JP2008524186A5 - - Google Patents
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- Publication number
- JP2008524186A5 JP2008524186A5 JP2007546178A JP2007546178A JP2008524186A5 JP 2008524186 A5 JP2008524186 A5 JP 2008524186A5 JP 2007546178 A JP2007546178 A JP 2007546178A JP 2007546178 A JP2007546178 A JP 2007546178A JP 2008524186 A5 JP2008524186 A5 JP 2008524186A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- pharmaceutically acceptable
- solvate
- acceptable salt
- group
- Prior art date
- Legal status (The legal status 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 status listed.)
- Pending
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- 150000001875 compounds Chemical class 0.000 claims 20
- 150000003839 salts Chemical class 0.000 claims 18
- 239000012453 solvate Substances 0.000 claims 17
- 125000000217 alkyl group Chemical group 0.000 claims 16
- 125000001424 substituent group Chemical group 0.000 claims 14
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 9
- 125000005843 halogen group Chemical group 0.000 claims 8
- 239000003814 drug Substances 0.000 claims 7
- 239000008194 pharmaceutical composition Substances 0.000 claims 6
- 229910052717 sulfur Inorganic materials 0.000 claims 6
- NINIDFKCEFEMDL-UHFFFAOYSA-N Sulfur Chemical compound [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 claims 5
- -1 hydroxy, amino Chemical group 0.000 claims 5
- 239000011593 sulfur Substances 0.000 claims 5
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims 5
- 208000006545 Chronic Obstructive Pulmonary Disease Diseases 0.000 claims 4
- 208000022559 Inflammatory bowel disease Diseases 0.000 claims 4
- 206010028980 Neoplasm Diseases 0.000 claims 4
- 208000001132 Osteoporosis Diseases 0.000 claims 4
- 201000004681 Psoriasis Diseases 0.000 claims 4
- 206010039085 Rhinitis allergic Diseases 0.000 claims 4
- 201000010105 allergic rhinitis Diseases 0.000 claims 4
- 208000006673 asthma Diseases 0.000 claims 4
- 201000011510 cancer Diseases 0.000 claims 4
- 125000001153 fluoro group Chemical group F* 0.000 claims 4
- 125000001072 heteroaryl group Chemical group 0.000 claims 4
- 239000001257 hydrogen Substances 0.000 claims 4
- 229910052739 hydrogen Inorganic materials 0.000 claims 4
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 4
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 4
- 201000008482 osteoarthritis Diseases 0.000 claims 4
- 229910052760 oxygen Inorganic materials 0.000 claims 4
- 206010039073 rheumatoid arthritis Diseases 0.000 claims 4
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 3
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical compound [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims 3
- 238000002648 combination therapy Methods 0.000 claims 3
- 125000004093 cyano group Chemical group *C#N 0.000 claims 3
- 208000002551 irritable bowel syndrome Diseases 0.000 claims 3
- 238000004519 manufacturing process Methods 0.000 claims 3
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 3
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims 3
- 239000001301 oxygen Substances 0.000 claims 3
- BDERNNFJNOPAEC-UHFFFAOYSA-N propan-1-ol Chemical compound CCCO BDERNNFJNOPAEC-UHFFFAOYSA-N 0.000 claims 3
- 150000003457 sulfones Chemical class 0.000 claims 3
- 150000003462 sulfoxides Chemical class 0.000 claims 3
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims 2
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 claims 2
- 125000003118 aryl group Chemical group 0.000 claims 2
- 125000004429 atom Chemical group 0.000 claims 2
- 125000000484 butyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])C([H])([H])[H] 0.000 claims 2
