JP2016520128A5 - - Google Patents
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- Publication number
- JP2016520128A5 JP2016520128A5 JP2016516749A JP2016516749A JP2016520128A5 JP 2016520128 A5 JP2016520128 A5 JP 2016520128A5 JP 2016516749 A JP2016516749 A JP 2016516749A JP 2016516749 A JP2016516749 A JP 2016516749A JP 2016520128 A5 JP2016520128 A5 JP 2016520128A5
- 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 38
- 125000003545 alkoxy group Chemical group 0.000 claims 19
- 125000004765 (C1-C4) haloalkyl group Chemical group 0.000 claims 18
- 229910052736 halogen Inorganic materials 0.000 claims 18
- 150000002367 halogens Chemical class 0.000 claims 17
- 125000001183 hydrocarbyl group Chemical group 0.000 claims 16
- 125000004767 (C1-C4) haloalkoxy group Chemical group 0.000 claims 13
- 239000003795 chemical substances by application Substances 0.000 claims 11
- 150000003839 salts Chemical class 0.000 claims 11
- 239000012453 solvate Substances 0.000 claims 11
- 150000001875 compounds Chemical class 0.000 claims 10
- 229920006395 saturated elastomer Polymers 0.000 claims 9
- 229910052799 carbon Inorganic materials 0.000 claims 8
- 229910052739 hydrogen Inorganic materials 0.000 claims 8
- 239000003814 drug Substances 0.000 claims 7
- 229910052731 fluorine Inorganic materials 0.000 claims 6
- 229910052760 oxygen Inorganic materials 0.000 claims 6
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 6
- 229910052717 sulfur Inorganic materials 0.000 claims 6
- 125000005842 heteroatom Chemical group 0.000 claims 5
- 125000000623 heterocyclic group Chemical group 0.000 claims 5
- 125000006645 (C3-C4) cycloalkyl group Chemical group 0.000 claims 4
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims 4
- 150000001721 carbon Chemical group 0.000 claims 4
- 125000004432 carbon atom Chemical group C* 0.000 claims 4
- 125000005843 halogen group Chemical group 0.000 claims 4
- 208000008338 non-alcoholic fatty liver disease Diseases 0.000 claims 4
- 229940124597 therapeutic agent Drugs 0.000 claims 4
- 125000006648 (C1-C8) haloalkyl group Chemical group 0.000 claims 3
- 125000004438 haloalkoxy group Chemical group 0.000 claims 3
- 125000001188 haloalkyl group Chemical group 0.000 claims 3
- 239000008194 pharmaceutical composition Substances 0.000 claims 3
- 125000000171 (C1-C6) haloalkyl group Chemical group 0.000 claims 2
- 125000006570 (C5-C6) heteroaryl group Chemical group 0.000 claims 2
- 206010060378 Hyperinsulinaemia Diseases 0.000 claims 2
- 208000031226 Hyperlipidaemia Diseases 0.000 claims 2
- 208000017442 Retinal disease Diseases 0.000 claims 2
- 206010038923 Retinopathy Diseases 0.000 claims 2
- 239000003472 antidiabetic agent Substances 0.000 claims 2
- 239000003524 antilipemic agent Substances 0.000 claims 2
- 230000036528 appetite Effects 0.000 claims 2
- 235000019789 appetite Nutrition 0.000 claims 2
- 125000000051 benzyloxy group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])O* 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
- 125000001072 heteroaryl group Chemical group 0.000 claims 2
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 2
- 201000008980 hyperinsulinism Diseases 0.000 claims 2
- 239000003112 inhibitor Substances 0.000 claims 2
- 208000017169 kidney disease Diseases 0.000 claims 2
- 206010053219 non-alcoholic steatohepatitis Diseases 0.000 claims 2
- 102000004169 proteins and genes Human genes 0.000 claims 2
- 108090000623 proteins and genes Proteins 0.000 claims 2
