JP2013510168A5 - - Google Patents
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- JP2013510168A5 JP2013510168A5 JP2012538024A JP2012538024A JP2013510168A5 JP 2013510168 A5 JP2013510168 A5 JP 2013510168A5 JP 2012538024 A JP2012538024 A JP 2012538024A JP 2012538024 A JP2012538024 A JP 2012538024A JP 2013510168 A5 JP2013510168 A5 JP 2013510168A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- oxo
- alkyloxy
- group
- dihydro
- 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.)
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- -1 2-oxo-1,2-dihydro-pyridinyl Chemical group 0.000 claims 128
- 150000001875 compounds Chemical class 0.000 claims 29
- 150000003839 salts Chemical class 0.000 claims 18
- 125000003118 aryl group Chemical group 0.000 claims 16
- 229910052731 fluorine Inorganic materials 0.000 claims 12
- 239000011737 fluorine Substances 0.000 claims 12
- 208000001072 type 2 diabetes mellitus Diseases 0.000 claims 12
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims 11
- 125000004432 carbon atom Chemical group C* 0.000 claims 11
- 229910052739 hydrogen Inorganic materials 0.000 claims 10
- 239000001257 hydrogen Substances 0.000 claims 10
- 239000008194 pharmaceutical composition Substances 0.000 claims 10
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 10
- 229910052799 carbon Inorganic materials 0.000 claims 9
- 125000004093 cyano group Chemical group *C#N 0.000 claims 9
- 125000006576 di-(C1-C3-alkyl)-aminocarbonyl group Chemical group 0.000 claims 9
- 201000010099 disease Diseases 0.000 claims 9
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 9
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 9
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims 9
- 125000006563 (C1-3) alkylaminocarbonyl group Chemical group 0.000 claims 8
- 125000006698 (C1-C3) dialkylamino group Chemical group 0.000 claims 8
- PXGOKWXKJXAPGV-UHFFFAOYSA-N Fluorine Chemical group FF PXGOKWXKJXAPGV-UHFFFAOYSA-N 0.000 claims 8
- 125000006559 (C1-C3) alkylamino group Chemical group 0.000 claims 7
- ZAMOUSCENKQFHK-UHFFFAOYSA-N Chlorine atom Chemical compound [Cl] ZAMOUSCENKQFHK-UHFFFAOYSA-N 0.000 claims 7
- 125000002915 carbonyl group Chemical group [*:2]C([*:1])=O 0.000 claims 7
- 229910052801 chlorine Inorganic materials 0.000 claims 7
- 239000000460 chlorine Substances 0.000 claims 7
- 229910052736 halogen Inorganic materials 0.000 claims 7
- 150000002367 halogens Chemical class 0.000 claims 7
- 150000002431 hydrogen Chemical class 0.000 claims 7
- 125000000499 benzofuranyl group Chemical group O1C(=CC2=C1C=CC=C2)* 0.000 claims 6
- 125000004196 benzothienyl group Chemical group S1C(=CC2=C1C=CC=C2)* 0.000 claims 6
- 125000002541 furyl group Chemical group 0.000 claims 6
- 125000001041 indolyl group Chemical group 0.000 claims 6
- 125000002183 isoquinolinyl group Chemical group C1(=NC=CC2=CC=CC=C12)* 0.000 claims 6
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 6
- 125000004076 pyridyl group Chemical group 0.000 claims 6
- 125000000168 pyrrolyl group Chemical group 0.000 claims 6
- 125000002943 quinolinyl group Chemical group N1=C(C=CC2=CC=CC=C12)* 0.000 claims 6
- 125000001544 thienyl group Chemical group 0.000 claims 6
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims 5
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 5
- 125000001424 substituent group Chemical group 0.000 claims 5
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 claims 4
- 208000032928 Dyslipidaemia Diseases 0.000 claims 4
- 206010022489 Insulin Resistance Diseases 0.000 claims 4
- 208000017170 Lipid metabolism disease Diseases 0.000 claims 4
