JP2010533726A5 - - Google Patents
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- Publication number
- JP2010533726A5 JP2010533726A5 JP2010517122A JP2010517122A JP2010533726A5 JP 2010533726 A5 JP2010533726 A5 JP 2010533726A5 JP 2010517122 A JP2010517122 A JP 2010517122A JP 2010517122 A JP2010517122 A JP 2010517122A JP 2010533726 A5 JP2010533726 A5 JP 2010533726A5
- Authority
- JP
- Japan
- Prior art keywords
- aryl
- cycloalkyl
- alkyl
- heterocyclyl
- alkenyl
- 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
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- 125000000753 cycloalkyl group Chemical group 0.000 claims 257
- 125000003118 aryl group Chemical group 0.000 claims 250
- 125000000217 alkyl group Chemical group 0.000 claims 224
- 125000000623 heterocyclic group Chemical group 0.000 claims 208
- 125000003342 alkenyl group Chemical group 0.000 claims 152
- 125000000304 alkynyl group Chemical group 0.000 claims 143
- 125000001072 heteroaryl group Chemical group 0.000 claims 141
- 125000004415 heterocyclylalkyl group Chemical group 0.000 claims 134
- 125000003710 aryl alkyl group Chemical group 0.000 claims 104
- 125000004446 heteroarylalkyl group Chemical group 0.000 claims 98
- 125000004093 cyano group Chemical group *C#N 0.000 claims 91
- 125000001475 halogen functional group Chemical group 0.000 claims 91
- 125000001188 haloalkyl group Chemical group 0.000 claims 77
- 125000001316 cycloalkyl alkyl group Chemical group 0.000 claims 76
- 229910052739 hydrogen Inorganic materials 0.000 claims 71
- 239000001257 hydrogen Substances 0.000 claims 71
- 150000002431 hydrogen Chemical class 0.000 claims 66
- -1 —NH 2 Chemical group 0.000 claims 63
- 125000003545 alkoxy group Chemical group 0.000 claims 17
- 150000001875 compounds Chemical class 0.000 claims 14
- 125000002950 monocyclic group Chemical group 0.000 claims 14
- 239000003795 chemical substances by application Substances 0.000 claims 6
- 239000003814 drug Substances 0.000 claims 6
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 5
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 5
- 229940124597 therapeutic agent Drugs 0.000 claims 5
- 208000035475 disorder Diseases 0.000 claims 3
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 3
- 102000016622 Dipeptidyl Peptidase 4 Human genes 0.000 claims 2
- 101000930822 Giardia intestinalis Dipeptidyl-peptidase 4 Proteins 0.000 claims 2
- 206010060378 Hyperinsulinaemia Diseases 0.000 claims 2
- 208000017170 Lipid metabolism disease Diseases 0.000 claims 2
- 208000017442 Retinal disease Diseases 0.000 claims 2
- 206010038923 Retinopathy Diseases 0.000 claims 2
- 230000005856 abnormality Effects 0.000 claims 2
- 239000003472 antidiabetic agent Substances 0.000 claims 2
- 201000010099 disease Diseases 0.000 claims 2
- 201000008980 hyperinsulinism Diseases 0.000 claims 2
- 208000017169 kidney disease Diseases 0.000 claims 2
- 230000037356 lipid metabolism Effects 0.000 claims 2
- 208000031225 myocardial ischemia Diseases 0.000 claims 2
- 239000008194 pharmaceutical composition Substances 0.000 claims 2
- 125000004076 pyridyl group Chemical group 0.000 claims 2
- 125000000714 pyrimidinyl group Chemical group 0.000 claims 2
