JP2013518888A5 - - Google Patents
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- JP2013518888A5 JP2013518888A5 JP2012552055A JP2012552055A JP2013518888A5 JP 2013518888 A5 JP2013518888 A5 JP 2013518888A5 JP 2012552055 A JP2012552055 A JP 2012552055A JP 2012552055 A JP2012552055 A JP 2012552055A JP 2013518888 A5 JP2013518888 A5 JP 2013518888A5
- Authority
- JP
- Japan
- Prior art keywords
- aryl
- heterocyclyl
- heteroaryl
- carbocyclyl
- alkyl
- 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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- 125000000623 heterocyclic group Chemical group 0.000 claims description 90
- 125000003118 aryl group Chemical group 0.000 claims description 88
- 125000004452 carbocyclyl group Chemical group 0.000 claims description 87
- 150000001875 compounds Chemical class 0.000 claims description 74
- 125000001072 heteroaryl group Chemical group 0.000 claims description 68
- 125000000217 alkyl group Chemical group 0.000 claims description 63
- 125000001424 substituent group Chemical group 0.000 claims description 46
- 125000003710 aryl alkyl group Chemical group 0.000 claims description 41
- 229910052739 hydrogen Inorganic materials 0.000 claims description 30
- 239000001257 hydrogen Substances 0.000 claims description 30
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 claims description 28
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims description 25
- 125000004093 cyano group Chemical group *C#N 0.000 claims description 22
- 125000005549 heteroarylene group Chemical group 0.000 claims description 22
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims description 20
- 125000000732 arylene group Chemical group 0.000 claims description 20
- 238000000034 method Methods 0.000 claims description 19
- 125000005843 halogen group Chemical group 0.000 claims description 18
- 125000004433 nitrogen atom Chemical group N* 0.000 claims description 16
- -1 3-hydroxyisoxazolyl Chemical group 0.000 claims description 13
- 125000004429 atom Chemical group 0.000 claims description 12
- 125000004432 carbon atom Chemical group C* 0.000 claims description 12
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims description 12
- 229910052799 carbon Inorganic materials 0.000 claims description 11
- 150000001540 azides Chemical class 0.000 claims description 10
- 150000002431 hydrogen Chemical class 0.000 claims description 10
- 125000006590 (C2-C6) alkenylene group Chemical group 0.000 claims description 8
- 125000006591 (C2-C6) alkynylene group Chemical group 0.000 claims description 8
- 125000003342 alkenyl group Chemical group 0.000 claims description 8
- 125000004450 alkenylene group Chemical group 0.000 claims description 7
- 125000004419 alkynylene group Chemical group 0.000 claims description 7
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 6
- 125000003831 tetrazolyl group Chemical group 0.000 claims description 6
- 125000000304 alkynyl group Chemical group 0.000 claims description 5
- 201000010099 disease Diseases 0.000 claims description 5
- 125000003107 substituted aryl group Chemical group 0.000 claims description 5
- 102000051325 Glucagon Human genes 0.000 claims description 4
- 108060003199 Glucagon Proteins 0.000 claims description 4
- NQRYJNQNLNOLGT-UHFFFAOYSA-N Piperidine Chemical group C1CCNCC1 NQRYJNQNLNOLGT-UHFFFAOYSA-N 0.000 claims description 4
- JUJWROOIHBZHMG-UHFFFAOYSA-N Pyridine Chemical group C1=CC=NC=C1 JUJWROOIHBZHMG-UHFFFAOYSA-N 0.000 claims description 4
- MASNOZXLGMXCHN-ZLPAWPGGSA-N glucagon Chemical compound C([C@@H](C(=O)N[C@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC=1C2=CC=CC=C2NC=1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H]([C@@H](C)O)C(O)=O)C(C)C)NC(=O)[C@H](CC(O)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(N)=N)NC(=O)[C@H](CCCNC(N)=N)NC(=O)[C@H](CO)NC(=O)[C@H](CC(O)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC=1C=CC(O)=CC=1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](CC=1C=CC(O)=CC=1)NC(=O)[C@H](CC(O)=O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](CC=1C=CC=CC=1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)[C@@H](N)CC=1NC=NC=1)[C@@H](C)O)[C@@H](C)O)C1=CC=CC=C1 MASNOZXLGMXCHN-ZLPAWPGGSA-N 0.000 claims description 4
- 229960004666 glucagon Drugs 0.000 claims description 4
- DTHNMHAUYICORS-KTKZVXAJSA-N Glucagon-like peptide 1 Chemical compound C([C@@H](C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](C)C(=O)N[C@@H](CC=1C2=CC=CC=C2NC=1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](CCCNC(N)=N)C(N)=O)NC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@H](CCC(N)=O)NC(=O)CNC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC=1C=CC(O)=CC=1)NC(=O)[C@H](CO)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](CC(O)=O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](CC=1C=CC=CC=1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](C)NC(=O)[C@@H](N)CC=1N=CNC=1)[C@@H](C)O)[C@@H](C)O)C(C)C)C1=CC=CC=C1 DTHNMHAUYICORS-KTKZVXAJSA-N 0.000 claims description 3
