WO2005113537B1 - Urees antagonistes vis-a-vis du recepteur p2y1 utiles dans le traitement des etats thrombotiques - Google Patents
Urees antagonistes vis-a-vis du recepteur p2y1 utiles dans le traitement des etats thrombotiquesInfo
- Publication number
- WO2005113537B1 WO2005113537B1 PCT/US2005/016525 US2005016525W WO2005113537B1 WO 2005113537 B1 WO2005113537 B1 WO 2005113537B1 US 2005016525 W US2005016525 W US 2005016525W WO 2005113537 B1 WO2005113537 B1 WO 2005113537B1
- Authority
- WO
- WIPO (PCT)
- Prior art keywords
- substituted
- alkyl
- occurrence
- carbon atoms
- heterocycle
- Prior art date
Links
- XSQUKJJJFZCRTK-UHFFFAOYSA-N urea Chemical compound NC(N)=O XSQUKJJJFZCRTK-UHFFFAOYSA-N 0.000 title abstract 4
- 108010028935 Purinergic P2Y1 Receptors Proteins 0.000 title abstract 3
- 102000016927 Purinergic P2Y1 Receptors Human genes 0.000 title abstract 3
- 230000003042 antagnostic Effects 0.000 title 1
- 239000005557 antagonist Substances 0.000 title 1
- 239000004202 carbamide Substances 0.000 title 1
- 230000001732 thrombotic Effects 0.000 title 1
- 125000000623 heterocyclic group Chemical group 0.000 claims abstract 96
- 125000000217 alkyl group Chemical group 0.000 claims 104
- 125000004432 carbon atoms Chemical group C* 0.000 claims 72
- 229910052760 oxygen Inorganic materials 0.000 claims 50
- 125000005842 heteroatoms Chemical group 0.000 claims 49
- 229910052717 sulfur Inorganic materials 0.000 claims 43
- JCXJVPUVTGWSNB-UHFFFAOYSA-N nitrogen dioxide Chemical compound O=[N]=O JCXJVPUVTGWSNB-UHFFFAOYSA-N 0.000 claims 34
- -1 thiadiazqlyl Chemical group 0.000 claims 32
- 229910052801 chlorine Inorganic materials 0.000 claims 29
- 229910052731 fluorine Inorganic materials 0.000 claims 25
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims 25
- 229910052794 bromium Inorganic materials 0.000 claims 23
- 125000003118 aryl group Chemical group 0.000 claims 21
- 229910052799 carbon Inorganic materials 0.000 claims 21
- 125000000876 trifluoromethoxy group Chemical group FC(F)(F)O* 0.000 claims 20
- 125000002915 carbonyl group Chemical group [*:2]C([*:1])=O 0.000 claims 18
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 18
- 125000002837 carbocyclic group Chemical group 0.000 claims 17
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims 16
- 229910052710 silicon Inorganic materials 0.000 claims 16
- 125000001960 7 membered carbocyclic group Chemical group 0.000 claims 13
- 125000003545 alkoxy group Chemical group 0.000 claims 13
- 125000004429 atoms Chemical group 0.000 claims 12
- 150000001875 compounds Chemical class 0.000 claims 12
- 229910052739 hydrogen Inorganic materials 0.000 claims 12
- 125000001313 C5-C10 heteroaryl group Chemical group 0.000 claims 11
- 125000000304 alkynyl group Chemical group 0.000 claims 10
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims 9
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 claims 8
- 125000000753 cycloalkyl group Chemical group 0.000 claims 8
- 125000006340 pentafluoro ethyl group Chemical group FC(F)(F)C(F)(F)* 0.000 claims 8
- XUIMIQQOPSSXEZ-UHFFFAOYSA-N silicon Chemical group [Si] XUIMIQQOPSSXEZ-UHFFFAOYSA-N 0.000 claims 8
- 125000000335 thiazolyl group Chemical group 0.000 claims 8
- 125000006570 (C5-C6) heteroaryl group Chemical group 0.000 claims 7
