JP2012503661A5 - - Google Patents
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- Publication number
- JP2012503661A5 JP2012503661A5 JP2011529149A JP2011529149A JP2012503661A5 JP 2012503661 A5 JP2012503661 A5 JP 2012503661A5 JP 2011529149 A JP2011529149 A JP 2011529149A JP 2011529149 A JP2011529149 A JP 2011529149A JP 2012503661 A5 JP2012503661 A5 JP 2012503661A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- heteroaryl
- substituted
- cycloalkyl
- aryl
- 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.)
- Granted
Links
- 125000000217 alkyl group Chemical group 0.000 claims 139
- 229910052736 halogen Inorganic materials 0.000 claims 33
- 150000002367 halogens Chemical class 0.000 claims 33
- 125000001072 heteroaryl group Chemical group 0.000 claims 32
- 125000001424 substituent group Chemical group 0.000 claims 32
- 125000003118 aryl group Chemical group 0.000 claims 26
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 23
- 229910052739 hydrogen Inorganic materials 0.000 claims 21
- 239000001257 hydrogen Substances 0.000 claims 18
- 125000004093 cyano group Chemical group *C#N 0.000 claims 17
- 150000001875 compounds Chemical class 0.000 claims 15
- 125000000753 cycloalkyl group Chemical group 0.000 claims 15
- 150000003839 salts Chemical class 0.000 claims 13
- 125000000392 cycloalkenyl group Chemical group 0.000 claims 12
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 12
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 11
- -1 —C 3-7 cycloalkyl Chemical group 0.000 claims 7
- 125000006272 (C3-C7) cycloalkyl group Chemical group 0.000 claims 6
- ZUOUZKKEUPVFJK-UHFFFAOYSA-N diphenyl Chemical compound C1=CC=CC=C1C1=CC=CC=C1 ZUOUZKKEUPVFJK-UHFFFAOYSA-N 0.000 claims 6
- 201000010099 disease Diseases 0.000 claims 6
- 150000002431 hydrogen Chemical class 0.000 claims 6
- 125000006376 (C3-C10) cycloalkyl group Chemical group 0.000 claims 4
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims 3
- 208000008589 Obesity Diseases 0.000 claims 3
- 235000010290 biphenyl Nutrition 0.000 claims 3
- 239000004305 biphenyl Substances 0.000 claims 3
- 239000000203 mixture Substances 0.000 claims 3
- 235000020824 obesity Nutrition 0.000 claims 3
- 208000001072 type 2 diabetes mellitus Diseases 0.000 claims 3
- 102000014156 AMP-Activated Protein Kinases Human genes 0.000 claims 2
- 108010011376 AMP-Activated Protein Kinases Proteins 0.000 claims 2
- 208000035150 Hypercholesterolemia Diseases 0.000 claims 2
- 206010020772 Hypertension Diseases 0.000 claims 2
- 208000001145 Metabolic Syndrome Diseases 0.000 claims 2
- 201000000690 abdominal obesity-metabolic syndrome Diseases 0.000 claims 2
- 230000004913 activation Effects 0.000 claims 2
- 125000005024 alkenyl aryl group Chemical group 0.000 claims 2
- 125000003342 alkenyl group Chemical group 0.000 claims 2
- 125000000304 alkynyl group Chemical group 0.000 claims 2
- 239000003937 drug carrier Substances 0.000 claims 2
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 2
- 201000001421 hyperglycemia Diseases 0.000 claims 2
- 125000006717 (C3-C10) cycloalkenyl group Chemical group 0.000 claims 1
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims 1
- 241000124008 Mammalia Species 0.000 claims 1
- 206010028980 Neoplasm Diseases 0.000 claims 1
- RYMZZMVNJRMUDD-UHFFFAOYSA-N SJ000286063 Natural products C12C(OC(=O)C(C)(C)CC)CC(C)C=C2C=CC(C)C1CCC1CC(O)CC(=O)O1 RYMZZMVNJRMUDD-UHFFFAOYSA-N 0.000 claims 1
- QLYKJCMUNUWAGO-GAJHUEQPSA-N Taranabant Chemical compound N([C@@H](C)[C@@H](CC=1C=CC(Cl)=CC=1)C=1C=C(C=CC=1)C#N)C(=O)C(C)(C)OC1=CC=C(C(F)(F)F)C=N1 QLYKJCMUNUWAGO-GAJHUEQPSA-N 0.000 claims 1
