JP2009542717A5 - - Google Patents
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- Publication number
- JP2009542717A5 JP2009542717A5 JP2009518610A JP2009518610A JP2009542717A5 JP 2009542717 A5 JP2009542717 A5 JP 2009542717A5 JP 2009518610 A JP2009518610 A JP 2009518610A JP 2009518610 A JP2009518610 A JP 2009518610A JP 2009542717 A5 JP2009542717 A5 JP 2009542717A5
- Authority
- JP
- Japan
- Prior art keywords
- group
- compound
- heteroaryl
- drug
- alkyl
- 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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- 150000001875 compounds Chemical class 0.000 claims 13
- 239000003814 drug Substances 0.000 claims 10
- 125000001072 heteroaryl group Chemical group 0.000 claims 9
- 125000000217 alkyl group Chemical group 0.000 claims 8
- 229940079593 drug Drugs 0.000 claims 8
- 125000003118 aryl group Chemical group 0.000 claims 6
- 229910052739 hydrogen Inorganic materials 0.000 claims 5
- 239000001257 hydrogen Substances 0.000 claims 5
- 208000031226 Hyperlipidaemia Diseases 0.000 claims 3
- 125000004450 alkenylene group Chemical group 0.000 claims 3
- 125000002947 alkylene group Chemical group 0.000 claims 3
- 239000003795 chemical substances by application Substances 0.000 claims 3
- 238000010276 construction Methods 0.000 claims 3
- 125000000753 cycloalkyl group Chemical group 0.000 claims 3
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 3
- 150000002431 hydrogen Chemical class 0.000 claims 3
- 229910052760 oxygen Inorganic materials 0.000 claims 3
- 150000003839 salts Chemical class 0.000 claims 3
- 229910052717 sulfur Inorganic materials 0.000 claims 3
- 201000001320 Atherosclerosis Diseases 0.000 claims 2
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 2
- 208000035150 Hypercholesterolemia Diseases 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
- 229910005965 SO 2 Inorganic materials 0.000 claims 2
- 230000002253 anti-ischaemic effect Effects 0.000 claims 2
- 125000004432 carbon atom Chemical group C* 0.000 claims 2
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims 2
- 201000010099 disease Diseases 0.000 claims 2
- 230000003451 hyperinsulinaemic effect Effects 0.000 claims 2
- 201000008980 hyperinsulinism Diseases 0.000 claims 2
- 208000006575 hypertriglyceridemia Diseases 0.000 claims 2
- 201000001119 neuropathy Diseases 0.000 claims 2
- 230000007823 neuropathy Effects 0.000 claims 2
- -1 nitro, amino, cyano, methyl Chemical group 0.000 claims 2
- 208000033808 peripheral neuropathy Diseases 0.000 claims 2
- 208000037803 restenosis Diseases 0.000 claims 2
- 229940124597 therapeutic agent Drugs 0.000 claims 2
- 208000001072 type 2 diabetes mellitus Diseases 0.000 claims 2
- 208000020084 Bone disease Diseases 0.000 claims 1
- 208000028698 Cognitive impairment Diseases 0.000 claims 1
- 206010012289 Dementia Diseases 0.000 claims 1
- 208000032928 Dyslipidaemia Diseases 0.000 claims 1
- PXGOKWXKJXAPGV-UHFFFAOYSA-N Fluorine Chemical compound FF PXGOKWXKJXAPGV-UHFFFAOYSA-N 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
- 206010020772 Hypertension Diseases 0.000 claims 1
- 206010022489 Insulin Resistance Diseases 0.000 claims 1
