JP2017508795A5 - - Google Patents
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- Publication number
- JP2017508795A5 JP2017508795A5 JP2016573682A JP2016573682A JP2017508795A5 JP 2017508795 A5 JP2017508795 A5 JP 2017508795A5 JP 2016573682 A JP2016573682 A JP 2016573682A JP 2016573682 A JP2016573682 A JP 2016573682A JP 2017508795 A5 JP2017508795 A5 JP 2017508795A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- independently selected
- independently
- haloalkyl
- substituted
- 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 43
- 125000003545 alkoxy group Chemical group 0.000 claims 17
- 229910052736 halogen Inorganic materials 0.000 claims 17
- 150000002367 halogens Chemical class 0.000 claims 15
- 229910052799 carbon Inorganic materials 0.000 claims 14
- 150000001875 compounds Chemical class 0.000 claims 12
- 125000004765 (C1-C4) haloalkyl group Chemical group 0.000 claims 10
- 125000004767 (C1-C4) haloalkoxy group Chemical group 0.000 claims 8
- 125000001183 hydrocarbyl group Chemical group 0.000 claims 8
- 229910052739 hydrogen Inorganic materials 0.000 claims 8
- 229910052760 oxygen Inorganic materials 0.000 claims 8
- 229910052717 sulfur Inorganic materials 0.000 claims 8
- 102100025271 2-acylglycerol O-acyltransferase 2 Human genes 0.000 claims 6
- 150000001721 carbon Chemical group 0.000 claims 6
- 229910052731 fluorine Inorganic materials 0.000 claims 6
- 125000005842 heteroatom Chemical group 0.000 claims 6
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 5
- 125000000623 heterocyclic group Chemical group 0.000 claims 5
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 5
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims 4
- 125000004432 carbon atom Chemical group C* 0.000 claims 4
- 125000001188 haloalkyl group Chemical group 0.000 claims 4
- 208000008338 non-alcoholic fatty liver disease Diseases 0.000 claims 4
- 239000008194 pharmaceutical composition Substances 0.000 claims 4
- 229920006395 saturated elastomer Polymers 0.000 claims 4
- 125000000171 (C1-C6) haloalkyl group Chemical group 0.000 claims 3
- 125000006645 (C3-C4) cycloalkyl group Chemical group 0.000 claims 3
- 101710186725 2-acylglycerol O-acyltransferase 2 Proteins 0.000 claims 3
- 102000015779 HDL Lipoproteins Human genes 0.000 claims 3
- 108010010234 HDL Lipoproteins Proteins 0.000 claims 3
- 101000577113 Homo sapiens 2-acylglycerol O-acyltransferase 2 Proteins 0.000 claims 3
- 102000007330 LDL Lipoproteins Human genes 0.000 claims 3
- 108010007622 LDL Lipoproteins Proteins 0.000 claims 3
- 238000003556 assay Methods 0.000 claims 3
- 125000004438 haloalkoxy group Chemical group 0.000 claims 3
- 238000004895 liquid chromatography mass spectrometry Methods 0.000 claims 3
- 150000003839 salts Chemical class 0.000 claims 3
- 239000012453 solvate Substances 0.000 claims 3
- 125000003831 tetrazolyl group Chemical group 0.000 claims 3
- 125000006648 (C1-C8) haloalkyl group Chemical group 0.000 claims 2
- 125000006570 (C5-C6) heteroaryl group Chemical group 0.000 claims 2
- 125000004008 6 membered carbocyclic group Chemical group 0.000 claims 2
- 102100025012 Dipeptidyl peptidase 4 Human genes 0.000 claims 2
- 101000930822 Giardia intestinalis Dipeptidyl-peptidase 4 Proteins 0.000 claims 2
- -1 OBn Chemical group 0.000 claims 2
- 125000004414 alkyl thio group Chemical group 0.000 claims 2
- HVYWMOMLDIMFJA-DPAQBDIFSA-N cholesterol Chemical compound C1C=C2C[C@@H](O)CC[C@]2(C)[C@@H]2[C@@H]1[C@@H]1CC[C@H]([C@H](C)CCCC(C)C)[C@@]1(C)CC2 HVYWMOMLDIMFJA-DPAQBDIFSA-N 0.000 claims 2
- 201000010099 disease Diseases 0.000 claims 2
- 208000035475 disorder Diseases 0.000 claims 2
- 125000004995 haloalkylthio group Chemical group 0.000 claims 2
- 125000005843 halogen group Chemical group 0.000 claims 2
- 125000001072 heteroaryl group Chemical group 0.000 claims 2
- 208000031225 myocardial ischemia Diseases 0.000 claims 2
- 206010053219 non-alcoholic steatohepatitis Diseases 0.000 claims 2