- 125000004648 C2-C8 alkenyl group Chemical group 0.000 claims 7
- 125000001072 heteroaryl group Chemical group 0.000 claims 7
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 claims 6
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims 6
- 125000004209 (C1-C8) alkyl group Chemical group 0.000 claims 6
- 125000003342 alkenyl group Chemical group 0.000 claims 6
- 125000004414 alkyl thio group Chemical group 0.000 claims 6
- 125000004438 haloalkoxy group Chemical group 0.000 claims 6
- 125000001188 haloalkyl group Chemical group 0.000 claims 6
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 5
- 125000004076 pyridyl group Chemical group 0.000 claims 5
- 125000006656 (C2-C4) alkenyl group Chemical group 0.000 claims 4
- 125000006650 (C2-C4) alkynyl group Chemical group 0.000 claims 4
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims 4
- WSFSSNUMVMOOMR-UHFFFAOYSA-N formaldehyde Chemical compound O=C WSFSSNUMVMOOMR-UHFFFAOYSA-N 0.000 claims 4
- IJGRMHOSHXDMSA-UHFFFAOYSA-N nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims 4
- 125000001544 thienyl group Chemical group 0.000 claims 4
- 125000004649 C2-C8 alkynyl group Chemical group 0.000 claims 3
- 125000001164 benzothiazolyl group Chemical group S1C(=NC2=C1C=CC=C2)* 0.000 claims 3
- 125000001070 dihydroindolyl group Chemical group N1(CCC2=CC=CC=C12)* 0.000 claims 3
- 125000002541 furyl group Chemical group 0.000 claims 3
- 125000000842 isoxazolyl group Chemical group 0.000 claims 3
- 125000000714 pyrimidinyl group Chemical group 0.000 claims 3
- 150000003839 salts Chemical class 0.000 claims 3
- 239000011780 sodium chloride Substances 0.000 claims 3
- 239000012453 solvate Substances 0.000 claims 3
- 125000006272 (C3-C7) cycloalkyl group Chemical group 0.000 claims 2
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 claims 2
- 125000000051 benzyloxy group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])O* 0.000 claims 2
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims 2
- 125000002933 cyclohexyloxy group Chemical group C1(CCCCC1)O* 0.000 claims 2
- 125000001511 cyclopentyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims 2
- 125000001160 methoxycarbonyl group Chemical group [H]C([H])([H])OC(*)=O 0.000 claims 2
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 2
- 125000006217 methyl sulfide group Chemical group [H]C([H])([H])S* 0.000 claims 2
- 229910052757 nitrogen Inorganic materials 0.000 claims 2
- 125000000951 phenoxy group Chemical group [H]C1=C([H])C([H])=C(O*)C([H])=C1[H] 0.000 claims 2
- 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 2
- 125000000168 pyrrolyl group Chemical group 0.000 claims 2
- 125000004214 1-pyrrolidinyl group Chemical group [H]C1([H])N(*)C([H])([H])C([H])([H])C1([H])[H] 0.000 claims 1
- 125000000954 2-hydroxyethyl group Chemical group [H]C([*])([H])C([H])([H])O[H] 0.000 claims 1
- 125000000339 4-pyridyl group Chemical group N1=C([H])C([H])=C([*])C([H])=C1[H] 0.000 claims 1
- 229910004673 OPr Inorganic materials 0.000 claims 1
- 125000002490 anilino group Chemical group [H]N(*)C1=C([H])C([H])=C([H])C([H])=C1[H] 0.000 claims 1
- 125000003236 benzoyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C(*)=O 0.000 claims 1
- OKTJSMMVPCPJKN-UHFFFAOYSA-N carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims 1