- 206010049287 Lipodystrophy acquired 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
- 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
- 125000003342 alkenyl group Chemical group 0.000 claims 1
- 125000003545 alkoxy group Chemical group 0.000 claims 1
- 125000000304 alkynyl group Chemical group 0.000 claims 1
- 125000004103 aminoalkyl group Chemical group 0.000 claims 1
- 125000005001 aminoaryl group Chemical group 0.000 claims 1
- 125000005214 aminoheteroaryl group Chemical group 0.000 claims 1
- 230000003178 anti-diabetic effect Effects 0.000 claims 1
- 230000002924 anti-infective effect Effects 0.000 claims 1
- 230000003579 anti-obesity Effects 0.000 claims 1
- 239000003472 antidiabetic agent Substances 0.000 claims 1
- 239000002220 antihypertensive agent Substances 0.000 claims 1
- 229940127088 antihypertensive drug Drugs 0.000 claims 1
- 239000002246 antineoplastic agent Substances 0.000 claims 1
- 229940041181 antineoplastic drug Drugs 0.000 claims 1
- 239000002830 appetite depressant Substances 0.000 claims 1
- 125000003710 aryl alkyl group Chemical group 0.000 claims 1
- 125000004429 atom Chemical group 0.000 claims 1
- 201000011510 cancer Diseases 0.000 claims 1
- 229910052799 carbon Inorganic materials 0.000 claims 1
- 208000010877 cognitive disease Diseases 0.000 claims 1
- 230000001149 cognitive effect Effects 0.000 claims 1
- 231100000433 cytotoxic Toxicity 0.000 claims 1
- 230000001472 cytotoxic effect Effects 0.000 claims 1
- 230000003111 delayed effect Effects 0.000 claims 1
- 206010012601 diabetes mellitus Diseases 0.000 claims 1
- 208000035475 disorder Diseases 0.000 claims 1
- 150000002148 esters Chemical class 0.000 claims 1
- 229910052731 fluorine Inorganic materials 0.000 claims 1
- 239000011737 fluorine Substances 0.000 claims 1
- 229940124828 glucokinase activator Drugs 0.000 claims 1
- 229910052736 halogen Inorganic materials 0.000 claims 1
- 125000005843 halogen group Chemical group 0.000 claims 1
- 150000002367 halogens Chemical class 0.000 claims 1
- 230000004217 heart function Effects 0.000 claims 1
- 125000004446 heteroarylalkyl group Chemical group 0.000 claims 1
- 125000000623 heterocyclic group Chemical group 0.000 claims 1
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 1
- 201000001421 hyperglycemia Diseases 0.000 claims 1
- 230000002218 hypoglycaemic effect Effects 0.000 claims 1
- 208000015181 infectious disease Diseases 0.000 claims 1
- 208000028867 ischemia Diseases 0.000 claims 1
- 210000003734 kidney Anatomy 0.000 claims 1
- 208000017169 kidney disease Diseases 0.000 claims 1
- 150000002632 lipids Chemical class 0.000 claims 1
- 208000006132 lipodystrophy Diseases 0.000 claims 1
- 239000003695 memory enhancer Substances 0.000 claims 1
- 125000004170 methylsulfonyl group Chemical group [H]C([H])([H])S(*)(=O)=O 0.000 claims 1
- 208000031225 myocardial ischemia Diseases 0.000 claims 1
- 230000004770 neurodegeneration Effects 0.000 claims 1
- 208000015122 neurodegenerative disease Diseases 0.000 claims 1
- 229910052757 nitrogen Inorganic materials 0.000 claims 1
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 1
- 235000020824 obesity Nutrition 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 201000009104 prediabetes syndrome Diseases 0.000 claims 1