- 208000008589 Obesity Diseases 0.000 claims 4
- NQRYJNQNLNOLGT-UHFFFAOYSA-N Piperidine Chemical compound C1CCNCC1 NQRYJNQNLNOLGT-UHFFFAOYSA-N 0.000 claims 4
- 239000000470 constituent Substances 0.000 claims 4
- 239000003937 drug carrier Substances 0.000 claims 4
- 125000001153 fluoro group Chemical group F* 0.000 claims 4
- 235000020824 obesity Nutrition 0.000 claims 4
- 125000004769 (C1-C4) alkylsulfonyl group Chemical group 0.000 claims 3
- WKBOTKDWSSQWDR-UHFFFAOYSA-N Bromine atom Chemical compound [Br] WKBOTKDWSSQWDR-UHFFFAOYSA-N 0.000 claims 3
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims 3
- 208000002705 Glucose Intolerance Diseases 0.000 claims 3
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 3
- 208000031226 Hyperlipidaemia Diseases 0.000 claims 3
- 125000005100 aryl amino carbonyl group Chemical group 0.000 claims 3
- 125000004104 aryloxy group Chemical group 0.000 claims 3
- GDTBXPJZTBHREO-UHFFFAOYSA-N bromine Substances BrBr GDTBXPJZTBHREO-UHFFFAOYSA-N 0.000 claims 3
- 229910052794 bromium Inorganic materials 0.000 claims 3
- 125000003016 chromanyl group Chemical group O1C(CCC2=CC=CC=C12)* 0.000 claims 3
- 125000000753 cycloalkyl group Chemical group 0.000 claims 3
- 125000001028 difluoromethyl group Chemical group [H]C(F)(F)* 0.000 claims 3
- 201000001421 hyperglycemia Diseases 0.000 claims 3
- 239000000203 mixture Substances 0.000 claims 3
- 125000001624 naphthyl group Chemical group 0.000 claims 3
- 201000009104 prediabetes syndrome Diseases 0.000 claims 3
- CXWXQJXEFPUFDZ-UHFFFAOYSA-N tetralin Chemical compound C1=CC=C2CCCCC2=C1 CXWXQJXEFPUFDZ-UHFFFAOYSA-N 0.000 claims 3
- 125000006595 (C1-C3) alkylsulfinyl group Chemical group 0.000 claims 2
- 125000004455 (C1-C3) alkylthio group Chemical group 0.000 claims 2
- 125000004605 1,2,3,4-tetrahydroisoquinolinyl group Chemical group C1(NCCC2=CC=CC=C12)* 0.000 claims 2
- 125000004607 1,2,3,4-tetrahydroquinolinyl group Chemical group N1(CCCC2=CC=CC=C12)* 0.000 claims 2
- 125000004539 5-benzimidazolyl group Chemical group N1=CNC2=C1C=CC(=C2)* 0.000 claims 2
- 102000011145 Hydroxysteroid Dehydrogenases Human genes 0.000 claims 2
- 108010062875 Hydroxysteroid Dehydrogenases Proteins 0.000 claims 2
- 125000004397 aminosulfonyl group Chemical group NS(=O)(=O)* 0.000 claims 2
- 125000004658 aryl carbonyl amino group Chemical group 0.000 claims 2
- 125000004657 aryl sulfonyl amino group Chemical group 0.000 claims 2
- 125000003917 carbamoyl group Chemical group [H]N([H])C(*)=O 0.000 claims 2
- 125000000332 coumarinyl group Chemical group O1C(=O)C(=CC2=CC=CC=C12)* 0.000 claims 2
- PQNFLJBBNBOBRQ-UHFFFAOYSA-N indane Chemical compound C1=CC=C2CCCC2=C1 PQNFLJBBNBOBRQ-UHFFFAOYSA-N 0.000 claims 2
- 125000003392 indanyl group Chemical group C1(CCC2=CC=CC=C12)* 0.000 claims 2
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims 2
- 125000006216 methylsulfinyl group Chemical group [H]C([H])([H])S(*)=O 0.000 claims 2
- 125000004170 methylsulfonyl group Chemical group [H]C([H])([H])S(*)(=O)=O 0.000 claims 2
- 125000004573 morpholin-4-yl group Chemical group N1(CCOCC1)* 0.000 claims 2
- 208000024891 symptom Diseases 0.000 claims 2
- 125000003831 tetrazolyl group Chemical group 0.000 claims 2
- 125000006599 (C1-C3) alkylaminocarbonylamino group Chemical group 0.000 claims 1
- 125000006603 (C1-C3) alkylaminosulfonyl group Chemical group 0.000 claims 1
- 125000006597 (C1-C3) alkylcarbonylamino group Chemical group 0.000 claims 1
- 125000006594 (C1-C3) alkylsulfony group Chemical group 0.000 claims 1