- HBAQYPYDRFILMT-UHFFFAOYSA-N 8-[3-(1-cyclopropylpyrazol-4-yl)-1H-pyrazolo[4,3-d]pyrimidin-5-yl]-3-methyl-3,8-diazabicyclo[3.2.1]octan-2-one Chemical class C1(CC1)N1N=CC(=C1)C1=NNC2=C1N=C(N=C2)N1C2C(N(CC1CC2)C)=O HBAQYPYDRFILMT-UHFFFAOYSA-N 0.000 claims 1
- 201000001320 Atherosclerosis Diseases 0.000 claims 1
- 208000020084 Bone disease Diseases 0.000 claims 1
- 208000028698 Cognitive impairment Diseases 0.000 claims 1
- 208000035473 Communicable disease Diseases 0.000 claims 1
- 206010012289 Dementia Diseases 0.000 claims 1
- 208000010412 Glaucoma Diseases 0.000 claims 1
- 208000002705 Glucose Intolerance Diseases 0.000 claims 1
- 108010010369 HIV Protease Proteins 0.000 claims 1
- 206010019280 Heart failures Diseases 0.000 claims 1
- 208000035150 Hypercholesterolemia 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
- 206010024604 Lipoatrophy Diseases 0.000 claims 1
- 208000001145 Metabolic Syndrome Diseases 0.000 claims 1
- 206010028980 Neoplasm Diseases 0.000 claims 1
- 208000008589 Obesity Diseases 0.000 claims 1
- 206010033645 Pancreatitis Diseases 0.000 claims 1
- 208000005764 Peripheral Arterial Disease Diseases 0.000 claims 1
- 208000006011 Stroke Diseases 0.000 claims 1
- 201000000690 abdominal obesity-metabolic syndrome Diseases 0.000 claims 1
- 230000002159 abnormal effect Effects 0.000 claims 1
- 239000013543 active substance Substances 0.000 claims 1
- 230000000879 anti-atherosclerotic effect Effects 0.000 claims 1
- 230000000326 anti-hypercholesterolaemic effect Effects 0.000 claims 1
- 230000001315 anti-hyperlipaemic effect Effects 0.000 claims 1
- 230000003276 anti-hypertensive effect Effects 0.000 claims 1
- 230000001346 anti-hypertriglyceridemic effect Effects 0.000 claims 1
- 229940121363 anti-inflammatory agent Drugs 0.000 claims 1
- 239000002260 anti-inflammatory agent Substances 0.000 claims 1
- 230000003063 anti-neuropathic effect Effects 0.000 claims 1
- 230000003579 anti-obesity Effects 0.000 claims 1
- 230000002769 anti-restenotic effect Effects 0.000 claims 1
- 229940125708 antidiabetic agent Drugs 0.000 claims 1
- 239000003524 antilipemic agent Substances 0.000 claims 1
- 239000002830 appetite depressant Substances 0.000 claims 1
- 239000008280 blood Substances 0.000 claims 1
- 210000004369 blood Anatomy 0.000 claims 1
- 201000011510 cancer Diseases 0.000 claims 1
- 208000010877 cognitive disease Diseases 0.000 claims 1
- 230000003111 delayed effect Effects 0.000 claims 1
- 206010012601 diabetes mellitus Diseases 0.000 claims 1
- 229940079593 drug Drugs 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 230000000694 effects Effects 0.000 claims 1
- 230000004217 heart function Effects 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
- 239000003112 inhibitor Substances 0.000 claims 1
- 150000002632 lipids Chemical class 0.000 claims 1
- 230000004770 neurodegeneration Effects 0.000 claims 1
- 208000015122 neurodegenerative disease 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
- 230000002265 prevention Effects 0.000 claims 1
- 102000004169 proteins and genes Human genes 0.000 claims 1
- 108090000623 proteins and genes Proteins 0.000 claims 1
- 125000003373 pyrazinyl group Chemical group 0.000 claims 1
