BRPI0720675A2 - Agonistas de receptor heterocíclico para o tratamento da diabetes e de distúrbios metabólicos - Google Patents
Agonistas de receptor heterocíclico para o tratamento da diabetes e de distúrbios metabólicos Download PDFInfo
- Publication number
- BRPI0720675A2 BRPI0720675A2 BRPI0720675-5A BRPI0720675A BRPI0720675A2 BR PI0720675 A2 BRPI0720675 A2 BR PI0720675A2 BR PI0720675 A BRPI0720675 A BR PI0720675A BR PI0720675 A2 BRPI0720675 A2 BR PI0720675A2
- Authority
- BR
- Brazil
- Prior art keywords
- substituted
- group
- alkyl
- aryl
- heteroaryl
- Prior art date
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- 125000000623 heterocyclic group Chemical group 0.000 title claims description 174
- 238000011282 treatment Methods 0.000 title claims description 32
- 206010012601 diabetes mellitus Diseases 0.000 title description 55
- 229940044601 receptor agonist Drugs 0.000 title description 3
- 239000000018 receptor agonist Substances 0.000 title description 3
- 208000030159 metabolic disease Diseases 0.000 title description 2
- 150000001875 compounds Chemical class 0.000 claims description 229
- -1 furanoyl Chemical group 0.000 claims description 181
- 125000001072 heteroaryl group Chemical group 0.000 claims description 166
- 125000003118 aryl group Chemical group 0.000 claims description 139
- 125000000217 alkyl group Chemical group 0.000 claims description 111
- NOESYZHRGYRDHS-UHFFFAOYSA-N insulin Chemical compound N1C(=O)C(NC(=O)C(CCC(N)=O)NC(=O)C(CCC(O)=O)NC(=O)C(C(C)C)NC(=O)C(NC(=O)CN)C(C)CC)CSSCC(C(NC(CO)C(=O)NC(CC(C)C)C(=O)NC(CC=2C=CC(O)=CC=2)C(=O)NC(CCC(N)=O)C(=O)NC(CC(C)C)C(=O)NC(CCC(O)=O)C(=O)NC(CC(N)=O)C(=O)NC(CC=2C=CC(O)=CC=2)C(=O)NC(CSSCC(NC(=O)C(C(C)C)NC(=O)C(CC(C)C)NC(=O)C(CC=2C=CC(O)=CC=2)NC(=O)C(CC(C)C)NC(=O)C(C)NC(=O)C(CCC(O)=O)NC(=O)C(C(C)C)NC(=O)C(CC(C)C)NC(=O)C(CC=2NC=NC=2)NC(=O)C(CO)NC(=O)CNC2=O)C(=O)NCC(=O)NC(CCC(O)=O)C(=O)NC(CCCNC(N)=N)C(=O)NCC(=O)NC(CC=3C=CC=CC=3)C(=O)NC(CC=3C=CC=CC=3)C(=O)NC(CC=3C=CC(O)=CC=3)C(=O)NC(C(C)O)C(=O)N3C(CCC3)C(=O)NC(CCCCN)C(=O)NC(C)C(O)=O)C(=O)NC(CC(N)=O)C(O)=O)=O)NC(=O)C(C(C)CC)NC(=O)C(CO)NC(=O)C(C(C)O)NC(=O)C1CSSCC2NC(=O)C(CC(C)C)NC(=O)C(NC(=O)C(CCC(N)=O)NC(=O)C(CC(N)=O)NC(=O)C(NC(=O)C(N)CC=1C=CC=CC=1)C(C)C)CC1=CN=CN1 NOESYZHRGYRDHS-UHFFFAOYSA-N 0.000 claims description 94
- 125000003107 substituted aryl group Chemical group 0.000 claims description 65
- 125000000304 alkynyl group Chemical group 0.000 claims description 63
- 125000000753 cycloalkyl group Chemical group 0.000 claims description 62
- WQZGKKKJIJFFOK-GASJEMHNSA-N Glucose Natural products OC[C@H]1OC(O)[C@H](O)[C@@H](O)[C@@H]1O WQZGKKKJIJFFOK-GASJEMHNSA-N 0.000 claims description 59
- 239000008103 glucose Substances 0.000 claims description 59
- 238000000034 method Methods 0.000 claims description 58
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- 210000000227 basophil cell of anterior lobe of hypophysis Anatomy 0.000 claims description 42
- 125000001188 haloalkyl group Chemical group 0.000 claims description 41
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- 229910052757 nitrogen Inorganic materials 0.000 claims description 34
- 125000004076 pyridyl group Chemical group 0.000 claims description 33
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 32
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- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims description 16
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- 125000001313 C5-C10 heteroaryl group Chemical group 0.000 claims description 15