- 230000002265 prevention Effects 0.000 claims 1
- 230000003449 preventive effect Effects 0.000 claims 1
- 229940002612 prodrug Drugs 0.000 claims 1
- 239000000651 prodrug Substances 0.000 claims 1
- 125000001424 substituent group Chemical group 0.000 claims 1
- 230000001225 therapeutic effect Effects 0.000 claims 1
- 238000002560 therapeutic procedure Methods 0.000 claims 1
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims 1
- 230000002792 vascular Effects 0.000 claims 1
- 230000029663 wound healing Effects 0.000 claims 1
- 0 CCC(*)c1c[n]c(C(*)CC)s1 Chemical compound CCC(*)c1c[n]c(C(*)CC)s1 0.000 description 7
- IOHHAJXQSHWGPW-UHFFFAOYSA-N CC(C1)(CC2)C1CP2=O Chemical compound CC(C1)(CC2)C1CP2=O IOHHAJXQSHWGPW-UHFFFAOYSA-N 0.000 description 1
- OYUDYQMFVRHPIY-UHFFFAOYSA-N CCOP(C[n](cc1)nc1NC(c1cc(Oc2ncc(C(N3CCC3)=O)nc2)cc(OC(C)C)c1)=O)(OCC)=O Chemical compound CCOP(C[n](cc1)nc1NC(c1cc(Oc2ncc(C(N3CCC3)=O)nc2)cc(OC(C)C)c1)=O)(OCC)=O OYUDYQMFVRHPIY-UHFFFAOYSA-N 0.000 description 1
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US81891206P | 2006-07-06 | 2006-07-06 | |
| US60/818,912 | 2006-07-06 | ||
| US11/769,964 | 2007-06-28 | ||
| US11/769,964 US7910747B2 (en) | 2006-07-06 | 2007-06-28 | Phosphonate and phosphinate pyrazolylamide glucokinase activators |
| PCT/US2007/072708 WO2008005964A2 (en) | 2006-07-06 | 2007-07-03 | Phosphonate and phosphinate compounds as glucokinase activators |
Related Child Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2012204939A Division JP5460799B2 (ja) | 2006-07-06 | 2012-09-18 | グルコキナーゼ活性化薬としてのホスホン酸およびホスフィン酸エステル化合物 |
| JP2012204945A Division JP5460800B2 (ja) | 2006-07-06 | 2012-09-18 | グルコキナーゼ活性化薬としてのホスホン酸およびホスフィン酸エステル化合物 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2009542717A JP2009542717A (ja) | 2009-12-03 |
| JP2009542717A5 true JP2009542717A5 (enExample) | 2010-03-18 |
| JP5361714B2 JP5361714B2 (ja) | 2013-12-04 |
Family
ID=38720453
Family Applications (3)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2009518610A Expired - Fee Related JP5361714B2 (ja) | 2006-07-06 | 2007-07-03 | グルコキナーゼ活性化薬としてのホスホン酸およびホスフィン酸エステル化合物 |
| JP2012204939A Expired - Fee Related JP5460799B2 (ja) | 2006-07-06 | 2012-09-18 | グルコキナーゼ活性化薬としてのホスホン酸およびホスフィン酸エステル化合物 |
| JP2012204945A Expired - Fee Related JP5460800B2 (ja) | 2006-07-06 | 2012-09-18 | グルコキナーゼ活性化薬としてのホスホン酸およびホスフィン酸エステル化合物 |
Family Applications After (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2012204939A Expired - Fee Related JP5460799B2 (ja) | 2006-07-06 | 2012-09-18 | グルコキナーゼ活性化薬としてのホスホン酸およびホスフィン酸エステル化合物 |
| JP2012204945A Expired - Fee Related JP5460800B2 (ja) | 2006-07-06 | 2012-09-18 | グルコキナーゼ活性化薬としてのホスホン酸およびホスフィン酸エステル化合物 |
Country Status (20)
| Country | Link |
|---|---|
| US (3) | US7910747B2 (enExample) |
| EP (1) | EP2059522B1 (enExample) |
| JP (3) | JP5361714B2 (enExample) |
| KR (1) | KR101375406B1 (enExample) |
| AR (1) | AR061858A1 (enExample) |
| AU (1) | AU2007269171B2 (enExample) |
| BR (1) | BRPI0713929A2 (enExample) |
| CA (1) | CA2658001C (enExample) |
| CL (1) | CL2007001994A1 (enExample) |
| CO (1) | CO6390122A2 (enExample) |
| EA (1) | EA015228B1 (enExample) |
| ES (1) | ES2449572T3 (enExample) |