- 125000002147 dimethylamino group Chemical group [H]C([H])([H])N(*)C([H])([H])[H] 0.000 claims 1
- 125000006222 dimethylaminomethyl group Chemical group [H]C([H])([H])N(C([H])([H])[H])C([H])([H])* 0.000 claims 1
- 125000000816 ethylene group Chemical group [H]C([H])([*:1])C([H])([H])[*:2] 0.000 claims 1
- 125000001041 indolyl group Chemical group 0.000 claims 1
- 125000001624 naphthyl group Chemical group 0.000 claims 1
- 125000001820 oxy group Chemical group [*:1]O[*:2] 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
- 125000004482 piperidin-4-yl group Chemical group N1CCC(CC1)* 0.000 claims 1
- 125000003386 piperidinyl group Chemical group 0.000 claims 1
- 125000001412 tetrahydropyranyl group Chemical group 0.000 claims 1
- 235000013877 carbamide Nutrition 0.000 abstract 1
- 201000010099 disease Diseases 0.000 abstract 1
- 230000000694 effects Effects 0.000 abstract 1
- 239000003112 inhibitor Substances 0.000 abstract 1
- 230000002401 inhibitory effect Effects 0.000 abstract 1
- 230000000051 modifying Effects 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
Abstract
L'invention concerne des urées qui renferment des hétérocycles à substitution N-aryle ou N-hétéroaryle et leurs analogues, qui sont des inhibiteurs sélectifs du récepteur humain P2Y1. L'invention concerne également diverses compositions pharmaceutiques renfermant ces urées, et des procédés de traitement de maladies réagissant à la modulation de l'activité du récepteur en question.
Priority Applications (12)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| AU2005245400A AU2005245400A1 (en) | 2004-05-12 | 2005-05-11 | Urea antagonists of P2Y1 receptor useful in the treatment of thrombotic conditions |
| DK05779448T DK1750704T3 (da) | 2004-05-12 | 2005-05-11 | Urinstof-antagonister af P2Y1-receptorer, der er anvendelige i behandlingen af trombotiske tilstande |
| CN2005800231306A CN1984655B (zh) | 2004-05-12 | 2005-05-11 | 可用于治疗血栓形成性疾病的p2y1受体脲拮抗剂 |
| JP2007513323A JP4795336B2 (ja) | 2004-05-12 | 2005-05-11 | 血栓症病態の治療に有用なｐ２ｙ１レセプターのウレアアンタゴニスト |
| MXPA06013024A MXPA06013024A (es) | 2004-05-12 | 2005-05-11 | Antagonistas de urea del receptor p2y1 util en el tratamiento de condiciones tromboticas. |
| CNA2005800236206A CN1984892A (zh) | 2004-05-12 | 2005-05-11 | 用于治疗血栓性疾病的p2y1受体的脲拮抗剂 |
| DE602005015577T DE602005015577D1 (de) | 2004-05-12 | 2005-05-11 | Harnstoff-antagonisten des p2y1-rezeptors zur behandlung von thromboseleiden |
| PL05779448T PL1750704T3 (pl) | 2004-05-12 | 2005-05-11 | Pochodne mocznika jako antagoniści receptora P2Y1 użyteczne w leczeniu stanów zakrzepowych |
| EP05779448A EP1750704B1 (fr) | 2004-05-12 | 2005-05-11 | Urees antagonistes vis-a-vis du recepteur p2y1 utiles dans le traitement des etats thrombotiques |
| NO20065544A NO20065544L (no) | 2004-05-12 | 2006-12-01 | Urea-antagonister av P2Y1-reseptor anvendbare i behandling av trombotiske tilstander. |
| HR20090468T HRP20090468T1 (hr) | 2004-05-12 | 2009-09-03 | Urea antagonisti p2y1 receptora korisni u liječenju trombotičkih stanja |
| CY20091101048T CY1109487T1 (el) | 2004-05-12 | 2009-10-13 | Ανταγωνιστες τυπου ουριας του υποδοχεα p2y1 χρησιμοι στην αγωγη θρομβωτικων καταστασεων |
Applications Claiming Priority (6)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US57028804P | 2004-05-12 | 2004-05-12 | |
| US60/570,288 | 2004-05-12 | ||