- 125000003226 pyrazolyl group Chemical group 0.000 claims 2
- 125000000335 thiazolyl group Chemical group 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
- 125000004008 6 membered carbocyclic 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
- 229940124213 Dipeptidyl peptidase 4 (DPP IV) inhibitor Drugs 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
- 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
- 229940127322 Sodium-Glucose Transporter 2 Inhibitors Drugs 0.000 claims 1
- 208000006011 Stroke Diseases 0.000 claims 1
- 201000000690 abdominal obesity-metabolic syndrome Diseases 0.000 claims 1
- 125000004414 alkyl thio group Chemical group 0.000 claims 1
- 230000000879 anti-atherosclerotic effect Effects 0.000 claims 1
- 230000001708 anti-dyslipidemic effect Effects 0.000 claims 1
- 230000002253 anti-ischaemic effect Effects 0.000 claims 1
- 230000003063 anti-neuropathic effect Effects 0.000 claims 1
- 239000000883 anti-obesity agent Substances 0.000 claims 1
- 229940125708 antidiabetic agent Drugs 0.000 claims 1
- 239000002220 antihypertensive agent Substances 0.000 claims 1
- 229940030600 antihypertensive agent Drugs 0.000 claims 1
- 229940125710 antiobesity agent Drugs 0.000 claims 1
- 125000004429 atom Chemical group 0.000 claims 1
- 125000002837 carbocyclic group Chemical group 0.000 claims 1
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims 1
- 230000000747 cardiac effect Effects 0.000 claims 1
- 235000012000 cholesterol Nutrition 0.000 claims 1
- 125000000392 cycloalkenyl group Chemical group 0.000 claims 1
- 125000000753 cycloalkyl group Chemical group 0.000 claims 1
- 230000003111 delayed effect Effects 0.000 claims 1
- 206010012601 diabetes mellitus Diseases 0.000 claims 1
- 239000003603 dipeptidyl peptidase IV inhibitor Substances 0.000 claims 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 1
- 208000035475 disorder Diseases 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 230000004064 dysfunction Effects 0.000 claims 1
- 208000004104 gestational diabetes Diseases 0.000 claims 1
- 125000004995 haloalkylthio group Chemical group 0.000 claims 1
- 201000001421 hyperglycemia Diseases 0.000 claims 1
- 230000003451 hyperinsulinaemic effect Effects 0.000 claims 1
- 208000006575 hypertriglyceridemia Diseases 0.000 claims 1
- 208000028867 ischemia Diseases 0.000 claims 1
- 150000002632 lipids Chemical class 0.000 claims 1
- 208000031225 myocardial ischemia Diseases 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
- 125000004076 pyridyl group Chemical group 0.000 claims 1
- 125000003831 tetrazolyl 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 *C1=S*C=C1 Chemical compound *C1=S*C=C1 0.000 description 2
- PLIPMCBHIKAKDR-UHFFFAOYSA-N Cc(cc1)n[n]1[Re] Chemical compound Cc(cc1)n[n]1[Re] PLIPMCBHIKAKDR-UHFFFAOYSA-N 0.000 description 1
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201361828219P | 2013-05-29 | 2013-05-29 | |
| US61/828,219 | 2013-05-29 | ||
| US201461982574P | 2014-04-22 | 2014-04-22 | |
| US61/982,574 | 2014-04-22 | ||
| PCT/US2014/039661 WO2014193884A1 (en) | 2013-05-29 | 2014-05-28 | Dihydropyridinone mgat2 inhibitors |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2016520128A JP2016520128A (ja) | 2016-07-11 |
| JP2016520128A5 true JP2016520128A5 (enExample) | 2017-07-06 |
| JP6417405B2 JP6417405B2 (ja) | 2018-11-07 |
Family
ID=50983206