- 125000004737 (C1-C6) haloalkoxy group Chemical group 0.000 claims 1
- 125000006569 (C5-C6) heterocyclic group Chemical group 0.000 claims 1
- 201000001320 Atherosclerosis Diseases 0.000 claims 1
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims 1
- 208000032928 Dyslipidaemia Diseases 0.000 claims 1
- 208000010412 Glaucoma Diseases 0.000 claims 1
- 208000002705 Glucose Intolerance Diseases 0.000 claims 1
- 101001094079 Homo sapiens Sodium- and chloride-dependent GABA transporter 2 Proteins 0.000 claims 1
- 206010060378 Hyperinsulinaemia Diseases 0.000 claims 1
- 208000031226 Hyperlipidaemia Diseases 0.000 claims 1
- 206010020772 Hypertension Diseases 0.000 claims 1
- 206010022489 Insulin Resistance Diseases 0.000 claims 1
- 208000017170 Lipid metabolism disease Diseases 0.000 claims 1
- 208000001145 Metabolic Syndrome Diseases 0.000 claims 1
- 208000008589 Obesity Diseases 0.000 claims 1
- 208000017442 Retinal disease Diseases 0.000 claims 1
- 206010038923 Retinopathy Diseases 0.000 claims 1
- 102100035242 Sodium- and chloride-dependent GABA transporter 2 Human genes 0.000 claims 1
- 208000006011 Stroke Diseases 0.000 claims 1
- 208000007536 Thrombosis Diseases 0.000 claims 1
- 201000000690 abdominal obesity-metabolic syndrome Diseases 0.000 claims 1
- 230000002159 abnormal effect Effects 0.000 claims 1
- 125000006367 bivalent amino carbonyl group Chemical group [H]N([*:1])C([*:2])=O 0.000 claims 1
- 125000006297 carbonyl amino group Chemical group [H]N([*:2])C([*:1])=O 0.000 claims 1
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims 1
- 235000012000 cholesterol Nutrition 0.000 claims 1
- 125000000392 cycloalkenyl group Chemical group 0.000 claims 1
- 230000003111 delayed effect Effects 0.000 claims 1
- 206010012601 diabetes mellitus Diseases 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 230000000694 effects Effects 0.000 claims 1
- 208000004104 gestational diabetes Diseases 0.000 claims 1
- 230000004217 heart function Effects 0.000 claims 1
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 1
- 201000001421 hyperglycemia Diseases 0.000 claims 1
- 230000003451 hyperinsulinaemic effect Effects 0.000 claims 1
- 201000008980 hyperinsulinism Diseases 0.000 claims 1
- 208000006575 hypertriglyceridemia Diseases 0.000 claims 1
- 239000003112 inhibitor Substances 0.000 claims 1
- 208000017169 kidney disease Diseases 0.000 claims 1
- 201000006370 kidney failure Diseases 0.000 claims 1
- 150000002632 lipids Chemical class 0.000 claims 1
- 201000001119 neuropathy Diseases 0.000 claims 1
- 230000007823 neuropathy Effects 0.000 claims 1
- 235000020824 obesity Nutrition 0.000 claims 1
- 208000033808 peripheral neuropathy Diseases 0.000 claims 1
- 201000009104 prediabetes syndrome Diseases 0.000 claims 1
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 1
- 125000003226 pyrazolyl group Chemical group 0.000 claims 1
- 125000004076 pyridyl group Chemical group 0.000 claims 1
- 125000000714 pyrimidinyl group Chemical group 0.000 claims 1
- 125000000168 pyrrolyl group Chemical group 0.000 claims 1
- 125000000335 thiazolyl group Chemical group 0.000 claims 1
- 125000001544 thienyl group Chemical group 0.000 claims 1
- 208000001072 type 2 diabetes mellitus Diseases 0.000 claims 1
- 230000029663 wound healing Effects 0.000 claims 1
- 0 CC(*)(C(C)(N1)I)C(C2=CC=CC=CC=CC=C2)=C(*)C1=O Chemical compound CC(*)(C(C)(N1)I)C(C2=CC=CC=CC=CC=C2)=C(*)C1=O 0.000 description 7
- ZGBILICFVRCTND-UHFFFAOYSA-N CC1=CN=CC=CC1 Chemical compound CC1=CN=CC=CC1 ZGBILICFVRCTND-UHFFFAOYSA-N 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201461949506P | 2014-03-07 | 2014-03-07 | |
| US61/949,506 | 2014-03-07 | ||
| PCT/US2015/018874 WO2015134701A1 (en) | 2014-03-07 | 2015-03-05 | Dihydropyridinone mgat2 inhibitors for use in the treatment of metabolic disorders |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2017508795A JP2017508795A (ja) | 2017-03-30 |
| JP2017508795A5 true JP2017508795A5 (enExample) | 2018-03-22 |