- 125000004452 carbocyclyl group Chemical group 0.000 claims 2
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 2
- 125000004051 hexyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])* 0.000 claims 2
- 238000000034 method Methods 0.000 claims 2
- 229910052757 nitrogen Inorganic materials 0.000 claims 2
- 125000001147 pentyl group Chemical group C(CCCC)* 0.000 claims 2
- 125000001436 propyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])[H] 0.000 claims 2
- 125000006239 protecting group Chemical group 0.000 claims 2
- 239000002904 solvent Substances 0.000 claims 2
- 125000000446 sulfanediyl group Chemical group *S* 0.000 claims 2
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 claims 1
- 125000004890 (C1-C6) alkylamino group Chemical group 0.000 claims 1
- 125000006619 (C1-C6) dialkylamino group Chemical group 0.000 claims 1
- 125000004209 (C1-C8) alkyl group Chemical group 0.000 claims 1
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims 1
- NJGRTZWZTNBVSV-UHFFFAOYSA-N 3-[[2-amino-5-[(2-fluorophenyl)methylsulfanyl]-[1,3]thiazolo[4,5-d]pyrimidin-7-yl]oxy]propanamide Chemical compound N=1C=2N=C(N)SC=2C(OCCC(=O)N)=NC=1SCC1=CC=CC=C1F NJGRTZWZTNBVSV-UHFFFAOYSA-N 0.000 claims 1
- RNNJGDUVKJUAAZ-UHFFFAOYSA-N 3-[[2-amino-5-[(2-fluorophenyl)methylsulfanyl]-[1,3]thiazolo[4,5-d]pyrimidin-7-yl]oxy]propanoic acid Chemical compound N=1C(OCCC(O)=O)=C2SC(N)=NC2=NC=1SCC1=CC=CC=C1F RNNJGDUVKJUAAZ-UHFFFAOYSA-N 0.000 claims 1
- ZCYVEMRRCGMTRW-UHFFFAOYSA-N 7553-56-2 Chemical compound [I] ZCYVEMRRCGMTRW-UHFFFAOYSA-N 0.000 claims 1
- WKBOTKDWSSQWDR-UHFFFAOYSA-N Bromine atom Chemical compound [Br] WKBOTKDWSSQWDR-UHFFFAOYSA-N 0.000 claims 1
- 102000009410 Chemokine receptor Human genes 0.000 claims 1
- 108050000299 Chemokine receptor Proteins 0.000 claims 1
- ZAMOUSCENKQFHK-UHFFFAOYSA-N Chlorine atom Chemical compound [Cl] ZAMOUSCENKQFHK-UHFFFAOYSA-N 0.000 claims 1
- PXGOKWXKJXAPGV-UHFFFAOYSA-N Fluorine Chemical compound FF PXGOKWXKJXAPGV-UHFFFAOYSA-N 0.000 claims 1
- 238000006751 Mitsunobu reaction Methods 0.000 claims 1
- 125000003545 alkoxy group Chemical group 0.000 claims 1
- 125000005115 alkyl carbamoyl group Chemical group 0.000 claims 1
- 150000001350 alkyl halides Chemical class 0.000 claims 1
- 150000001540 azides Chemical class 0.000 claims 1
- HNYOPLTXPVRDBG-UHFFFAOYSA-N barbituric acid Chemical compound O=C1CC(=O)NC(=O)N1 HNYOPLTXPVRDBG-UHFFFAOYSA-N 0.000 claims 1
- 230000009286 beneficial effect Effects 0.000 claims 1
- GDTBXPJZTBHREO-UHFFFAOYSA-N bromine Substances BrBr GDTBXPJZTBHREO-UHFFFAOYSA-N 0.000 claims 1
- 229910052794 bromium Inorganic materials 0.000 claims 1
- 125000003917 carbamoyl group Chemical group [H]N([H])C(*)=O 0.000 claims 1
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims 1
- 239000003795 chemical substances by application Substances 0.000 claims 1
- 229910052801 chlorine Inorganic materials 0.000 claims 1
- 239000000460 chlorine Substances 0.000 claims 1
- 239000003085 diluting agent Substances 0.000 claims 1
- 201000010099 disease Diseases 0.000 claims 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 1
- 229940079593 drug Drugs 0.000 claims 1
- 230000000694 effects Effects 0.000 claims 1
- 229910052731 fluorine Inorganic materials 0.000 claims 1
- 239000011737 fluorine Substances 0.000 claims 1
- 238000009472 formulation Methods 0.000 claims 1
- 125000000623 heterocyclic group Chemical group 0.000 claims 1
- 239000011630 iodine Substances 0.000 claims 1
- 229910052740 iodine Inorganic materials 0.000 claims 1
- 125000002757 morpholinyl group Chemical group 0.000 claims 1
