1C=CC=C2)* 0.000 claims description 2
125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 claims description 2
125000002618 bicyclic heterocycle group Chemical group 0.000 claims description 2
125000002147 dimethylamino group Chemical group [H]C([H])([H])N(*)C([H])([H])[H] 0.000 claims description 2
125000003983 fluorenyl group Chemical group C1(=CC=CC=2C3=CC=CC=C3CC12)* 0.000 claims description 2
125000002541 furyl group Chemical group 0.000 claims description 2
125000005843 halogen group Chemical group 0.000 claims description 2
125000002140 imidazol-4-yl group Chemical group [H]N1C([H])=NC([*])=C1[H] 0.000 claims description 2
125000002883 imidazolyl group Chemical group 0.000 claims description 2
208000027866 inflammatory disease Diseases 0.000 claims description 2
125000002911 monocyclic heterocycle group Chemical group 0.000 claims description 2
125000002757 morpholinyl group Chemical group 0.000 claims description 2
VMCIBFJGIHLADM-TXHDDHBJSA-N n-[2-(dimethylamino)ethyl]-6-(2,2-diphenylethylamino)-9-[(2r,3r,4s,5s)-5-(ethylcarbamoyl)-3,4-dihydroxyoxolan-2-yl]purine-2-carboxamide Chemical compound O[C@@H]1[C@H](O)[C@@H](C(=O)NCC)O[C@H]1N1C2=NC(C(=O)NCCN(C)C)=NC(NCC(C=3C=CC=CC=3)C=3C=CC=CC=3)=C2N=C1 VMCIBFJGIHLADM-TXHDDHBJSA-N 0.000 claims description 2
HFNCQYDXTMXESR-CWFKBQJKSA-N n-[3-(diethylamino)propyl]-6-(2,2-diphenylethylamino)-9-[(2r,3r,4s,5s)-5-(ethylcarbamoyl)-3,4-dihydroxyoxolan-2-yl]purine-2-carboxamide Chemical compound O[C@@H]1[C@H](O)[C@@H](C(=O)NCC)O[C@H]1N1C2=NC(C(=O)NCCCN(CC)CC)=NC(NCC(C=3C=CC=CC=3)C=3C=CC=CC=3)=C2N=C1 HFNCQYDXTMXESR-CWFKBQJKSA-N 0.000 claims description 2
125000004123 n-propyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])* 0.000 claims description 2
125000004430 oxygen atom Chemical group O* 0.000 claims description 2
239000008194 pharmaceutical composition Substances 0.000 claims description 2
125000004592 phthalazinyl group Chemical group C1(=NN=CC2=CC=CC=C12)* 0.000 claims description 2
125000000719 pyrrolidinyl group Chemical group 0.000 claims description 2
125000005493 quinolyl group Chemical group 0.000 claims description 2
125000001567 quinoxalinyl group Chemical group N1=C(C=NC2=CC=CC=C12)* 0.000 claims description 2
201000009890 sinusitis Diseases 0.000 claims description 2
229910052717 sulfur Inorganic materials 0.000 claims description 2
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ZPFGTLTZVCPULS-LQHHRKQYSA-N 6-(2,2-diphenylethylamino)-9-[(2r,3r,4s,5s)-5-(ethylcarbamoyl)-3,4-dihydroxyoxolan-2-yl]-n-(2-phenylethyl)purine-2-carboxamide Chemical compound O[C@@H]1[C@H](O)[C@@H](C(=O)NCC)O[C@H]1N1C2=NC(C(=O)NCCC=3C=CC=CC=3)=NC(NCC(C=3C=CC=CC=3)C=3C=CC=CC=3)=C2N=C1 ZPFGTLTZVCPULS-LQHHRKQYSA-N 0.000 claims 1
NZLDCINKSRAJSR-LQHHRKQYSA-N 6-(2,2-diphenylethylamino)-9-[(2r,3r,4s,5s)-5-(ethylcarbamoyl)-3,4-dihydroxyoxolan-2-yl]-n-[3-(pyridin-2-ylamino)propyl]purine-2-carboxamide Chemical compound O[C@@H]1[C@H](O)[C@@H](C(=O)NCC)O[C@H]1N1C2=NC(C(=O)NCCCNC=3N=CC=CC=3)=NC(NCC(C=3C=CC=CC=3)C=3C=CC=CC=3)=C2N=C1 NZLDCINKSRAJSR-LQHHRKQYSA-N 0.000 claims 1
NNJXUMMOWJZHQG-WKGYELDXSA-N 9-[(2r,3r,4s,5s)-5-(ethylcarbamoyl)-3,4-dihydroxyoxolan-2-yl]-6-(pentan-3-ylamino)-n-(2-piperidin-1-ylethyl)purine-2-carboxamide Chemical compound O[C@@H]1[C@H](O)[C@@H](C(=O)NCC)O[C@H]1N1C2=NC(C(=O)NCCN3CCCCC3)=NC(NC(CC)CC)=C2N=C1 NNJXUMMOWJZHQG-WKGYELDXSA-N 0.000 claims 1
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GOBHYUHHXFEITR-ZVJSOJQNSA-N n-[3-(dimethylamino)propyl]-6-(2,2-diphenylethylamino)-9-[(2r,3r,4s,5s)-5-(ethylcarbamoyl)-3,4-dihydroxyoxolan-2-yl]purine-2-carboxamide Chemical compound O[C@@H]1[C@H](O)[C@@H](C(=O)NCC)O[C@H]1N1C2=NC(C(=O)NCCCN(C)C)=NC(NCC(C=3C=CC=CC=3)C=3C=CC=CC=3)=C2N=C1 GOBHYUHHXFEITR-ZVJSOJQNSA-N 0.000 claims 1
230000000414 obstructive effect Effects 0.000 claims 1
125000000286 phenylethyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])C([H])([H])* 0.000 claims 1
125000003170 phenylsulfonyl group Chemical group C1(=CC=CC=C1)S(=O)(=O)* 0.000 claims 1
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238000002360 preparation method Methods 0.000 abstract description 29
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OKKJLVBELUTLKV-UHFFFAOYSA-N Methanol Chemical compound OC OKKJLVBELUTLKV-UHFFFAOYSA-N 0.000 description 84
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239000000243 solution Substances 0.000 description 64
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238000005160 1H NMR spectroscopy Methods 0.000 description 57
RTZKZFJDLAIYFH-UHFFFAOYSA-N Diethyl ether Chemical compound CCOCC RTZKZFJDLAIYFH-UHFFFAOYSA-N 0.000 description 44
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Classifications