- 125000006602 (C1-C3) alkylsulfonylamino group Chemical group 0.000 claims 1
- 125000004768 (C1-C4) alkylsulfinyl group Chemical group 0.000 claims 1
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims 1
- 208000009304 Acute Kidney Injury Diseases 0.000 claims 1
- 208000019901 Anxiety disease Diseases 0.000 claims 1
- 201000001320 Atherosclerosis Diseases 0.000 claims 1
- 125000003830 C1- C4 alkylcarbonylamino group Chemical group 0.000 claims 1
- 206010007558 Cardiac failure chronic Diseases 0.000 claims 1
- 102000004190 Enzymes Human genes 0.000 claims 1
- 108090000790 Enzymes Proteins 0.000 claims 1
- 208000010412 Glaucoma Diseases 0.000 claims 1
- 206010060378 Hyperinsulinaemia Diseases 0.000 claims 1
- 206010020772 Hypertension Diseases 0.000 claims 1
- 201000001431 Hyperuricemia Diseases 0.000 claims 1
- 208000013016 Hypoglycemia Diseases 0.000 claims 1
- 206010024229 Leprosy Diseases 0.000 claims 1
- 208000001145 Metabolic Syndrome Diseases 0.000 claims 1
- 206010030113 Oedema Diseases 0.000 claims 1
- 208000001132 Osteoporosis Diseases 0.000 claims 1
- 201000004681 Psoriasis Diseases 0.000 claims 1
- 208000033626 Renal failure acute Diseases 0.000 claims 1
- 208000017442 Retinal disease Diseases 0.000 claims 1
- 206010038923 Retinopathy Diseases 0.000 claims 1
- 206010067584 Type 1 diabetes mellitus Diseases 0.000 claims 1
- 201000000690 abdominal obesity-metabolic syndrome Diseases 0.000 claims 1
- 201000011040 acute kidney failure Diseases 0.000 claims 1
- 208000012998 acute renal failure Diseases 0.000 claims 1
- 125000001931 aliphatic group Chemical group 0.000 claims 1
- 125000003342 alkenyl group Chemical group 0.000 claims 1
- 125000003545 alkoxy group Chemical group 0.000 claims 1
- 125000000217 alkyl group Chemical group 0.000 claims 1
- 125000004414 alkyl thio group Chemical group 0.000 claims 1
- 125000002947 alkylene group Chemical group 0.000 claims 1
- 125000000304 alkynyl group Chemical group 0.000 claims 1
- 125000006598 aminocarbonylamino group Chemical group 0.000 claims 1
- 230000036506 anxiety Effects 0.000 claims 1
- 125000005129 aryl carbonyl group Chemical group 0.000 claims 1
- 125000004391 aryl sulfonyl group Chemical group 0.000 claims 1
- 125000005605 benzo group Chemical group 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
- 208000010877 cognitive disease Diseases 0.000 claims 1
- 125000004786 difluoromethoxy group Chemical group [H]C(F)(F)O* 0.000 claims 1
- 125000002147 dimethylamino group Chemical group [H]C([H])([H])N(*)C([H])([H])[H] 0.000 claims 1
- 208000016097 disease of metabolism Diseases 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 1
- 230000003451 hyperinsulinaemic effect Effects 0.000 claims 1
- 201000008980 hyperinsulinism Diseases 0.000 claims 1
- 230000002218 hypoglycaemic effect Effects 0.000 claims 1
- 230000002401 inhibitory effect Effects 0.000 claims 1
- 208000017169 kidney disease Diseases 0.000 claims 1
- 208000030159 metabolic disease Diseases 0.000 claims 1
- 201000001119 neuropathy Diseases 0.000 claims 1
- 230000007823 neuropathy Effects 0.000 claims 1
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims 1
- 125000005740 oxycarbonyl group Chemical group [*:1]OC([*:2])=O 0.000 claims 1
- 208000033808 peripheral neuropathy Diseases 0.000 claims 1
- 125000003170 phenylsulfonyl group Chemical group C1(=CC=CC=C1)S(=O)(=O)* 0.000 claims 1
- 125000004194 piperazin-1-yl group Chemical group [H]N1C([H])([H])C([H])([H])N(*)C([H])([H])C1([H])[H] 0.000 claims 1
- 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 1
- 230000002265 prevention Effects 0.000 claims 1