- 208000037803 restenosis Diseases 0.000 claims 1
- 150000003839 salts Chemical class 0.000 claims 1
- 239000012453 solvate Substances 0.000 claims 1
- 208000001072 type 2 diabetes mellitus Diseases 0.000 claims 1
- 230000002792 vascular Effects 0.000 claims 1
- 230000029663 wound healing Effects 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US95016207P | 2007-07-17 | 2007-07-17 | |
| US60/950,162 | 2007-07-17 | ||
| PCT/US2008/070101 WO2009012275A1 (en) | 2007-07-17 | 2008-07-16 | Pyridone gpr119 g protein-coupled receptor agonists |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2013144778A Division JP2013237680A (ja) | 2007-07-17 | 2013-07-10 | ピリドンｇｐｒ１１９ｇタンパク質共役受容体アゴニスト |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2010533726A JP2010533726A (ja) | 2010-10-28 |
| JP2010533726A5 true JP2010533726A5 (enExample) | 2011-02-24 |
| JP5318867B2 JP5318867B2 (ja) | 2013-10-16 |
Family
ID=39864683
Family Applications (3)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2010517123A Expired - Fee Related JP5301539B2 (ja) | 2007-07-17 | 2008-07-16 | Ｇｐｒ１１９ｇタンパク質共役受容体の調節方法および選択された化合物 |
| JP2010517122A Expired - Fee Related JP5318867B2 (ja) | 2007-07-17 | 2008-07-16 | ピリドンｇｐｒ１１９ｇタンパク質共役受容体アゴニスト |
| JP2013144778A Withdrawn JP2013237680A (ja) | 2007-07-17 | 2013-07-10 | ピリドンｇｐｒ１１９ｇタンパク質共役受容体アゴニスト |
Family Applications Before (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2010517123A Expired - Fee Related JP5301539B2 (ja) | 2007-07-17 | 2008-07-16 | Ｇｐｒ１１９ｇタンパク質共役受容体の調節方法および選択された化合物 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2013144778A Withdrawn JP2013237680A (ja) | 2007-07-17 | 2013-07-10 | ピリドンｇｐｒ１１９ｇタンパク質共役受容体アゴニスト |
Country Status (26)
| Country | Link |
|---|---|
| US (6) | US7928230B2 (enExample) |
| EP (2) | EP2170864B1 (enExample) |
| JP (3) | JP5301539B2 (enExample) |
| KR (2) | KR20100045471A (enExample) |
| CN (3) | CN103550218A (enExample) |
| AR (2) | AR067569A1 (enExample) |
| AT (2) | ATE524460T1 (enExample) |
| AU (2) | AU2008276055B2 (enExample) |
| BR (2) | BRPI0814428A2 (enExample) |
| CA (2) | CA2693439A1 (enExample) |
| CL (2) | CL2008002110A1 (enExample) |
| CO (1) | CO6160315A2 (enExample) |
| CY (2) | CY1112151T1 (enExample) |
| DK (2) | DK2173737T3 (enExample) |
| EA (2) | EA018709B1 (enExample) |
| ES (2) | ES2371515T3 (enExample) |
| HR (2) | HRP20110806T1 (enExample) |
| IL (1) | IL228120A0 (enExample) |
| NZ (2) | NZ582661A (enExample) |
| PE (2) | PE20090888A1 (enExample) |
| PL (2) | PL2170864T3 (enExample) |
| PT (2) | PT2173737E (enExample) |
| SI (2) | SI2170864T1 (enExample) |
| TW (2) | TW200904440A (enExample) |
| WO (2) | WO2009012277A1 (enExample) |
| ZA (2) | ZA201000151B (enExample) |
Families Citing this family (52)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AU2005310467B2 (en) * | 2004-12-01 | 2011-06-23 | Msd K.K. | Substituted pyridone derivative |
| PE20090222A1 (es) | 2007-05-04 | 2009-03-27 | Bristol Myers Squibb Co | Compuestos [6,6] y [6,7]-biciclicos como agonistas del receptor acoplado a la proteina g gpr119 |
| EP2170864B1 (en) | 2007-07-17 | 2011-09-14 | Bristol-Myers Squibb Company | Pyridone gpr119 g protein-coupled receptor agonists |