- C—CHEMISTRY; METALLURGY
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- C07D473/00—Heterocyclic compounds containing purine ring systems
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
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- C07H19/02—Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof sharing nitrogen
- C07H19/04—Heterocyclic radicals containing only nitrogen atoms as ring hetero atom
- C07H19/16—Purine radicals
- C07H19/167—Purine radicals with ribosyl as the saccharide radical
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- A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
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- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
- A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/12—Antihypertensives
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/14—Vasoprotectives; Antihaemorrhoidals; Drugs for varicose therapy; Capillary stabilisers
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
- C07H13/00—Compounds containing saccharide radicals esterified by carbonic acid or derivatives thereof, or by organic acids, e.g. phosphonic acids
- C07H13/02—Compounds containing saccharide radicals esterified by carbonic acid or derivatives thereof, or by organic acids, e.g. phosphonic acids by carboxylic acids
- C07H13/08—Compounds containing saccharide radicals esterified by carbonic acid or derivatives thereof, or by organic acids, e.g. phosphonic acids by carboxylic acids having the esterifying carboxyl radicals directly attached to carbocyclic rings
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
- C07H15/00—Compounds containing hydrocarbon or substituted hydrocarbon radicals directly attached to hetero atoms of saccharide radicals
- C07H15/02—Acyclic radicals, not substituted by cyclic structures
- C07H15/04—Acyclic radicals, not substituted by cyclic structures attached to an oxygen atom of the saccharide radical
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
- C07H19/00—Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof
- C07H19/02—Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof sharing nitrogen
- C07H19/04—Heterocyclic radicals containing only nitrogen atoms as ring hetero atom
- C07H19/16—Purine radicals

