JP2013544805A5 - - Google Patents
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- Publication number
- JP2013544805A5 JP2013544805A5 JP2013536709A JP2013536709A JP2013544805A5 JP 2013544805 A5 JP2013544805 A5 JP 2013544805A5 JP 2013536709 A JP2013536709 A JP 2013536709A JP 2013536709 A JP2013536709 A JP 2013536709A JP 2013544805 A5 JP2013544805 A5 JP 2013544805A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- independently
- substituted
- halogen
- het
- 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 50
- 229910052736 halogen Inorganic materials 0.000 claims 42
- 150000002367 halogens Chemical class 0.000 claims 42
- 150000001875 compounds Chemical class 0.000 claims 27
- 125000001072 heteroaryl group Chemical group 0.000 claims 12
- 125000001424 substituent group Chemical group 0.000 claims 12
- 125000004093 cyano group Chemical group *C#N 0.000 claims 11
- 125000005842 heteroatom Chemical group 0.000 claims 11
- 150000003839 salts Chemical class 0.000 claims 11
- 229910052717 sulfur Inorganic materials 0.000 claims 10
- 125000000753 cycloalkyl group Chemical group 0.000 claims 9
- RAXXELZNTBOGNW-UHFFFAOYSA-N imidazole Natural products C1=CNC=N1 RAXXELZNTBOGNW-UHFFFAOYSA-N 0.000 claims 9
- 229910052760 oxygen Inorganic materials 0.000 claims 8
- 125000002618 bicyclic heterocycle group Chemical group 0.000 claims 6
- 125000002911 monocyclic heterocycle group Chemical group 0.000 claims 6
- 229910052799 carbon Inorganic materials 0.000 claims 5
- 239000008194 pharmaceutical composition Substances 0.000 claims 5
- RWRDLPDLKQPQOW-UHFFFAOYSA-N Pyrrolidine Chemical compound C1CCNC1 RWRDLPDLKQPQOW-UHFFFAOYSA-N 0.000 claims 4
- 229910052739 hydrogen Inorganic materials 0.000 claims 4
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 4
- 201000001320 Atherosclerosis Diseases 0.000 claims 3
- YNAVUWVOSKDBBP-UHFFFAOYSA-N Morpholine Chemical compound C1COCCN1 YNAVUWVOSKDBBP-UHFFFAOYSA-N 0.000 claims 3
- 125000002915 carbonyl group Chemical group [*:2]C([*:1])=O 0.000 claims 3
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims 3
- YLQBMQCUIZJEEH-UHFFFAOYSA-N Furan Chemical compound C=1C=COC=1 YLQBMQCUIZJEEH-UHFFFAOYSA-N 0.000 claims 2
- 108010007622 LDL Lipoproteins Proteins 0.000 claims 2
- 102000007330 LDL Lipoproteins Human genes 0.000 claims 2
- 102100031545 Microsomal triglyceride transfer protein large subunit Human genes 0.000 claims 2
- NQRYJNQNLNOLGT-UHFFFAOYSA-N Piperidine Chemical compound C1CCNCC1 NQRYJNQNLNOLGT-UHFFFAOYSA-N 0.000 claims 2
- KYQCOXFCLRTKLS-UHFFFAOYSA-N Pyrazine Chemical compound C1=CN=CC=N1 KYQCOXFCLRTKLS-UHFFFAOYSA-N 0.000 claims 2
- WTKZEGDFNFYCGP-UHFFFAOYSA-N Pyrazole Chemical compound C=1C=NNC=1 WTKZEGDFNFYCGP-UHFFFAOYSA-N 0.000 claims 2
- JUJWROOIHBZHMG-UHFFFAOYSA-N Pyridine Chemical compound C1=CC=NC=C1 JUJWROOIHBZHMG-UHFFFAOYSA-N 0.000 claims 2
- KAESVJOAVNADME-UHFFFAOYSA-N Pyrrole Chemical compound C=1C=CNC=1 KAESVJOAVNADME-UHFFFAOYSA-N 0.000 claims 2