| EP2146210A1 (en) | 2008-04-07 | 2010-01-20 | Arena Pharmaceuticals, Inc. | Methods of using A G protein-coupled receptor to identify peptide YY (PYY) secretagogues and compounds useful in the treatment of conditions modulated by PYY |
| CA3034994A1 (en) | 2008-06-03 | 2009-12-10 | Intermune, Inc. | Substituted aryl-2 pyridone compounds and use thereof for treating inflammatory and fibrotic disorders |
| TW201006821A (en) * | 2008-07-16 | 2010-02-16 | Bristol Myers Squibb Co | Pyridone and pyridazone analogues as GPR119 modulators |
| AU2009270984A1 (en) * | 2008-07-16 | 2010-01-21 | Schering Corporation | Bicyclic Heterocycle Derivatives and methods of use thereof |
| CN102159572A (zh) * | 2008-07-16 | 2011-08-17 | 先灵公司 | 双环杂环衍生物及其作为gpr 119调节剂的用途 |
| GB0904287D0 (en) | 2009-03-12 | 2009-04-22 | Prosidion Ltd | Compounds for the treatment of metabolic disorders |
| EP2408780A2 (en) * | 2009-03-20 | 2012-01-25 | Pfizer Inc. | 3-oxa-7-azabicycloý3.3.1¨nonanes |
| US8293729B2 (en) | 2009-06-24 | 2012-10-23 | Boehringer Ingelheim International Gmbh | Compounds, pharmaceutical composition and methods relating thereto |
| EP2445901A1 (en) | 2009-06-24 | 2012-05-02 | Boehringer Ingelheim International GmbH | New compounds, pharmaceutical composition and methods relating thereto |
| WO2011107494A1 (de) | 2010-03-03 | 2011-09-09 | Sanofi | Neue aromatische glykosidderivate, diese verbindungen enthaltende arzneimittel und deren verwendung |
| JP2013522279A (ja) | 2010-03-18 | 2013-06-13 | 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 | 糖尿病及び関連状態の治療で用いるｇｐｒ１１９作動薬とｄｄｐ−ｉｖ阻害薬リナグリプチンの組合せ |
| BR112012025590A2 (pt) | 2010-04-08 | 2016-06-21 | Bristol Myers Squibb Co | análogos de pirimidinilpiperidiniloxipiridinona como moduladores de gpr119 |
| EA201270778A1 (ru) | 2010-05-06 | 2013-04-30 | Бристол-Майерс Сквибб Компани | Бициклические гетероарильные аналоги в качестве модуляторов рецептора gpr119 |
| US8729084B2 (en) | 2010-05-06 | 2014-05-20 | Bristol-Myers Squibb Company | Benzofuranyl analogues as GPR119 modulators |
| US8530413B2 (en) | 2010-06-21 | 2013-09-10 | Sanofi | Heterocyclically substituted methoxyphenyl derivatives with an oxo group, processes for preparation thereof and use thereof as medicaments |
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| TW201215387A (en) | 2010-07-05 | 2012-04-16 | Sanofi Aventis | Spirocyclically substituted 1,3-propane dioxide derivatives, processes for preparation thereof and use thereof as a medicament |
| PH12013500671A1 (en) | 2010-10-08 | 2018-04-11 | Cadila Healthcare Ltd | Novel gpr 119 agonists |
| US9359300B2 (en) | 2010-12-06 | 2016-06-07 | Confluence Life Sciences, Inc. | Methyl/difluorophenyl-methoxy substituted pyridinone-pyridinyl compounds, methyl-pyridinyl-methoxy substituted pyridinone-pyridinyl compounds, and methyl-pyrimidinyl-methoxy substituted pyridinone-pyridinyl compounds |
| EP2648516B1 (en) | 2010-12-06 | 2018-09-05 | Aclaris Therapeutics, Inc. | Substituted pyridinone-pyridinyl compounds |
| WO2012123449A1 (en) * | 2011-03-14 | 2012-09-20 | Boehringer Ingelheim International Gmbh | N- cyclopropyl - n- piperidinylbenzamides as gpr119 modulators |