| US66573505P | 2005-03-28 | 2005-03-28 | |
| US60/665,735 | 2005-03-28 | ||
| US11/126,567 | 2005-05-10 | ||
| US11/126,567 US7550499B2 (en) | 2004-05-12 | 2005-05-10 | Urea antagonists of P2Y1 receptor useful in the treatment of thrombotic conditions |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| WO2005113537A2 WO2005113537A2 (fr) | 2005-12-01 |
| WO2005113537A3 WO2005113537A3 (fr) | 2005-12-22 |
| WO2005113537B1 true WO2005113537B1 (fr) | 2006-02-16 |
Family
ID=35169638
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PCT/US2005/016525 WO2005113537A2 (fr) | 2004-05-12 | 2005-05-11 | Urees antagonistes vis-a-vis du recepteur p2y1 utiles dans le traitement des etats thrombotiques |
Country Status (17)
| Country | Link |
|---|---|
| US (1) | US7550499B2 (fr) |
| EP (1) | EP1750704B1 (fr) |
| JP (1) | JP4795336B2 (fr) |
| KR (1) | KR20070011479A (fr) |
| CN (2) | CN1984655B (fr) |
| AU (1) | AU2005245400A1 (fr) |
| CY (1) | CY1109487T1 (fr) |
| DE (1) | DE602005015577D1 (fr) |
| DK (1) | DK1750704T3 (fr) |
| ES (1) | ES2328716T3 (fr) |
| HR (1) | HRP20090468T1 (fr) |
| MX (1) | MXPA06013024A (fr) |
| NO (1) | NO20065544L (fr) |
| PL (1) | PL1750704T3 (fr) |
| PT (1) | PT1750704E (fr) |
| SI (1) | SI1750704T1 (fr) |
| WO (1) | WO2005113537A2 (fr) |
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| DE602006017694D1 (de) * | 2005-06-27 | 2010-12-02 | Bristol Myers Squibb Co | C-verknüpfte zyklische antagonisten des p2y1-rezeptors mit eignung bei der behandlung thrombotischer leiden |
| DE602006020871D1 (de) * | 2005-06-27 | 2011-05-05 | Bristol Myers Squibb Co | Lineare harnstoffmimetika-antagonisten des p2y1-rezeptors zur behandlung von thromboseleiden |
| WO2007002634A1 (fr) * | 2005-06-27 | 2007-01-04 | Bristol-Myers Squibb Company | Antagonistes carbocycliques et heherocycliques du recepteur p2y1, utiles pour traiter des etats pathologiques thrombotiques |
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-
2005
- 2005-05-10 US US11/126,567 patent/US7550499B2/en active Active
- 2005-05-11 PT PT05779448T patent/PT1750704E/pt unknown
- 2005-05-11 MX MXPA06013024A patent/MXPA06013024A/es active IP Right Grant
- 2005-05-11 DE DE602005015577T patent/DE602005015577D1/de active Active
- 2005-05-11 AU AU2005245400A patent/AU2005245400A1/en not_active Abandoned
- 2005-05-11 CN CN2005800231306A patent/CN1984655B/zh not_active Expired - Fee Related
- 2005-05-11 KR KR1020067023615A patent/KR20070011479A/ko not_active Application Discontinuation
- 2005-05-11 PL PL05779448T patent/PL1750704T3/pl unknown
- 2005-05-11 JP JP2007513323A patent/JP4795336B2/ja not_active Expired - Fee Related
- 2005-05-11 WO PCT/US2005/016525 patent/WO2005113537A2/fr active Application Filing
- 2005-05-11 SI SI200530770T patent/SI1750704T1/sl unknown
- 2005-05-11 ES ES05779448T patent/ES2328716T3/es active Active
- 2005-05-11 EP EP05779448A patent/EP1750704B1/fr active Active
- 2005-05-11 CN CNA2005800236206A patent/CN1984892A/zh active Pending
- 2005-05-11 DK DK05779448T patent/DK1750704T3/da active
-
2006
- 2006-12-01 NO NO20065544A patent/NO20065544L/no not_active Application Discontinuation
-
2009
- 2009-09-03 HR HR20090468T patent/HRP20090468T1/hr unknown
- 2009-10-13 CY CY20091101048T patent/CY1109487T1/el unknown
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