- 101800000224 Glucagon-like peptide 1 Proteins 0.000 claims description 3
- 102100040918 Pro-glucagon Human genes 0.000 claims description 3
- 230000000694 effects Effects 0.000 claims description 3
- 239000008194 pharmaceutical composition Substances 0.000 claims description 3
- 208000024891 symptom Diseases 0.000 claims description 3
- 208000024172 Cardiovascular disease Diseases 0.000 claims description 2
- 102000007446 Glucagon-Like Peptide-1 Receptor Human genes 0.000 claims description 2
- 108010086246 Glucagon-Like Peptide-1 Receptor Proteins 0.000 claims description 2
- 208000031226 Hyperlipidaemia Diseases 0.000 claims description 2
- 208000008589 Obesity Diseases 0.000 claims description 2
- CZPWVGJYEJSRLH-UHFFFAOYSA-N Pyrimidine Chemical group C1=CN=CN=C1 CZPWVGJYEJSRLH-UHFFFAOYSA-N 0.000 claims description 2
- 230000036528 appetite Effects 0.000 claims description 2
- 235000019789 appetite Nutrition 0.000 claims description 2
- 125000000051 benzyloxy group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])O* 0.000 claims description 2
- 150000007942 carboxylates Chemical class 0.000 claims description 2
- 206010012601 diabetes mellitus Diseases 0.000 claims description 2
- 235000005911 diet Nutrition 0.000 claims description 2
- 230000000378 dietary effect Effects 0.000 claims description 2
- 239000003937 drug carrier Substances 0.000 claims description 2
- 230000037406 food intake Effects 0.000 claims description 2
- 235000012631 food intake Nutrition 0.000 claims description 2
- 230000030136 gastric emptying Effects 0.000 claims description 2
- 230000030135 gastric motility Effects 0.000 claims description 2
- 125000004446 heteroarylalkyl group Chemical group 0.000 claims description 2
- 230000003914 insulin secretion Effects 0.000 claims description 2
- 125000002346 iodo group Chemical group I* 0.000 claims description 2
- 208000030159 metabolic disease Diseases 0.000 claims description 2
- 235000020824 obesity Nutrition 0.000 claims description 2
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 2
- 239000000651 prodrug Substances 0.000 claims description 2
- 229940002612 prodrug Drugs 0.000 claims description 2
- UMJSCPRVCHMLSP-UHFFFAOYSA-N pyridine Chemical group COC1=CC=CN=C1 UMJSCPRVCHMLSP-UHFFFAOYSA-N 0.000 claims description 2
- 102000005962 receptors Human genes 0.000 claims description 2
- 108020003175 receptors Proteins 0.000 claims description 2
- 150000003839 salts Chemical class 0.000 claims description 2
- 229920006395 saturated elastomer Polymers 0.000 claims description 2
- 230000028327 secretion Effects 0.000 claims description 2
- 239000012453 solvate Substances 0.000 claims description 2
- 238000006467 substitution reaction Methods 0.000 claims description 2
- 230000001235 sensitizing effect Effects 0.000 description 3
- 230000001270 agonistic effect Effects 0.000 description 2
- 239000003814 drug Substances 0.000 description 2
- 229940124597 therapeutic agent Drugs 0.000 description 2
- 239000000556 agonist Substances 0.000 description 1
- 230000002401 inhibitory effect Effects 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNPCT/CN2010/000141 | 2010-02-02 | ||
| PCT/CN2010/000141 WO2011094890A1 (en) | 2010-02-02 | 2010-02-02 | Phenylalanine derivatives and their use as non-peptide glp-1 receptor modulators |
| PCT/US2011/023482 WO2011097300A1 (en) | 2010-02-02 | 2011-02-02 | Phenylalanine derivatives and their use as non-peptide glp-1 receptor modulators |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2016035147A Division JP2016166182A (ja) | 2010-02-02 | 2016-02-26 | 非ペプチドｇｌｐ−１受容体調節因子としてのフェニルアラニン誘導体およびその使用 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2013518888A JP2013518888A (ja) | 2013-05-23 |
| JP2013518888A5 true JP2013518888A5 (https=) | 2014-02-27 |
Family
ID=44354851
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2012552055A Pending JP2013518888A (ja) | 2010-02-02 | 2011-02-02 | 非ペプチドｇｌｐ−１受容体調節因子としてのフェニルアラニン誘導体およびその使用 |
| JP2016035147A Pending JP2016166182A (ja) | 2010-02-02 | 2016-02-26 | 非ペプチドｇｌｐ−１受容体調節因子としてのフェニルアラニン誘導体およびその使用 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2016035147A Pending JP2016166182A (ja) | 2010-02-02 | 2016-02-26 | 非ペプチドｇｌｐ−１受容体調節因子としてのフェニルアラニン誘導体およびその使用 |
Country Status (6)
| Country | Link |
|---|---|
| US (1) | US8748412B2 (https=) |
| EP (1) | EP2531198A4 (https=) |
| JP (2) | JP2013518888A (https=) |
| AR (1) | AR080112A1 (https=) |
| CA (1) | CA2788782A1 (https=) |
| WO (2) | WO2011094890A1 (https=) |
Families Citing this family (100)
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| MX353408B (es) | 2010-04-22 | 2018-01-11 | Vertex Pharma | Proceso para producir compuestos de cicloalquilcarboxamido-indol. |
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2011
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- 2011-02-02 US US13/019,851 patent/US8748412B2/en active Active
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2016
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