| ES2602813T3 (es) | 2011-06-09 | 2017-02-22 | Rhizen Pharmaceuticals S.A. | Nuevos compuestos como moduladores de GPR-119 |
| WO2013037390A1 (en) | 2011-09-12 | 2013-03-21 | Sanofi | 6-(4-hydroxy-phenyl)-3-styryl-1h-pyrazolo[3,4-b]pyridine-4-carboxylic acid amide derivatives as kinase inhibitors |
| WO2013045413A1 (en) | 2011-09-27 | 2013-04-04 | Sanofi | 6-(4-hydroxy-phenyl)-3-alkyl-1h-pyrazolo[3,4-b]pyridine-4-carboxylic acid amide derivatives as kinase inhibitors |
| WO2013173198A1 (en) | 2012-05-16 | 2013-11-21 | Bristol-Myers Squibb Company | Pyrimidinylpiperidinyloxypyridone analogues as gpr119 modulators |
| CA2878625A1 (en) | 2012-07-11 | 2014-01-16 | Elcelyx Therapeutics, Inc. | Compositions comprising statins, biguanides and further agents for reducing cardiometabolic risk |
| AR092742A1 (es) | 2012-10-02 | 2015-04-29 | Intermune Inc | Piridinonas antifibroticas |
| US9695148B2 (en) * | 2012-11-13 | 2017-07-04 | Nissan Chemical Industries, Ltd. | 2-pyridone compound |
| CN102993088A (zh) * | 2012-12-31 | 2013-03-27 | 东华大学 | 一种4-羟基-2-吡啶酮的制备方法 |
| TW201444849A (zh) | 2013-03-13 | 2014-12-01 | Janssen Pharmaceutica Nv | 經取代的7-氮雜雙環類及其作為食慾激素受體調節劑之用途 |
| TW201444821A (zh) | 2013-03-13 | 2014-12-01 | Janssen Pharmaceutica Nv | 經取代之哌啶化合物及其作為食慾素受體調節劑之用途 |
| TWI621618B (zh) | 2013-03-13 | 2018-04-21 | 比利時商健生藥品公司 | 經取代２－氮雜雙環類及其作為食慾素受體調控劑之用途 |
| JP6699909B2 (ja) | 2013-06-07 | 2020-05-27 | アクラリス セラピューティクス，インコーポレイテッド | メチル／フルオロ−ピリジニル−メトキシ置換ピリジノン−ピリジニル化合物及びフルオロ−ピリミジニル−メトキシ置換ピリジノン−ピリジニル化合物 |
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| ES2728531T3 (es) | 2013-07-08 | 2019-10-25 | Bayer Cropscience Ag | Derivados de arilsulfuro y arilsulfóxido de seis miembros enlazados con C-N como agentes para combatir parásitos |
| CA2943363A1 (en) | 2014-04-02 | 2015-10-08 | Intermune, Inc. | Anti-fibrotic pyridinones |
| EP2929883A1 (en) | 2014-04-08 | 2015-10-14 | Institut Pasteur | Pyrazole derivatives as dihydroorotate dehydrogenase (DHODH) inhibitors |
| US9611262B2 (en) | 2014-09-11 | 2017-04-04 | Janssen Pharmaceutica Nv | Substituted 2-azabicycles and their use as orexin receptor modulators |
| WO2016130652A1 (en) | 2015-02-10 | 2016-08-18 | Vanderbilt University | Negative allosteric modulators of metabotropic glutamate receptor 3 |
| JP6578116B2 (ja) * | 2015-03-25 | 2019-09-18 | 公益財団法人相模中央化学研究所 | 一置換（フルオロアルキル）エチレン類及びその製造方法 |
| US10865194B2 (en) | 2017-11-03 | 2020-12-15 | Fondazione Istituto Italiano Di Tecnologia | Therapeutically active bicyclic-sulphonamides and pharmaceutical compositions |
| CN115667277A (zh) | 2020-02-28 | 2023-01-31 | 卡尔优普公司 | Gpr40激动剂 |
| PH12022552263A1 (en) | 2020-03-27 | 2023-11-13 | Aclaris Therapeutics Inc | Oral compositions of mk2 pathway inhibitor for treatment of immune conditions |
| UY39222A (es) | 2020-05-19 | 2021-11-30 | Kallyope Inc | Activadores de la ampk |
| CA3183575A1 (en) | 2020-06-26 | 2021-12-30 | Iyassu Sebhat | Ampk activators |
| WO2022081573A1 (en) * | 2020-10-12 | 2022-04-21 | University Of Tennessee Research Foundation | Transient receptor potential canonical 3 inhibitors and methods of use thereof |
| CN115504927A (zh) * | 2022-08-15 | 2022-12-23 | 广西中医药大学 | 4-甲基-2-对甲苯基-6-羰基吡啶-3-甲酸及其制备方法和用途 |
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