- YTPLMLYBLZKORZ-UHFFFAOYSA-N Thiophene Chemical compound C=1C=CSC=1 YTPLMLYBLZKORZ-UHFFFAOYSA-N 0.000 claims 2
- RMRCNWBMXRMIRW-BYFNXCQMSA-M cyanocobalamin Chemical compound N#C[Co+]N([C@]1([H])[C@H](CC(N)=O)[C@]\2(CCC(=O)NC[C@H](C)OP(O)(=O)OC3[C@H]([C@H](O[C@@H]3CO)N3C4=CC(C)=C(C)C=C4N=C3)O)C)C/2=C(C)\C([C@H](C/2(C)C)CCC(N)=O)=N\C\2=C\C([C@H]([C@@]/2(CC(N)=O)C)CCC(N)=O)=N\C\2=C(C)/C2=N[C@]1(C)[C@@](C)(CC(N)=O)[C@@H]2CCC(N)=O RMRCNWBMXRMIRW-BYFNXCQMSA-M 0.000 claims 2
- 239000003937 drug carrier Substances 0.000 claims 2
- OVBPIULPVIDEAO-LBPRGKRZSA-N folic acid Chemical compound C=1N=C2NC(N)=NC(=O)C2=NC=1CNC1=CC=C(C(=O)N[C@@H](CCC(O)=O)C(O)=O)C=C1 OVBPIULPVIDEAO-LBPRGKRZSA-N 0.000 claims 2
- 239000003112 inhibitor Substances 0.000 claims 2
- 108010038232 microsomal triglyceride transfer protein Proteins 0.000 claims 2
- 229910052757 nitrogen Inorganic materials 0.000 claims 2
- HSINOMROUCMIEA-FGVHQWLLSA-N (2s,4r)-4-[(3r,5s,6r,7r,8s,9s,10s,13r,14s,17r)-6-ethyl-3,7-dihydroxy-10,13-dimethyl-2,3,4,5,6,7,8,9,11,12,14,15,16,17-tetradecahydro-1h-cyclopenta[a]phenanthren-17-yl]-2-methylpentanoic acid Chemical compound C([C@@]12C)C[C@@H](O)C[C@H]1[C@@H](CC)[C@@H](O)[C@@H]1[C@@H]2CC[C@]2(C)[C@@H]([C@H](C)C[C@H](C)C(O)=O)CC[C@H]21 HSINOMROUCMIEA-FGVHQWLLSA-N 0.000 claims 1
- 125000006645 (C3-C4) cycloalkyl group Chemical group 0.000 claims 1
- XGYCWCIGCYGQFU-UHFFFAOYSA-N 1,2-thiazolidine 1,1-dioxide Chemical compound O=S1(=O)CCCN1 XGYCWCIGCYGQFU-UHFFFAOYSA-N 0.000 claims 1
- 101150092476 ABCA1 gene Proteins 0.000 claims 1
- 102000018616 Apolipoproteins B Human genes 0.000 claims 1
- 108010027006 Apolipoproteins B Proteins 0.000 claims 1
- 229940122502 Cholesterol absorption inhibitor Drugs 0.000 claims 1
- 101000783577 Dendroaspis angusticeps Thrombostatin Proteins 0.000 claims 1
- 101000783578 Dendroaspis jamesoni kaimosae Dendroaspin Proteins 0.000 claims 1
- 208000032928 Dyslipidaemia Diseases 0.000 claims 1
- 108010023302 HDL Cholesterol Proteins 0.000 claims 1
- 229940121710 HMGCoA reductase inhibitor Drugs 0.000 claims 1
- 108010028554 LDL Cholesterol Proteins 0.000 claims 1
- 208000017170 Lipid metabolism disease Diseases 0.000 claims 1
- OVBPIULPVIDEAO-UHFFFAOYSA-N N-Pteroyl-L-glutaminsaeure Natural products C=1N=C2NC(N)=NC(=O)C2=NC=1CNC1=CC=C(C(=O)NC(CCC(O)=O)C(O)=O)C=C1 OVBPIULPVIDEAO-UHFFFAOYSA-N 0.000 claims 1
- PVNIIMVLHYAWGP-UHFFFAOYSA-N Niacin Chemical compound OC(=O)C1=CC=CN=C1 PVNIIMVLHYAWGP-UHFFFAOYSA-N 0.000 claims 1
- 102000023984 PPAR alpha Human genes 0.000 claims 1
- PCNDJXKNXGMECE-UHFFFAOYSA-N Phenazine Natural products C1=CC=CC2=NC3=CC=CC=C3N=C21 PCNDJXKNXGMECE-UHFFFAOYSA-N 0.000 claims 1
- 102000001494 Sterol O-Acyltransferase Human genes 0.000 claims 1
- 108010054082 Sterol O-acyltransferase Proteins 0.000 claims 1
- FZWLAAWBMGSTSO-UHFFFAOYSA-N Thiazole Chemical compound C1=CSC=N1 FZWLAAWBMGSTSO-UHFFFAOYSA-N 0.000 claims 1