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Health & Medical Sciences (AREA)
Chemical & Material Sciences (AREA)
Organic Chemistry (AREA)
Engineering & Computer Science (AREA)
General Health & Medical Sciences (AREA)
Life Sciences & Earth Sciences (AREA)
Bioinformatics & Cheminformatics (AREA)
Public Health (AREA)
Animal Behavior & Ethology (AREA)
Veterinary Medicine (AREA)
Chemical Kinetics & Catalysis (AREA)
General Chemical & Material Sciences (AREA)
Medicinal Chemistry (AREA)
Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
Pharmacology & Pharmacy (AREA)
Molecular Biology (AREA)
Biochemistry (AREA)
Biotechnology (AREA)
Genetics & Genomics (AREA)
Pulmonology (AREA)
Neurology (AREA)
Biomedical Technology (AREA)
Neurosurgery (AREA)
Heart & Thoracic Surgery (AREA)
Diabetes (AREA)
Dermatology (AREA)
Pain & Pain Management (AREA)
Cardiology (AREA)
Rheumatology (AREA)
Endocrinology (AREA)
Vascular Medicine (AREA)
Crystallography & Structural Chemistry (AREA)
Reproductive Health (AREA)
Orthopedic Medicine & Surgery (AREA)
Obesity (AREA)
Emergency Medicine (AREA)
Gynecology & Obstetrics (AREA)
Psychiatry (AREA)
Immunology (AREA)
Hematology (AREA)

SK1169-2002A 2000-02-18 2001-02-09 Purínové deriváty SK11692002A3 (sk)

Applications Claiming Priority (2)

Application Number	Priority Date	Filing Date	Title
GBGB0003960.2A GB0003960D0 (en)	2000-02-18	2000-02-18	Purine derivatives
PCT/IB2001/000167 WO2001060835A1 (en)	2000-02-18	2001-02-09	Purine derivatives

Publications (1)

Publication Number	Publication Date
SK11692002A3 true SK11692002A3 (sk)	2003-11-04

Family

ID=9886026

Family Applications (1)

Application Number	Title	Priority Date	Filing Date
SK1169-2002A SK11692002A3 (sk)	2000-02-18	2001-02-09	Purínové deriváty

Country Status (39)

Country	Link
US (1)	US6525032B2 (es)
EP (1)	EP1255764B8 (es)
JP (1)	JP2004508284A (es)
KR (1)	KR20030036138A (es)
CN (1)	CN1400975A (es)
AP (1)	AP2002002598A0 (es)
AR (1)	AR027437A1 (es)
AT (1)	ATE325807T1 (es)
AU (1)	AU2001230440A1 (es)
BG (1)	BG106906A (es)
BR (1)	BR0108408A (es)
CA (1)	CA2400619A1 (es)
CO (1)	CO5271668A1 (es)
CR (1)	CR6722A (es)
CZ (1)	CZ20022703A3 (es)
DE (1)	DE60119492T2 (es)
EA (1)	EA004987B1 (es)
EE (1)	EE200200452A (es)
ES (1)	ES2260199T3 (es)
GB (1)	GB0003960D0 (es)
GT (1)	GT200100027A (es)
HN (1)	HN2001000027A (es)
HR (1)	HRP20020676A2 (es)
HU (1)	HUP0301055A2 (es)
IL (1)	IL150543A0 (es)
IS (1)	IS6458A (es)
MA (1)	MA26873A1 (es)
MX (1)	MXPA02008068A (es)
NO (1)	NO20023894L (es)
NZ (1)	NZ519971A (es)
OA (1)	OA12177A (es)
PA (1)	PA8511801A1 (es)
PE (1)	PE20011122A1 (es)
PL (1)	PL357220A1 (es)
SK (1)	SK11692002A3 (es)
SV (1)	SV2002000317A (es)
TN (1)	TNSN01028A1 (es)
WO (1)	WO2001060835A1 (es)
ZA (1)	ZA200206526B (es)