- 125000000876 trifluoromethoxy group Chemical group FC(F)(F)O* 0.000 claims 1
- 201000008827 tuberculosis Diseases 0.000 claims 1
- VVZNCSHIBODHMZ-UZLBHIALSA-N N#Cc1ccc(C[C@@H]([C@@H]2CCC3)N3C(c3ccc4[nH]cnc4c3)=O)c2c1 Chemical compound N#Cc1ccc(C[C@@H]([C@@H]2CCC3)N3C(c3ccc4[nH]cnc4c3)=O)c2c1 VVZNCSHIBODHMZ-UZLBHIALSA-N 0.000 description 2
- YKJMSVPGIQUKAE-UHFFFAOYSA-N COc(c(CC1)c2C(CCC3)C1N3C(c1ccccc1)=O)ccc2OC Chemical compound COc(c(CC1)c2C(CCC3)C1N3C(c1ccccc1)=O)ccc2OC YKJMSVPGIQUKAE-UHFFFAOYSA-N 0.000 description 1
- WBRBKXDJEFBTPS-UHFFFAOYSA-N COc(ccc(C1CCC2)c3CCC1N2C(c1c(cccc2)c2ccc1)=O)c3OC Chemical compound COc(ccc(C1CCC2)c3CCC1N2C(c1c(cccc2)c2ccc1)=O)c3OC WBRBKXDJEFBTPS-UHFFFAOYSA-N 0.000 description 1
- VVZNCSHIBODHMZ-UHFFFAOYSA-N N#Cc1ccc(CC(C2CCC3)N3C(c3ccc4[nH]cnc4c3)=O)c2c1 Chemical compound N#Cc1ccc(CC(C2CCC3)N3C(c3ccc4[nH]cnc4c3)=O)c2c1 VVZNCSHIBODHMZ-UHFFFAOYSA-N 0.000 description 1
- PJOXCTCDMCPNMB-UHFFFAOYSA-N O=C(c1ccc2[nH]cnc2c1)N(CCC1)C2C1c1ccccc1C2 Chemical compound O=C(c1ccc2[nH]cnc2c1)N(CCC1)C2C1c1ccccc1C2 PJOXCTCDMCPNMB-UHFFFAOYSA-N 0.000 description 1
- LDXJDJWFSSSGPR-UHFFFAOYSA-N O=C(c1ccc2[nH]cnc2c1)N(CCC1)C2C1c1ccccc1CC2 Chemical compound O=C(c1ccc2[nH]cnc2c1)N(CCC1)C2C1c1ccccc1CC2 LDXJDJWFSSSGPR-UHFFFAOYSA-N 0.000 description 1
- PJOXCTCDMCPNMB-APWZRJJASA-N O=C(c1ccc2[nH]cnc2c1)N(CCC1)[C@@H](C2)[C@H]1c1c2cccc1 Chemical compound O=C(c1ccc2[nH]cnc2c1)N(CCC1)[C@@H](C2)[C@H]1c1c2cccc1 PJOXCTCDMCPNMB-APWZRJJASA-N 0.000 description 1
- LJPINMOPGGIXOP-UHFFFAOYSA-N O=C(c1ccccc1)N(CCC1)C2C1c1ccccc1CC2 Chemical compound O=C(c1ccccc1)N(CCC1)C2C1c1ccccc1CC2 LJPINMOPGGIXOP-UHFFFAOYSA-N 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP09175233 | 2009-11-06 | ||
| EP09175233.7 | 2009-11-06 | ||
| PCT/US2010/055586 WO2011057054A1 (en) | 2009-11-06 | 2010-11-05 | Aryl- and heteroarylcarbonyl derivatives of hexahydroindenopyridine and octahydrobenzoquinoline |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2013510168A JP2013510168A (ja) | 2013-03-21 |
| JP2013510168A5 true JP2013510168A5 (cg-RX-API-DMAC7.html) | 2013-11-28 |
| JP5796015B2 JP5796015B2 (ja) | 2015-10-21 |
Family
ID=41683136
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2012538024A Active JP5796015B2 (ja) | 2009-11-06 | 2010-11-05 | ヘキサヒドロインデノピリジン及びオクタヒドロベンゾキノリンのアリール−及びヘテロアリールカルボニル誘導体 |
Country Status (27)
Families Citing this family (31)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ATE554078T1 (de) | 2007-07-26 | 2012-05-15 | Vitae Pharmaceuticals Inc | Synthese von 11-beta-hydroxysteroid-dehydrogenase-1-hemmern |
| AR069207A1 (es) | 2007-11-07 | 2010-01-06 | Vitae Pharmaceuticals Inc | Ureas ciclicas como inhibidores de la 11 beta - hidroxi-esteroide deshidrogenasa 1 |
| WO2009063061A2 (en) * | 2007-11-16 | 2009-05-22 | Boehringer Ingelheim International Gmbh | Aryl- and heteroarylcarbonyl derivatives of benzomorphanes and related scaffolds, medicaments containing such compounds and their use |
| WO2009075835A1 (en) | 2007-12-11 | 2009-06-18 | Vitae Pharmaceutical, Inc | CYCLIC UREA INHIBITORS OF 11β-HYDROXYSTEROID DEHYDROGENASE 1 |
| TW200934490A (en) | 2008-01-07 | 2009-08-16 | Vitae Pharmaceuticals Inc | Lactam inhibitors of 11 &abgr;-hydroxysteroid dehydrogenase 1 |
| JP5490020B2 (ja) | 2008-01-24 | 2014-05-14 | ヴァイティー ファーマシューティカルズ，インコーポレイテッド | １１β−ヒドロキシステロイドデヒドロゲナーゼ１の環状カルバゼート及びセミカルバジドインヒビター |
| US20110028445A1 (en) * | 2008-02-12 | 2011-02-03 | Boehringer Ingelheim International Gmbh | Urea derivatives of benzomorphanes and related scaffolds, medicaments containing such compounds and their use |