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- 206010067584 Type 1 diabetes mellitus Diseases 0.000 claims description 13
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- 239000008194 pharmaceutical composition Substances 0.000 claims description 12
- 229910052705 radium Inorganic materials 0.000 claims description 12
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- 201000000690 abdominal obesity-metabolic syndrome Diseases 0.000 claims description 9
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- 125000006570 (C5-C6) heteroaryl group Chemical group 0.000 claims description 8
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- 125000006163 5-membered heteroaryl group Chemical group 0.000 claims description 5
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- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims description 5
- 125000006376 (C3-C10) cycloalkyl group Chemical group 0.000 claims description 4
- ZAMOUSCENKQFHK-UHFFFAOYSA-N Chlorine atom Chemical compound [Cl] ZAMOUSCENKQFHK-UHFFFAOYSA-N 0.000 claims description 4
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- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims description 3
- 101150073096 NRAS gene Proteins 0.000 claims description 2
- ZCQWOFVYLHDMMC-UHFFFAOYSA-N Oxazole Chemical compound C1=COC=N1 ZCQWOFVYLHDMMC-UHFFFAOYSA-N 0.000 claims description 2
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- MPVDXIMFBOLMNW-UHFFFAOYSA-N chembl1615565 Chemical compound OC1=CC=C2C=C(S(O)(=O)=O)C=C(S(O)(=O)=O)C2=C1N=NC1=CC=CC=C1 MPVDXIMFBOLMNW-UHFFFAOYSA-N 0.000 claims description 2
- 125000001786 isothiazolyl group Chemical group 0.000 claims description 2
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- 125000003226 pyrazolyl group Chemical group 0.000 claims description 2
- 125000000168 pyrrolyl group Chemical group 0.000 claims description 2
- VLLMWSRANPNYQX-UHFFFAOYSA-N thiadiazole Chemical compound C1=CSN=N1.C1=CSN=N1 VLLMWSRANPNYQX-UHFFFAOYSA-N 0.000 claims description 2
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Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
- C07D417/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
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Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US87790306P | 2006-12-28 | 2006-12-28 | |
| US60/877,903 | 2006-12-28 | ||
| US11/964,461 US7638541B2 (en) | 2006-12-28 | 2007-12-26 | 5-ethyl-2-{4-[4-(4-tetrazol-1-yl-phenoxymethyl)-thiazol-2-yl]-piperidin-1-yl}-pyrimidine |
| US11/964.461 | 2007-12-26 | ||
| PCT/US2007/088978 WO2008083238A2 (en) | 2006-12-28 | 2007-12-27 | Heterocyclic receptor agonists for the treatment of diabetes and metabolic disorders |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| BRPI0720675A2 true BRPI0720675A2 (pt) | 2014-02-04 |
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| BRPI0720675-5A BRPI0720675A2 (pt) | 2006-12-28 | 2007-12-27 | Agonistas de receptor heterocíclico para o tratamento da diabetes e de distúrbios metabólicos |
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| EP (1) | EP2111107B1 (enExample) |
| JP (1) | JP5455645B2 (enExample) |
| KR (1) | KR101539308B1 (enExample) |
| AU (1) | AU2007339772B9 (enExample) |
| BR (1) | BRPI0720675A2 (enExample) |
| CA (1) | CA2672725C (enExample) |
| EA (1) | EA016720B1 (enExample) |
| ES (1) | ES2405105T3 (enExample) |
| IL (1) | IL199397A (enExample) |
| MX (1) | MX2009007023A (enExample) |
| NZ (1) | NZ577996A (enExample) |
| WO (1) | WO2008083238A2 (enExample) |
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