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GB0607951D0 (en) *	2006-04-21	2006-05-31	Novartis Ag	Organic compounds
US8188063B2 (en) *	2006-06-19	2012-05-29	University Of Virginia Patent Foundation	Use of adenosine A2A modulators to treat spinal cord injury
EP1889846A1 (en)	2006-07-13	2008-02-20	Novartis AG	Purine derivatives as A2a agonists
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KR20090073121A (ko)	2006-09-29	2009-07-02	노파르티스 아게	Ｐｉ3ｋ 지질 키나제 억제제로서의 피라졸로피리미딘
BRPI0718266A2 (pt)	2006-10-30	2014-01-07	Novartis Ag	Compostos heterocíclicos como agentes anti-inflamatórios.
JP2008285478A (ja) *	2007-04-16	2008-11-27	Santen Pharmaceut Co Ltd	アデノシンａ２ａ受容体アゴニストを有効成分として含有する緑内障治療剤
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MX371119B (es)	2012-04-03	2020-01-17	Novartis Ag	Productos de combinacion con los inhibidores de cinasa de tirosina y su uso.
JP2016513706A (ja)	2013-03-15	2016-05-16	イノテックファーマシューティカルズコーポレイション	点眼用製剤
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2000
- 2000-02-18 GB GBGB0003960.2A patent/GB0003960D0/en not_active Ceased
2001
- 2001-02-09 HR HRP20020676 patent/HRP20020676A2/hr not_active Application Discontinuation
- 2001-02-09 CZ CZ20022703A patent/CZ20022703A3/cs unknown
- 2001-02-09 NZ NZ519971A patent/NZ519971A/en unknown
- 2001-02-09 PL PL01357220A patent/PL357220A1/xx not_active Application Discontinuation
- 2001-02-09 EE EEP200200452A patent/EE200200452A/xx unknown
- 2001-02-09 EP EP01902583A patent/EP1255764B8/en not_active Expired - Lifetime
- 2001-02-09 AP APAP/P/2002/002598A patent/AP2002002598A0/en unknown
- 2001-02-09 ES ES01902583T patent/ES2260199T3/es not_active Expired - Lifetime
- 2001-02-09 CN CN01805069A patent/CN1400975A/zh active Pending
- 2001-02-09 CA CA002400619A patent/CA2400619A1/en not_active Abandoned
- 2001-02-09 BR BR0108408-9A patent/BR0108408A/pt not_active IP Right Cessation
- 2001-02-09 AU AU2001230440A patent/AU2001230440A1/en not_active Abandoned
- 2001-02-09 EA EA200200770A patent/EA004987B1/ru not_active IP Right Cessation
- 2001-02-09 JP JP2001560219A patent/JP2004508284A/ja active Pending
- 2001-02-09 SK SK1169-2002A patent/SK11692002A3/sk unknown
- 2001-02-09 AT AT01902583T patent/ATE325807T1/de not_active IP Right Cessation
- 2001-02-09 OA OA1200200250A patent/OA12177A/en unknown
- 2001-02-09 DE DE60119492T patent/DE60119492T2/de not_active Expired - Fee Related
- 2001-02-09 KR KR1020027010481A patent/KR20030036138A/ko not_active Abandoned
- 2001-02-09 WO PCT/IB2001/000167 patent/WO2001060835A1/en not_active Ceased
- 2001-02-09 HU HU0301055A patent/HUP0301055A2/hu unknown
- 2001-02-09 MX MXPA02008068A patent/MXPA02008068A/es active IP Right Grant
- 2001-02-09 IL IL15054301A patent/IL150543A0/xx unknown
- 2001-02-12 GT GT200100027A patent/GT200100027A/es unknown
- 2001-02-15 PA PA20018511801A patent/PA8511801A1/es unknown
- 2001-02-15 HN HN2001000027A patent/HN2001000027A/es unknown
- 2001-02-15 CO CO01012091A patent/CO5271668A1/es not_active Application Discontinuation
- 2001-02-15 AR ARP010100690A patent/AR027437A1/es not_active Application Discontinuation
- 2001-02-16 SV SV2001000317A patent/SV2002000317A/es not_active Application Discontinuation
- 2001-02-16 TN TNTNSN01028A patent/TNSN01028A1/fr unknown
- 2001-02-16 PE PE2001000174A patent/PE20011122A1/es not_active Application Discontinuation
- 2001-02-20 US US09/789,236 patent/US6525032B2/en not_active Expired - Fee Related
2002
- 2002-07-05 IS IS6458A patent/IS6458A/is unknown
- 2002-07-05 BG BG106906A patent/BG106906A/xx unknown
- 2002-08-06 CR CR6722A patent/CR6722A/es not_active Application Discontinuation
- 2002-08-12 MA MA26771A patent/MA26873A1/fr unknown
- 2002-08-15 ZA ZA200206526A patent/ZA200206526B/en unknown
- 2002-08-16 NO NO20023894A patent/NO20023894L/no not_active Application Discontinuation