- AUYYCJSJGJYCDS-LBPRGKRZSA-N Thyrolar Chemical class IC1=CC(C[C@H](N)C(O)=O)=CC(I)=C1OC1=CC=C(O)C(I)=C1 AUYYCJSJGJYCDS-LBPRGKRZSA-N 0.000 claims 1
- 229930003779 Vitamin B12 Natural products 0.000 claims 1
- 239000004480 active ingredient Substances 0.000 claims 1
- 125000002252 acyl group Chemical group 0.000 claims 1
- 239000000556 agonist Substances 0.000 claims 1
- 239000003963 antioxidant agent Substances 0.000 claims 1
- 230000003078 antioxidant effect Effects 0.000 claims 1
- 229940127218 antiplatelet drug Drugs 0.000 claims 1
- MNFORVFSTILPAW-UHFFFAOYSA-N azetidin-2-one Chemical compound O=C1CCN1 MNFORVFSTILPAW-UHFFFAOYSA-N 0.000 claims 1
- HONIICLYMWZJFZ-UHFFFAOYSA-N azetidine Chemical compound C1CNC1 HONIICLYMWZJFZ-UHFFFAOYSA-N 0.000 claims 1
- 239000003613 bile acid Substances 0.000 claims 1
- 108091022863 bile acid binding Proteins 0.000 claims 1
- 102000030904 bile acid binding Human genes 0.000 claims 1
- 239000003795 chemical substances by application Substances 0.000 claims 1
- AGVAZMGAQJOSFJ-WZHZPDAFSA-M cobalt(2+);[(2r,3s,4r,5s)-5-(5,6-dimethylbenzimidazol-1-yl)-4-hydroxy-2-(hydroxymethyl)oxolan-3-yl] [(2r)-1-[3-[(1r,2r,3r,4z,7s,9z,12s,13s,14z,17s,18s,19r)-2,13,18-tris(2-amino-2-oxoethyl)-7,12,17-tris(3-amino-3-oxopropyl)-3,5,8,8,13,15,18,19-octamethyl-2 Chemical compound [Co+2].N#[C-].[N-]([C@@H]1[C@H](CC(N)=O)[C@@]2(C)CCC(=O)NC[C@@H](C)OP(O)(=O)O[C@H]3[C@H]([C@H](O[C@@H]3CO)N3C4=CC(C)=C(C)C=C4N=C3)O)\C2=C(C)/C([C@H](C\2(C)C)CCC(N)=O)=N/C/2=C\C([C@H]([C@@]/2(CC(N)=O)C)CCC(N)=O)=N\C\2=C(C)/C2=N[C@]1(C)[C@@](C)(CC(N)=O)[C@@H]2CCC(N)=O AGVAZMGAQJOSFJ-WZHZPDAFSA-M 0.000 claims 1
- 235000000639 cyanocobalamin Nutrition 0.000 claims 1
- 239000011666 cyanocobalamin Substances 0.000 claims 1
- 229960002104 cyanocobalamin Drugs 0.000 claims 1
- 150000003950 cyclic amides Chemical group 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 150000002148 esters Chemical class 0.000 claims 1
- 229960000304 folic acid Drugs 0.000 claims 1
- 235000019152 folic acid Nutrition 0.000 claims 1
- 239000011724 folic acid Substances 0.000 claims 1
- 230000014509 gene expression Effects 0.000 claims 1
- 239000002471 hydroxymethylglutaryl coenzyme A reductase inhibitor Substances 0.000 claims 1
- 239000000411 inducer Substances 0.000 claims 1
- CTAPFRYPJLPFDF-UHFFFAOYSA-N isoxazole Chemical compound C=1C=NOC=1 CTAPFRYPJLPFDF-UHFFFAOYSA-N 0.000 claims 1
- 239000003446 ligand Substances 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 125000001570 methylene group Chemical group [H]C([H])([*:1])[*:2] 0.000 claims 1
- 230000003278 mimic effect Effects 0.000 claims 1
- 239000000203 mixture Substances 0.000 claims 1
- 229960003512 nicotinic acid Drugs 0.000 claims 1
- 235000001968 nicotinic acid Nutrition 0.000 claims 1
- 239000011664 nicotinic acid Substances 0.000 claims 1
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 1
- 108091008725 peroxisome proliferator-activated receptors alpha Proteins 0.000 claims 1