| EP2254872A2 (en) | 2008-02-15 | 2010-12-01 | Vitae Pharmaceuticals, Inc. | Cycloalkyl lactame derivatives as inhibitors of 11-beta-hydroxysteroid dehydrogenase 1 |
| AU2009241727B2 (en) | 2008-05-01 | 2013-05-02 | Vitae Pharmaceuticals, Inc | Cyclic inhibitors of 11beta-hydroxysteroid dehydrogenase 1 |
| US8592410B2 (en) | 2008-05-01 | 2013-11-26 | Vitae Pharmaceuticals, Inc. | Cyclic inhibitors of 11BETA-hydroxysteroid dehydrogenase 1 |
| CL2009001058A1 (es) | 2008-05-01 | 2010-09-10 | Vitae Pharmaceuticals Inc | Compuestos derivados de oxazinas sustituidas, inhibidores de la 11b-hidroxiesteroide deshidrogenasa de tipo-1; composicion farmaceutica; y uso del compuesto para inhibir la actividad de 11b-hsd1, como en el tratamiento de la diabetes, dislipidemia, hipertension, obesidad, cancer, glaucoma, entre otras. |
| US8765780B2 (en) | 2008-05-13 | 2014-07-01 | Boehringer Ingelheim International Gmbh | Alicyclic carboxylic acid derivatives of benzomorphans and related scaffolds, medicaments containing such compounds and their use |
| JP5379160B2 (ja) | 2008-07-25 | 2013-12-25 | ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング | １１β−ヒドロキシステロイドデヒドロゲナーゼ１の環状インヒビター |
| CA2729998A1 (en) | 2008-07-25 | 2010-01-28 | Boehringer Ingelheim International Gmbh | Inhibitors of 11beta-hydroxysteroid dehydrogenase 1 |
| WO2010046445A2 (en) | 2008-10-23 | 2010-04-29 | Boehringer Ingelheim International Gmbh | Urea derivatives of substituted nortropanes, medicaments containing such compounds and their use |
| CA2744946A1 (en) | 2009-02-04 | 2010-08-12 | Boehringer Ingelheim International Gmbh | Cyclic inhibitors of 11.beta.-hydroxysteroid dehydrogenase 1 |
| MA33216B1 (fr) | 2009-04-30 | 2012-04-02 | Boehringer Ingelheim Int | Inhibiteurs cycliques de la 11béta-hydroxysteroïde déshydrogénase 1 |
| WO2010139673A1 (en) | 2009-06-02 | 2010-12-09 | Boehringer Ingelheim International Gmbh | Cyclic inhibitors of 11beta-hydroxysteroid dehydrogenase 1 |
| EP2440537A1 (en) | 2009-06-11 | 2012-04-18 | Vitae Pharmaceuticals, Inc. | Cyclic inhibitors of 11beta-hydroxysteroid dehydrogenase 1 based on the 1,3 -oxazinan- 2 -one structure |
| UY33001A (es) * | 2009-11-06 | 2011-05-31 | Boehringer Ingelheim Int | Derivados arilo y heteroarilcarbonilo de hexahidroindenopiridina y octahidrobenzoquinolina |
| JP5860042B2 (ja) | 2010-06-16 | 2016-02-16 | ヴァイティー ファーマシューティカルズ，インコーポレイテッド | 置換５、６及び７員複素環、そのような化合物を含有する医薬及びそれらの使用 |
| JP5813106B2 (ja) | 2010-06-25 | 2015-11-17 | ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング | 代謝障害の処置のための１１−β−ＨＳＤ１のインヒビターとしてのアザスピロヘキサノン |
| CA2813671A1 (en) | 2010-11-02 | 2012-05-10 | Boehringer Ingelheim International Gmbh | Pharmaceutical combinations for the treatment of metabolic disorders |
| TWI537258B (zh) * | 2010-11-05 | 2016-06-11 | 百靈佳殷格翰國際股份有限公司 | 六氫茚并吡啶及八氫苯并喹啉之芳基－及雜環芳基羰基衍生物 |
| EP2744783A1 (en) | 2011-08-17 | 2014-06-25 | Boehringer Ingelheim International GmbH | Indenopyridine derivatives |
| BR112014027884A2 (pt) * | 2012-05-09 | 2017-06-27 | Boehringer Ingelheim Int | combinações farmacêuticas para tratamento de distúrbios metabólicos |
| JO3407B1 (ar) | 2012-05-31 | 2019-10-20 | Eisai R&D Man Co Ltd | مركبات رباعي هيدرو بيرازولو بيريميدين |
| US20150141651A1 (en) * | 2013-11-20 | 2015-05-21 | Boehringer Ingelheim International Gmbh | Hexahydroindenopyridine derivatives |
| CN109045035B (zh) * | 2018-07-19 | 2020-07-28 | 广西科技大学 | 7-(2,2-二甲基-3-丁烯酰胺基)-八氢苯喹啉乙酸酯在制备治疗肝病药物的应用 |
| AR127706A1 (es) * | 2021-11-19 | 2024-02-21 | Hoffmann La Roche | Síntesis de 2-(7,7-dimetil-1h,7h-espiro[furo[3,4-b]piridin-5,4-piperidin]-1-il)-1,3-dihidro-4h-espiro[inden-2,5-[1,3]oxazol]-4-ona |