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2016516749A Expired - Fee Related JP6417405B2 (ja) | 2013-05-29 | 2014-05-28 | ジヒドロピリジノンｍｇａｔ２阻害剤 |
Country Status (14)
| Country | Link |
|---|---|
| US (3) | US9365558B2 (enExample) |
| EP (1) | EP3004059B1 (enExample) |
| JP (1) | JP6417405B2 (enExample) |
| KR (1) | KR102291444B1 (enExample) |
| CN (1) | CN105339350B (enExample) |
| AU (1) | AU2014274354A1 (enExample) |
| BR (1) | BR112015029598A2 (enExample) |
| CA (1) | CA2913913A1 (enExample) |
| EA (1) | EA201592268A1 (enExample) |
| IL (1) | IL242803A0 (enExample) |
| MX (1) | MX2015015562A (enExample) |
| SG (1) | SG11201509070YA (enExample) |
| TW (1) | TW201534585A (enExample) |
| WO (1) | WO2014193884A1 (enExample) |
Families Citing this family (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| MY176921A (en) | 2014-03-07 | 2020-08-26 | Bristol Myers Squibb Co | Tetrazolone-substituted dihydropyridinone mgat2 inhibitors |
| MX2016011105A (es) | 2014-03-07 | 2016-12-12 | Bristol Myers Squibb Co | Inhibidores de monoacilglicerol aciltransferasa 2 (mgat2) de dihidropiridinona para usarse en el tratamiento de trastornos metabolicos. |
| ES2666569T3 (es) | 2014-06-11 | 2018-05-07 | Bristol-Myers Squibb Company | Piridinonas sustituidas como inhibidores de MGAT2 |
| 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 |
| 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 |
| JP7608166B2 (ja) | 2019-01-11 | 2025-01-06 | 塩野義製薬株式会社 | Ｍｇａｔ２阻害活性を有するジヒドロピラゾロピラジノン誘導体 |
| WO2021132577A1 (ja) * | 2019-12-27 | 2021-07-01 | 日本たばこ産業株式会社 | アシルスルファミド化合物及びその医薬用途 |
| CN118215478A (zh) * | 2021-09-08 | 2024-06-18 | 盐野义制药株式会社 | 用于预防和治疗与抗肥胖作用有关的疾病的药物 |
Family Cites Families (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP3996657B2 (ja) * | 1995-05-31 | 2007-10-24 | 大日本住友製薬株式会社 | 新規ナフチリジン誘導体 |
| US8344132B2 (en) * | 2005-06-22 | 2013-01-01 | BioCryst Pharmaceticals, Inc. | Methods for the preparation of 9-deazapurine derivatives |
| US8324385B2 (en) * | 2008-10-30 | 2012-12-04 | Madrigal Pharmaceuticals, Inc. | Diacylglycerol acyltransferase inhibitors |
| US20110275647A1 (en) * | 2009-02-23 | 2011-11-10 | Msd K.K. | Pyrimidin-4-(3h)-one derivatives |
| US8791091B2 (en) | 2011-12-02 | 2014-07-29 | Bristol-Myers Squibb Company | Aryl dihydropyridinone and piperidinone MGAT2 inhibitors |
-
2014
- 2014-05-28 JP JP2016516749A patent/JP6417405B2/ja not_active Expired - Fee Related
- 2014-05-28 CN CN201480029460.5A patent/CN105339350B/zh not_active Expired - Fee Related
- 2014-05-28 BR BR112015029598A patent/BR112015029598A2/pt not_active IP Right Cessation
- 2014-05-28 WO PCT/US2014/039661 patent/WO2014193884A1/en not_active Ceased
- 2014-05-28 SG SG11201509070YA patent/SG11201509070YA/en unknown
- 2014-05-28 EP EP14732767.0A patent/EP3004059B1/en not_active Not-in-force
- 2014-05-28 US US14/288,422 patent/US9365558B2/en active Active
- 2014-05-28 KR KR1020157036367A patent/KR102291444B1/ko not_active Expired - Fee Related
- 2014-05-28 TW TW103118681A patent/TW201534585A/zh unknown
- 2014-05-28 CA CA2913913A patent/CA2913913A1/en not_active Abandoned
- 2014-05-28 AU AU2014274354A patent/AU2014274354A1/en not_active Abandoned
- 2014-05-28 MX MX2015015562A patent/MX2015015562A/es unknown
- 2014-05-28 EA EA201592268A patent/EA201592268A1/ru unknown
-
2015
- 2015-11-26 IL IL242803A patent/IL242803A0/en unknown
-
2016
- 2016-05-13 US US15/154,210 patent/US20160256445A1/en not_active Abandoned
-
2017
- 2017-06-09 US US15/618,182 patent/US9822074B2/en active Active