- 239000002530 phenolic antioxidant Substances 0.000 claims 1
- 239000000106 platelet aggregation inhibitor Substances 0.000 claims 1
- UMJSCPRVCHMLSP-UHFFFAOYSA-N pyridine Natural products COC1=CC=CN=C1 UMJSCPRVCHMLSP-UHFFFAOYSA-N 0.000 claims 1
- 239000002516 radical scavenger Substances 0.000 claims 1
- 108020003175 receptors Proteins 0.000 claims 1
- 102000005962 receptors Human genes 0.000 claims 1
- 230000028327 secretion Effects 0.000 claims 1
- 150000003536 tetrazoles Chemical class 0.000 claims 1
- 229930192474 thiophene Natural products 0.000 claims 1
- 239000005495 thyroid hormone Substances 0.000 claims 1
- 229940036555 thyroid hormone Drugs 0.000 claims 1
- 150000003852 triazoles Chemical class 0.000 claims 1
- 239000011782 vitamin Substances 0.000 claims 1
- 235000013343 vitamin Nutrition 0.000 claims 1
- 229940088594 vitamin Drugs 0.000 claims 1
- 229930003231 vitamin Natural products 0.000 claims 1
- 239000011715 vitamin B12 Substances 0.000 claims 1
- 235000019163 vitamin B12 Nutrition 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US40830810P | 2010-10-29 | 2010-10-29 | |
| US61/408,308 | 2010-10-29 | ||
| PCT/US2011/057584 WO2012058187A1 (en) | 2010-10-29 | 2011-10-25 | Cyclic amine substituted oxazolidinone cetp inhibitor |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2013544805A JP2013544805A (ja) | 2013-12-19 |
| JP2013544805A5 true JP2013544805A5 (https=) | 2014-12-11 |
| JP5852662B2 JP5852662B2 (ja) | 2016-02-03 |
Family
ID=45994352
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2013536709A Expired - Fee Related JP5852662B2 (ja) | 2010-10-29 | 2011-10-25 | 環状アミン置換されたオキサゾリジノン系ｃｅｔｐ阻害薬 |
Country Status (10)
| Country | Link |
|---|---|
| US (1) | US9221834B2 (https=) |
| EP (1) | EP2632269B1 (https=) |
| JP (1) | JP5852662B2 (https=) |
| CN (1) | CN103269592B (https=) |
| AR (1) | AR083579A1 (https=) |
| AU (1) | AU2011320665B2 (https=) |
| CA (1) | CA2814846A1 (https=) |
| ES (1) | ES2623759T3 (https=) |
| TW (1) | TW201305146A (https=) |
| WO (1) | WO2012058187A1 (https=) |
Families Citing this family (14)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JO3210B1 (ar) | 2011-10-28 | 2018-03-08 | Merck Sharp & Dohme | مثبط منصهر لبروتين نقل الكوليسترليستير اوكسازوليدينون ثمائي الحلقة |
| EP2844252B1 (en) * | 2012-05-02 | 2016-11-30 | Merck Sharp & Dohme Corp. | Cyclic amine substituted heterocyclic compounds as cetp inhibitors |
| WO2014012428A1 (zh) * | 2012-07-19 | 2014-01-23 | 上海恒瑞医药有限公司 | 噁唑烷酮类衍生物、其制备方法及其在医药上的应用 |
| CN102977044A (zh) * | 2012-11-26 | 2013-03-20 | 盛世泰科生物医药技术(苏州)有限公司 | 一种3-(4-甲氧基苯基)-异噁唑-5-羧酸的制备方法 |
| US9717714B2 (en) | 2012-12-19 | 2017-08-01 | Merck Sharp & Dohme Corp. | Spirocyclic CETP inhibitors |
| EP2934519B1 (en) | 2012-12-20 | 2021-05-12 | Merck Sharp & Dohme Corp. | Therapeutic thiazolidinone compounds |