| CN116554000B (zh) * | 2023-04-28 | 2025-07-25 | 南京林业大学 | 一种金属铑不对称催化二烷基取代的内炔制备茚醇的方法 |
Family Cites Families (67)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| NL127995C (cg-RX-API-DMAC7.html) | 1963-12-20 | Geigy Ag J R | ||
| US3341538A (en) * | 1965-06-18 | 1967-09-12 | Geigy Chem Corp | Certain 2, 6-methano-3-benzazocines |
| DE1785124A1 (de) * | 1968-08-13 | 1971-11-11 | Prym Werke William | Reissverschluss |
| DE2108954A1 (en) | 1971-02-25 | 1972-09-07 | Boehringer Sohn Ingelheim | 2-(furylmethyl)-6,7-benzomorphans - useful as cns active agents |
| GB1304175A (cg-RX-API-DMAC7.html) * | 1969-03-31 | 1973-01-24 | ||
| DE2105743C3 (de) | 1971-02-08 | 1979-11-29 | Boehringer Sohn Ingelheim | 2-(Furylmethyl)- a -5,9-dialkyl -6,7benzomorphane, Verfahren zu ihrer Herstellung und deren Verwendung |
| US3681349A (en) * | 1970-03-05 | 1972-08-01 | Morton Norwich Products Inc | 1-(substituted benzyl) tetrahydro-2-(1h) pyrimidones |
| US3657257A (en) * | 1970-08-31 | 1972-04-18 | Robins Co Inc A H | 3-aryl-8-carbamoyl nortropanes |
| DE2229695A1 (de) | 1972-06-19 | 1974-01-31 | Boehringer Sohn Ingelheim | 2-(heteroaryl-methyl)-5,9 beta-dialkyl6,7-benzomorphane, deren saeureadditionssalze sowie verfahren zu deren herstellung |
| DE2338369A1 (de) * | 1973-07-26 | 1975-02-13 | Schering Ag | Mikrobiologische hydroxylierung von 2,6-methano-3-benzazocinen |
| SU510999A3 (ru) * | 1973-10-27 | 1976-04-15 | К.Х.Берингер Зон, (Фирма) | Способ получени (метоксиметил-фурилметил)6,7-бензоморфанов илиморфинанов |
| US4009171A (en) * | 1974-02-21 | 1977-02-22 | Sterling Drug Inc. | N-acylated-11-oxygenated-2,6-methano-3-benzazocine intermediates |
| DE2411382C3 (de) | 1974-03-09 | 1979-09-06 | C.H. Boehringer Sohn, 6507 Ingelheim | 2-Tetrahydrofurfuryl-6,7-benzomorphane, Verfahren zur Herstellung und deren Verwendung |
| US4087532A (en) * | 1974-03-09 | 1978-05-02 | Boehringer Ingelheim Gmbh | Analgesically useful 2-tetrahydrofurfuryl-5-lower alkyl-2-oxy-6,7-benzomorphans and salts thereof |
| DE2437610A1 (de) | 1974-08-05 | 1976-02-26 | Boehringer Sohn Ingelheim | Neue 5,9-beta-disubstituierte 2-tetrahydrofurfuryl-6,7-benzomorphane, deren saeureadditionssalze, ihre verwendung als arzneimittel und verfahren zu deren herstellung |
| US4108857A (en) * | 1975-08-18 | 1978-08-22 | Sterling Drug Inc. | Imidazolylmethyl methanobenzazocines |
| DE2828039A1 (de) * | 1978-06-26 | 1980-01-10 | Boehringer Sohn Ingelheim | 2-(2-alkoxyethyl)-2'-hydroxy-6,7-benzomorphane deren saeureadditionssalze diese enthaltende arzneimittel und verfahren zu deren herstellung |
| GB9510459D0 (en) | 1995-05-24 | 1995-07-19 | Zeneca Ltd | Bicyclic amines |
| GB9517622D0 (en) * | 1995-08-29 | 1995-11-01 | Univ Edinburgh | Regulation of intracellular glucocorticoid concentrations |
| JP3192662B2 (ja) | 1996-07-31 | 2001-07-30 | 日研化学株式会社 | ６―フェニルテトラヒドロ―１，３―オキサジン―２―オン誘導体及びそれを含む医薬組成物 |
| GB9623944D0 (en) | 1996-11-15 | 1997-01-08 | Zeneca Ltd | Bicyclic amine derivatives |
| DE69816758T2 (de) | 1997-05-20 | 2004-06-03 | Heraeus Quarzglas Gmbh & Co. Kg | Synthetisches quarzglas zur verwendung in uv-strahlung und verfahren zu seiner herstellung |
| US6514977B1 (en) | 1997-05-22 | 2003-02-04 | G.D. Searle & Company | Substituted pyrazoles as p38 kinase inhibitors |
| YU54202A (sh) | 2000-01-18 | 2006-01-16 | Agouron Pharmaceuticals Inc. | Jedinjenja indazola, farmaceutske smeše i postupci za stimulisanje i inhibiranje ćelijske proliferacije |
| WO2001055063A1 (en) | 2000-01-25 | 2001-08-02 | Idemitsu Petrochemical Co., Ltd. | Novel bisadamantane compounds, process for preparing the same, and novel biadamantane derivatives |