| JP6498705B2 JP6498705B2 (ja) | 2019-04-10 |
Family
ID=52686514
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2016573682A Expired - Fee Related JP6498705B2 (ja) | 2014-03-07 | 2015-03-05 | 代謝障害の治療に用いるためのジヒドロピリジノンｍｇａｔ２阻害剤 |
Country Status (13)
| Country | Link |
|---|---|
| US (2) | US9701672B2 (enExample) |
| EP (1) | EP3114121B1 (enExample) |
| JP (1) | JP6498705B2 (enExample) |
| KR (1) | KR20160120790A (enExample) |
| CN (1) | CN106068265B (enExample) |
| AU (1) | AU2015227142A1 (enExample) |
| CA (1) | CA2941955A1 (enExample) |
| EA (1) | EA201691600A1 (enExample) |
| ES (1) | ES2700574T3 (enExample) |
| IL (1) | IL247589A0 (enExample) |
| MX (1) | MX2016011105A (enExample) |
| SG (1) | SG11201607392SA (enExample) |
| WO (1) | WO2015134701A1 (enExample) |
Families Citing this family (11)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US8791091B2 (en) | 2011-12-02 | 2014-07-29 | Bristol-Myers Squibb Company | Aryl dihydropyridinone and piperidinone MGAT2 inhibitors |
| PT3114120T (pt) | 2014-03-07 | 2019-05-08 | Bristol Myers Squibb Co | Inibidores de mgat2 di-hidropiridinona tetrazolonasubstituída |
| WO2015191681A2 (en) | 2014-06-11 | 2015-12-17 | Bristol-Myers Squibb Company | Substituted pyridinones as mgat2 inhibitors |
| WO2017069224A1 (ja) * | 2015-10-22 | 2017-04-27 | 塩野義製薬株式会社 | Ｍｇａｔ２阻害活性を有するスピロ環誘導体 |
| JPWO2017110841A1 (ja) | 2015-12-21 | 2018-10-11 | 塩野義製薬株式会社 | Ｍｇａｔ２阻害活性を有する非芳香族複素環誘導体 |
| WO2017172368A1 (en) | 2016-03-31 | 2017-10-05 | Oncternal Therapeutics, Inc. | Indoline analogs and uses thereof |
| JP2020158390A (ja) * | 2017-06-20 | 2020-10-01 | 塩野義製薬株式会社 | Ｍｇａｔ２阻害活性を有する非芳香族複素環誘導体およびそれらを含有する医薬組成物 |
| TWI782056B (zh) | 2017-07-14 | 2022-11-01 | 日商鹽野義製藥股份有限公司 | 具有ｍｇａｔ２抑制活性的縮合環衍生物 |
| MX2021008050A (es) | 2019-01-11 | 2021-08-05 | Shionogi & Co | Derivado de dihidropirazolopirazinona que tiene actividad inhibidora de monoacilglicerol aciltransferasa 2 (mgat2). |
| JP7068743B2 (ja) * | 2019-01-11 | 2022-05-17 | 塩野義製薬株式会社 | Ｍｇａｔ２阻害活性を有する縮合環誘導体を含有する医薬組成物 |
| CN112194659A (zh) | 2019-07-08 | 2021-01-08 | 浙江海正药业股份有限公司 | 炔类衍生物及其制备方法和用途 |
Family Cites Families (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5614492A (en) | 1986-05-05 | 1997-03-25 | The General Hospital Corporation | Insulinotropic hormone GLP-1 (7-36) and uses thereof |
| ATE396731T1 (de) | 2003-03-25 | 2008-06-15 | Vertex Pharma | Thiazole zur verwendung als inhibitoren von protein-kinasen |
| JPWO2008038768A1 (ja) | 2006-09-28 | 2010-01-28 | 大日本住友製薬株式会社 | 二環性ピリミジン構造を有する化合物及びそれを含有する医薬組成物 |
| US8791091B2 (en) | 2011-12-02 | 2014-07-29 | Bristol-Myers Squibb Company | Aryl dihydropyridinone and piperidinone MGAT2 inhibitors |
| US9073856B2 (en) * | 2012-01-23 | 2015-07-07 | Eli Lilly And Company | Phenyl methanesulfonamide derivatives useful as MGAT-2 inhibitors |
| US9365558B2 (en) * | 2013-05-29 | 2016-06-14 | Bristol-Myers Squibb Company | Dihydropyridinone MGAT2 inhibitors |
-
2015
- 2015-03-05 EA EA201691600A patent/EA201691600A1/ru unknown
- 2015-03-05 AU AU2015227142A patent/AU2015227142A1/en not_active Abandoned
- 2015-03-05 EP EP15710687.3A patent/EP3114121B1/en not_active Not-in-force
- 2015-03-05 KR KR1020167027386A patent/KR20160120790A/ko not_active Ceased
- 2015-03-05 CA CA2941955A patent/CA2941955A1/en not_active Abandoned
- 2015-03-05 SG SG11201607392SA patent/SG11201607392SA/en unknown
- 2015-03-05 US US15/123,791 patent/US9701672B2/en active Active
- 2015-03-05 WO PCT/US2015/018874 patent/WO2015134701A1/en not_active Ceased
- 2015-03-05 JP JP2016573682A patent/JP6498705B2/ja not_active Expired - Fee Related
- 2015-03-05 MX MX2016011105A patent/MX2016011105A/es unknown
- 2015-03-05 ES ES15710687T patent/ES2700574T3/es active Active
- 2015-03-05 CN CN201580012205.4A patent/CN106068265B/zh not_active Expired - Fee Related
-
2016
- 2016-09-01 IL IL247589A patent/IL247589A0/en unknown
-
2017
- 2017-06-08 US US15/617,079 patent/US9856244B2/en active Active