| WO2014119947A1 (en) * | 2013-01-31 | 2014-08-07 | Chong Kun Dang Pharmaceutical Corp. | Biaryl- or heterocyclic biaryl-substituted cyclohexene derivative compounds as cetp inhibitors |
| WO2015017302A2 (en) | 2013-07-30 | 2015-02-05 | Merck Sharp & Dohme Corp. | Bicyclic ureas and thiadiazolidine-1,1-dioxides as cetp inhibitors |
| US9688630B2 (en) | 2013-10-10 | 2017-06-27 | Merck Sharp & Dohme Corp. | 3,3′-disubstituted indolines as inhibitors of cholesterol ester transfer protein |
| CN105814064A (zh) | 2013-12-17 | 2016-07-27 | 默沙东公司 | 作为胆固醇酯转运蛋白的抑制剂的稠合双环异噁唑啉类 |
| WO2016018729A1 (en) | 2014-07-29 | 2016-02-04 | Merck Sharp & Dohme Corp. | Monocyclic isoxazolines as inhibitors of cholesterol ester transfer protein |
| US10023519B2 (en) * | 2014-09-09 | 2018-07-17 | Bristol-Myers Squibb Company | Cyclobutane containing carboxylic acid GPR120 modulators |
| EP3322420B1 (en) | 2015-07-13 | 2021-12-29 | Merck Sharp & Dohme Corp. | Bicyclic heterocycles as inhibitors of cholesterol ester transfer protein |
| KR20200091395A (ko) * | 2017-09-27 | 2020-07-30 | 페도라 파마슈티칼스 인코포레이티드 | 디아자비시클로옥탄 유도체의 결정형 및 그의 제조 방법 |
Family Cites Families (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AU1856997A (en) | 1996-02-02 | 1997-08-22 | Merck & Co., Inc. | Method for raising hdl cholesterol levels |
| DOP2005000123A (es) | 2004-07-02 | 2011-07-15 | Merck Sharp & Dohme | Inhibidores de cetp |
| HN2005000340A (es) * | 2004-07-02 | 2009-11-06 | Merck Sharp & Dohme | Inhibidores de cetp |
| EP1971595B1 (en) | 2005-12-30 | 2013-10-16 | Merck Sharp & Dohme Corp. | Cetp inhibitors |
| EP1973889B1 (en) | 2005-12-30 | 2016-08-24 | Merck Sharp & Dohme Corp. | Cetp inhibitors |
| US7915271B2 (en) | 2005-12-30 | 2011-03-29 | Merck Sharp & Dohme Corp. | 1,3-oxazolidin-2-one derivatives useful as CETP inhibitors |
| WO2011028395A1 (en) * | 2009-08-24 | 2011-03-10 | Merck Sharp & Dohme Corp. | Pyridyl oxazolidinone cetp inhibitor |
| JO3210B1 (ar) | 2011-10-28 | 2018-03-08 | Merck Sharp & Dohme | مثبط منصهر لبروتين نقل الكوليسترليستير اوكسازوليدينون ثمائي الحلقة |
| EP2844252B1 (en) | 2012-05-02 | 2016-11-30 | Merck Sharp & Dohme Corp. | Cyclic amine substituted heterocyclic compounds as cetp inhibitors |
-
2011
- 2011-10-25 ES ES11836937.0T patent/ES2623759T3/es active Active
- 2011-10-25 CA CA2814846A patent/CA2814846A1/en not_active Abandoned
- 2011-10-25 WO PCT/US2011/057584 patent/WO2012058187A1/en not_active Ceased
- 2011-10-25 AU AU2011320665A patent/AU2011320665B2/en not_active Ceased
- 2011-10-25 EP EP11836937.0A patent/EP2632269B1/en active Active
- 2011-10-25 CN CN201180062829.9A patent/CN103269592B/zh not_active Expired - Fee Related
- 2011-10-25 JP JP2013536709A patent/JP5852662B2/ja not_active Expired - Fee Related
- 2011-10-25 US US13/881,896 patent/US9221834B2/en active Active
- 2011-10-27 AR ARP110103977A patent/AR083579A1/es not_active Application Discontinuation
- 2011-10-28 TW TW100139480A patent/TW201305146A/zh unknown
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