| DE10034623A1 (de) | 2000-07-17 | 2002-01-31 | Bayer Ag | Heterocyclisch substituierte Pyridine als Cytokin-Inhibitoren |
| AU2003234621A1 (en) | 2002-05-17 | 2003-12-02 | Jenken Biosciences, Inc. | Opioid and opioid-like compounds and uses thereof |
| AU2004226452B2 (en) * | 2003-03-26 | 2008-07-24 | Merck Sharp & Dohme Corp. | Bicyclic piperidine derivatives as melanocortin-4 receptor agonists |
| US7700583B2 (en) * | 2003-04-11 | 2010-04-20 | High Point Pharmaceuticals, Llc | 11β-hydroxysteroid dehydrogenase type 1 active compounds |
| ATE482747T1 (de) * | 2003-04-11 | 2010-10-15 | High Point Pharmaceuticals Llc | Neue amide derivate und deren pharmazeutische verwendungen |
| EP1862181A3 (en) * | 2003-04-11 | 2010-09-15 | High Point Pharmaceuticals, LLC | New pyrazolo[1,5-a] pyrimidine derivatives and pharmaceutical use thereof |
| CN101001842B (zh) * | 2004-05-07 | 2015-10-07 | 因塞特公司 | 酰氨基化合物及其作为药物的应用 |
| DE602005007344D1 (de) | 2004-05-07 | 2008-07-17 | Janssen Pharmaceutica Nv | Adamantyl pyrrolidin-2-on-derivate als 11-beta hydroxysteroid dehydrogenas inhibitoren |
| WO2006024628A1 (en) | 2004-08-30 | 2006-03-09 | Janssen Pharmaceutica N.V. | Tricyclic lactam derivatives as 11-beta hydroxysteroid dehydrogenase inhibitors |
| JP2008515956A (ja) | 2004-10-12 | 2008-05-15 | ノボ ノルディスク アクティーゼルスカブ | １１β−ヒドロキシステロイドデヒドロゲナーゼ１型活性スピロ化合物 |
| JP2008515972A (ja) | 2004-10-13 | 2008-05-15 | ニューロジェン・コーポレーション | メラニン濃縮ホルモン受容体のリガンドとしてのアリール置換８−アザビシクロ［３．２．１］オクタン化合物 |
| US20090264650A1 (en) | 2005-03-31 | 2009-10-22 | Nobuo Cho | Prophylactic/Therapeutic Agent for Diabetes |
| RU2381217C2 (ru) * | 2005-04-05 | 2010-02-10 | Ф.Хоффман-Ля Рош Аг | Пиразолы |
| KR20080076916A (ko) | 2005-11-01 | 2008-08-20 | 트랜스테크 파르마, 인크. | 치환된 아미드의 약학적 사용 |
| EP1945207A2 (en) | 2005-11-01 | 2008-07-23 | Transtech Pharma, Inc. | Pharmaceutical use of substituted amides |
| JP2007140188A (ja) | 2005-11-18 | 2007-06-07 | Fujifilm Corp | ポジ型感光性組成物及びそれを用いたパターン形成方法 |
| WO2007076055A2 (en) | 2005-12-22 | 2007-07-05 | Entremed, Inc. | Compositions and methods comprising proteinase activated receptor antagonists |
| AU2006335109B2 (en) | 2005-12-30 | 2011-04-07 | Merck Sharp & Dohme Corp. | Cholesteryl ester transfer protein inhibitors |
| TW200804341A (en) * | 2006-01-31 | 2008-01-16 | Incyte Corp | Amido compounds and their use as pharmaceuticals |
| EP2016047B1 (en) | 2006-04-21 | 2013-08-28 | Eli Lilly And Company | Biphenyl amide lactam derivatives as inhibitors of 11- beta-hydroxysteroid dehydrogenase 1 |
| EA016959B1 (ru) | 2006-04-24 | 2012-08-30 | Эли Лилли Энд Компани | Замещенные пирролидиноны в качестве ингибиторов 11-бета-гидроксистероиддегидрогеназы 1 типа |
| CA2648019C (en) | 2006-04-25 | 2014-04-01 | Eli Lilly And Company | Inhibitors of 11-beta-hydroxysteroid dehydrogenase 1 |
| TW200811170A (en) * | 2006-06-27 | 2008-03-01 | Sanofi Aventis | Urea derivatives of tropane, their preparation and their therapeutic application |
| CN101553474B (zh) | 2006-10-19 | 2013-02-27 | 霍夫曼-拉罗奇有限公司 | 作为糖尿病用11b-HSD1抑制剂的咪唑啉酮和咪唑烷酮衍生物 |
| TW200829171A (en) * | 2006-11-17 | 2008-07-16 | Nihon Nohyaku Co Ltd | Haloalkyl sulfonanilide derivatives or salts thereof, herbicide using it as effective constituent and use-method thereof |
| EP1935420A1 (en) | 2006-12-21 | 2008-06-25 | Merck Sante | 2-Adamantyl-butyramide derivatives as selective 11beta-HSD1 inhibitors |
| US8835426B2 (en) | 2007-02-26 | 2014-09-16 | Vitae Pharmaceuticals, Inc. | Cyclic urea and carbamate inhibitors of 11β-hydroxysteroid dehydrogenase 1 |