- IWTFJSAERVORPI-UHFFFAOYSA-N n-[2-[[2-amino-5-[(2-fluorophenyl)methylsulfanyl]-[1,3]thiazolo[4,5-d]pyrimidin-7-yl]oxy]ethyl]acetamide Chemical compound N=1C=2N=C(N)SC=2C(OCCNC(=O)C)=NC=1SCC1=CC=CC=C1F IWTFJSAERVORPI-UHFFFAOYSA-N 0.000 claims 1
- 150000002825 nitriles Chemical class 0.000 claims 1
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 1
- 230000000269 nucleophilic effect Effects 0.000 claims 1
- 239000007800 oxidant agent Substances 0.000 claims 1
- 230000001590 oxidative effect Effects 0.000 claims 1
- 229910000073 phosphorus hydride Inorganic materials 0.000 claims 1
- 125000004482 piperidin-4-yl group Chemical group N1CCC(CC1)* 0.000 claims 1
- 125000003718 tetrahydrofuranyl group Chemical group 0.000 claims 1
- 238000002560 therapeutic procedure Methods 0.000 claims 1
- 0 **c1nc(**)nc2c1[s]c(*)n2 Chemical compound **c1nc(**)nc2c1[s]c(*)n2 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| GB0427698A GB0427698D0 (en) | 2004-12-17 | 2004-12-17 | Compounds |
| GB0502542A GB0502542D0 (en) | 2005-02-08 | 2005-02-08 | Method |
| PCT/GB2005/004825 WO2006064228A2 (en) | 2004-12-17 | 2005-12-14 | Thiazolopyramidine compounds for the modulation of chemokine receptor activity |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2008524186A JP2008524186A (ja) | 2008-07-10 |
| JP2008524186A5 true JP2008524186A5 (enExample) | 2009-01-29 |
Family
ID=36062251
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2007546178A Pending JP2008524186A (ja) | 2004-12-17 | 2005-12-14 | ケモカイン受容体活性の調節のためのチアゾロピラミジン化合物 |
Country Status (4)
| Country | Link |
|---|---|
| US (1) | US20090239882A1 (enExample) |
| EP (1) | EP1844054A2 (enExample) |
| JP (1) | JP2008524186A (enExample) |
| WO (1) | WO2006064228A2 (enExample) |
Families Citing this family (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| SE9903544D0 (sv) | 1999-10-01 | 1999-10-01 | Astra Pharma Prod | Novel compounds |
| GB2359551A (en) | 2000-02-23 | 2001-08-29 | Astrazeneca Uk Ltd | Pharmaceutically active pyrimidine derivatives |
| GB0221828D0 (en) | 2002-09-20 | 2002-10-30 | Astrazeneca Ab | Novel compound |
| GB0328243D0 (en) | 2003-12-05 | 2004-01-07 | Astrazeneca Ab | Methods |
| UA90707C2 (en) * | 2005-04-06 | 2010-05-25 | Астразенека Аб | Novel 5-substituted 7-amino-[1,3]thiazolo[4,5-d]pyrimidine derivatives |
| TW200820973A (en) | 2006-09-29 | 2008-05-16 | Astrazeneca Ab | Novel compounds 480 |
| EP2069365A4 (en) * | 2006-09-29 | 2011-11-02 | Astrazeneca Ab | NOVEL [1, 3] THIAZOLO [4,5-D] PYRIMIDIN-2 (3H) -AMINE 5,7-DISUBSTITUTED DERIVATIVES AND THEIR USE IN THERAPY |
| RU2554947C2 (ru) * | 2009-11-30 | 2015-07-10 | Цзянсу Хансох Фармасьютикал Груп Ко., Лтд. | Соли азилсартана с органическими аминами, способ их получения и применение |
Family Cites Families (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| SE9802729D0 (sv) * | 1998-08-13 | 1998-08-13 | Astra Pharma Prod | Novel Compounds |
| SE9903544D0 (sv) * | 1999-10-01 | 1999-10-01 | Astra Pharma Prod | Novel compounds |
| DE60101372T2 (de) * | 2000-02-11 | 2004-10-14 | Astrazeneca Ab | Pyrimidinverbindungen und ihre verwendung als modulatoren der chemokin-rezeptor-aktivität |
| JP2007507494A (ja) * | 2003-10-07 | 2007-03-29 | アストラゼネカ・アクチエボラーグ | ケモカイン受容体アンタゴニストとりわけＣＸ３ＣＲ１として有用な新規な２−置換４−アミノ−チアゾロ［４，５−ｄ］ピリミジン |
| WO2005082865A1 (ja) * | 2004-02-27 | 2005-09-09 | Astellas Pharma Inc. | 縮合二環性ピリミジン誘導体 |
-
2005
- 2005-12-14 WO PCT/GB2005/004825 patent/WO2006064228A2/en not_active Ceased
- 2005-12-14 EP EP05818307A patent/EP1844054A2/en not_active Withdrawn
- 2005-12-14 US US11/721,583 patent/US20090239882A1/en not_active Abandoned
- 2005-12-14 JP JP2007546178A patent/JP2008524186A/ja active Pending
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