Also Published As

Publication number	Publication date
EP1255764B1 (en)	2006-05-10
CZ20022703A3 (cs)	2003-09-17
DE60119492D1 (de)	2006-06-14
NO20023894D0 (no)	2002-08-16
KR20030036138A (ko)	2003-05-09
EP1255764B8 (en)	2006-06-28
IL150543A0 (en)	2003-02-12
EP1255764A1 (en)	2002-11-13
CN1400975A (zh)	2003-03-05
US20010020089A1 (en)	2001-09-06
ES2260199T3 (es)	2006-11-01
IS6458A (is)	2002-07-05
NO20023894L (no)	2002-10-01
AR027437A1 (es)	2003-03-26
DE60119492T2 (de)	2006-11-09
HN2001000027A (es)	2001-09-11
AU2001230440A1 (en)	2001-08-27
ATE325807T1 (de)	2006-06-15
BR0108408A (pt)	2002-11-26
WO2001060835A8 (en)	2001-11-29
ZA200206526B (en)	2003-10-16
PE20011122A1 (es)	2001-11-06
OA12177A (en)	2006-05-09
PL357220A1 (en)	2004-07-26
TNSN01028A1 (fr)	2005-11-10
HUP0301055A2 (hu)	2003-08-28
EA004987B1 (ru)	2004-10-28
US6525032B2 (en)	2003-02-25
PA8511801A1 (es)	2002-02-21
BG106906A (en)	2003-04-30
CA2400619A1 (en)	2001-08-23
NZ519971A (en)	2004-04-30
WO2001060835A1 (en)	2001-08-23
EE200200452A (et)	2003-12-15
AP2002002598A0 (en)	2002-09-30
MA26873A1 (fr)	2004-12-20
EA200200770A1 (ru)	2002-12-26
JP2004508284A (ja)	2004-03-18
HRP20020676A2 (en)	2004-12-31
SV2002000317A (es)	2002-07-16
GB0003960D0 (en)	2000-04-12
CO5271668A1 (es)	2003-04-30
CR6722A (es)	2003-11-25
MXPA02008068A (es)	2004-04-05
GT200100027A (es)	2001-12-19

Publication	Publication Date	Title
SK11692002A3 (sk)	2003-11-04	Purínové deriváty
EP1292604B1 (en)	2009-05-13	2-aminocarbonyl-9h-purine derivatives
US6900309B1 (en)	2005-05-31	Purine derivatives
DE60002356T2 (de)	2004-02-19	Purin-derivate
SK4742002A3 (en)	2003-05-02	Purine derivatives
CZ20023992A3 (cs)	2003-12-17	Purinové deriváty
US6921753B2 (en)	2005-07-26	Purine derivatives
US6753322B2 (en)	2004-06-22	2-aminocarbonyl-9H-purine derivatives
HK1089447B (en)	2008-08-22	A process for the preparation of 2-aminocarbonyl-9h-purine derivatives and the intermediates thereof