| RU64276U1 (ru) | 2007-03-01 | 2007-06-27 | Открытое акционерное общество "Татнефть" им. В.Д. Шашина | Трубная обвязка устьевой арматуры нагнетательной скважины |
| CN101652359A (zh) | 2007-03-09 | 2010-02-17 | 高点制药有限责任公司 | 作为羟类固醇脱氢酶抑制剂的吲哚-和苯并咪唑酰胺类 |
| ATE554078T1 (de) | 2007-07-26 | 2012-05-15 | Vitae Pharmaceuticals Inc | Synthese von 11-beta-hydroxysteroid-dehydrogenase-1-hemmern |
| AR069207A1 (es) | 2007-11-07 | 2010-01-06 | Vitae Pharmaceuticals Inc | Ureas ciclicas como inhibidores de la 11 beta - hidroxi-esteroide deshidrogenasa 1 |
| WO2009063061A2 (en) * | 2007-11-16 | 2009-05-22 | Boehringer Ingelheim International Gmbh | Aryl- and heteroarylcarbonyl derivatives of benzomorphanes and related scaffolds, medicaments containing such compounds and their use |
| JP5734666B2 (ja) | 2008-02-11 | 2015-06-17 | ヴァイティー ファーマシューティカルズ，インコーポレイテッド | １１β−ヒドロキシステロイドデヒドロゲナーゼ１の１，３−オキサアゼパン−２−オン及び１，３−ジアゼパン−２−オン阻害剤 |
| US20110028445A1 (en) * | 2008-02-12 | 2011-02-03 | Boehringer Ingelheim International Gmbh | Urea derivatives of benzomorphanes and related scaffolds, medicaments containing such compounds and their use |
| EP2254872A2 (en) | 2008-02-15 | 2010-12-01 | Vitae Pharmaceuticals, Inc. | Cycloalkyl lactame derivatives as inhibitors of 11-beta-hydroxysteroid dehydrogenase 1 |
| JP5538356B2 (ja) | 2008-03-18 | 2014-07-02 | ヴァイティー ファーマシューティカルズ，インコーポレイテッド | １１β−ヒドロキシステロイドデヒドロゲナーゼ１型の阻害剤 |
| US8592410B2 (en) * | 2008-05-01 | 2013-11-26 | Vitae Pharmaceuticals, Inc. | Cyclic inhibitors of 11BETA-hydroxysteroid dehydrogenase 1 |
| AU2009241727B2 (en) | 2008-05-01 | 2013-05-02 | Vitae Pharmaceuticals, Inc | Cyclic inhibitors of 11beta-hydroxysteroid dehydrogenase 1 |
| CA2729998A1 (en) | 2008-07-25 | 2010-01-28 | Boehringer Ingelheim International Gmbh | Inhibitors of 11beta-hydroxysteroid dehydrogenase 1 |
| JP5379160B2 (ja) | 2008-07-25 | 2013-12-25 | ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング | １１β−ヒドロキシステロイドデヒドロゲナーゼ１の環状インヒビター |
| MA33216B1 (fr) * | 2009-04-30 | 2012-04-02 | Boehringer Ingelheim Int | Inhibiteurs cycliques de la 11béta-hydroxysteroïde déshydrogénase 1 |
| UY33001A (es) * | 2009-11-06 | 2011-05-31 | Boehringer Ingelheim Int | Derivados arilo y heteroarilcarbonilo de hexahidroindenopiridina y octahidrobenzoquinolina |
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- 2010-11-04 UY UY0001033001A patent/UY33001A/es not_active Application Discontinuation
- 2010-11-04 AR ARP100104083A patent/AR078887A1/es unknown
- 2010-11-04 TW TW099137926A patent/TWI531571B/zh not_active IP Right Cessation
- 2010-11-05 EP EP10782081.3A patent/EP2496559B1/en active Active
- 2010-11-05 PE PE2012000605A patent/PE20121182A1/es not_active Application Discontinuation
- 2010-11-05 MX MX2012005309A patent/MX2012005309A/es active IP Right Grant
- 2010-11-05 US US12/940,387 patent/US8497281B2/en active Active
- 2010-11-05 CA CA2778161A patent/CA2778161A1/en not_active Abandoned
- 2010-11-05 WO PCT/US2010/055586 patent/WO2011057054A1/en not_active Ceased
- 2010-11-05 CN CN201510296816.8A patent/CN105037326A/zh active Pending
- 2010-11-05 BR BR112012010792A patent/BR112012010792A2/pt not_active IP Right Cessation
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- 2010-11-05 EA EA201270562A patent/EA022323B1/ru not_active IP Right Cessation
- 2010-11-05 KR KR1020127014706A patent/KR20120102688A/ko not_active Ceased
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- 2010-11-05 CN CN201080050242.1A patent/CN102666491B/zh not_active Expired - Fee Related
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