- 125000005025 alkynylaryl group Chemical group 0.000 claims 1
- 125000006367 bivalent amino carbonyl group Chemical group [H]N([*:1])C([*:2])=O 0.000 claims 1
- 201000011510 cancer Diseases 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- OLNTVTPDXPETLC-XPWALMASSA-N ezetimibe Chemical compound N1([C@@H]([C@H](C1=O)CC[C@H](O)C=1C=CC(F)=CC=1)C=1C=CC(O)=CC=1)C1=CC=C(F)C=C1 OLNTVTPDXPETLC-XPWALMASSA-N 0.000 claims 1
- 229960000815 ezetimibe Drugs 0.000 claims 1
- 125000004404 heteroalkyl group Chemical group 0.000 claims 1
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- RYMZZMVNJRMUDD-HGQWONQESA-N simvastatin Chemical compound C([C@H]1[C@@H](C)C=CC2=C[C@H](C)C[C@@H]([C@H]12)OC(=O)C(C)(C)CC)C[C@@H]1C[C@@H](O)CC(=O)O1 RYMZZMVNJRMUDD-HGQWONQESA-N 0.000 claims 1
- 229960002855 simvastatin Drugs 0.000 claims 1
- MFFMDFFZMYYVKS-SECBINFHSA-N sitagliptin Chemical compound C([C@H](CC(=O)N1CC=2N(C(=NN=2)C(F)(F)F)CC1)N)C1=CC(F)=C(F)C=C1F MFFMDFFZMYYVKS-SECBINFHSA-N 0.000 claims 1
- 229960004034 sitagliptin Drugs 0.000 claims 1
- 229950005022 taranabant Drugs 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US19433708P | 2008-09-26 | 2008-09-26 | |
| US61/194,337 | 2008-09-26 | ||
| PCT/US2009/057686 WO2010036613A1 (en) | 2008-09-26 | 2009-09-21 | Novel cyclic benzimidazole derivatives useful anti-diabetic agents |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2012503661A JP2012503661A (ja) | 2012-02-09 |
| JP2012503661A5 true JP2012503661A5 (enExample) | 2012-09-27 |
| JP5764064B2 JP5764064B2 (ja) | 2015-08-12 |
Family
ID=41395799
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2011529149A Active JP5764064B2 (ja) | 2008-09-26 | 2009-09-21 | 抗糖尿病薬として有用な新規な環状ベンゾイミダゾール誘導体 |
Country Status (10)
| Country | Link |
|---|---|
| US (1) | US8394969B2 (enExample) |
| EP (1) | EP3924343A1 (enExample) |
| JP (1) | JP5764064B2 (enExample) |
| CN (1) | CN102361857B (enExample) |
| AR (1) | AR073677A1 (enExample) |
| AU (1) | AU2009296820B2 (enExample) |
| CA (1) | CA2737694C (enExample) |
| MX (1) | MX2011003239A (enExample) |
| TW (1) | TWI393709B (enExample) |
| WO (1) | WO2010036613A1 (enExample) |
Families Citing this family (54)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US8410284B2 (en) | 2008-10-22 | 2013-04-02 | Merck Sharp & Dohme Corp | Cyclic benzimidazole derivatives useful as anti-diabetic agents |
| JP2012507530A (ja) | 2008-10-29 | 2012-03-29 | メルク・シャープ・エンド・ドーム・コーポレイション | 有用な抗糖尿病剤である新規な環状ベンズイミダゾール誘導体 |
| EP2362731B1 (en) | 2008-10-31 | 2016-04-06 | Merck Sharp & Dohme Corp. | Novel cyclic benzimidazole derivatives useful anti-diabetic agents |
| EA201290808A1 (ru) | 2010-02-18 | 2013-03-29 | ХАЙ ПОЙНТ ФАРМАСЬЮТИКАЛЗ, ЭлЭлСи | Замещенные конденсированные производные имидазола, фармацевтические композиции и способы их применения |
| US8759535B2 (en) | 2010-02-18 | 2014-06-24 | High Point Pharmaceuticals, Llc | Substituted fused imidazole derivatives, pharmaceutical compositions, and methods of use thereof |
| JP2013520502A (ja) * | 2010-02-25 | 2013-06-06 | メルク・シャープ・エンド・ドーム・コーポレイション | 有用な抗糖尿病薬である新規な環状ベンズイミダゾール誘導体 |
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| EP2970119B1 (en) | 2013-03-14 | 2021-11-03 | Merck Sharp & Dohme Corp. | Novel indole derivatives useful as anti-diabetic agents |
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| US10519115B2 (en) | 2013-11-15 | 2019-12-31 | Merck Sharp & Dohme Corp. | Antidiabetic tricyclic compounds |
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2009
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- 2009-09-21 WO PCT/US2009/057686 patent/WO2010036613A1/en not_active Ceased
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