| IL (1) | IL196226A (enExample) |
| MX (1) | MX2008016514A (enExample) |
| NO (1) | NO20085160L (enExample) |
| NZ (1) | NZ573734A (enExample) |
| PE (1) | PE20081001A1 (enExample) |
| SG (1) | SG173358A1 (enExample) |
| TW (1) | TWI418558B (enExample) |
| WO (1) | WO2008005964A2 (enExample) |
Families Citing this family (50)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CA2656618C (en) | 2006-07-06 | 2014-08-26 | Array Biopharma Inc. | Cyclopenta [d] pyrimidines as akt protein kinase inhibitors |
| EP2054418B1 (en) | 2006-07-06 | 2011-11-09 | Array Biopharma Inc. | Dihydrothieno pyrimidines as akt protein kinase inhibitors |
| US7910747B2 (en) * | 2006-07-06 | 2011-03-22 | Bristol-Myers Squibb Company | Phosphonate and phosphinate pyrazolylamide glucokinase activators |
| DE602007011628D1 (de) | 2006-07-06 | 2011-02-10 | Array Biopharma Inc | Dihydrofuropyrimidine als akt-proteinkinaseinhibitoren |
| US8063050B2 (en) | 2006-07-06 | 2011-11-22 | Array Biopharma Inc. | Hydroxylated and methoxylated pyrimidyl cyclopentanes as AKT protein kinase inhibitors |
| TW200831081A (en) * | 2006-12-25 | 2008-08-01 | Kyorin Seiyaku Kk | Glucokinase activator |
| CN101687800B (zh) * | 2007-03-07 | 2012-03-21 | 杏林制药株式会社 | 葡糖激酶活化物质 |
| WO2008154563A1 (en) * | 2007-06-11 | 2008-12-18 | Bristol-Myers Squibb Company | 1, 3 - dihydroxy substituted phenylamide glucokinase activators |
| ES2533557T3 (es) | 2007-07-05 | 2015-04-13 | Array Biopharma, Inc. | Pirimidil ciclopentanos como inhibidores de proteína cinasa AKT |
| AR067413A1 (es) | 2007-07-05 | 2009-10-07 | Genentech Inc | Compuestos heterociclicos que contienen ciclopenta[d]pirimidina inhibidores de proteinquinasas akt, composiciones farmaceuticas que los contienen, metodo de preparacion y uso de las mismas para el tratamiento de enfermedades hiperproliferativas, tales como cancer |
| US9409886B2 (en) | 2007-07-05 | 2016-08-09 | Array Biopharma Inc. | Pyrimidyl cyclopentanes as AKT protein kinase inhibitors |
| US8846683B2 (en) | 2007-07-05 | 2014-09-30 | Array Biopharma, Inc. | Pyrimidyl cyclopentanes as Akt protein kinase inhibitors |
| CA2695583A1 (en) * | 2007-08-13 | 2009-02-19 | Metabasis Therapeutics, Inc. | Novel activators of glucokinase |
| EP2025674A1 (de) | 2007-08-15 | 2009-02-18 | sanofi-aventis | Substituierte Tetrahydronaphthaline, Verfahren zu ihrer Herstellung und ihre Verwendung als Arzneimittel |
| MX2010007546A (es) | 2008-01-09 | 2010-09-30 | Array Biopharma Inc | Pirimidil ciclopentanos hidroxilados en forma de inhibidores de akt proteína quinasa. |
| WO2009089459A1 (en) | 2008-01-09 | 2009-07-16 | Array Biopharma Inc. | Hydroxylated pyrimidyl cyclopentanes as akt protein kinase inhibitors |
| AU2009205070A1 (en) | 2008-01-18 | 2009-07-23 | Astellas Pharma Inc. | Phenyl acetamide derivative |
| US7741327B2 (en) | 2008-04-16 | 2010-06-22 | Hoffmann-La Roche Inc. | Pyrrolidinone glucokinase activators |
| MY163114A (en) * | 2008-04-28 | 2017-08-15 | Kyorin Seiyaku Kk | Cyclopentylacrylamide derivative |
| TWI445707B (zh) | 2008-05-16 | 2014-07-21 | Takeda California Inc | 葡萄糖激酶活化劑 |
| WO2010107610A1 (en) * | 2009-03-17 | 2010-09-23 | Merck Sharp & Dohme Corp. | Method for treatment of diabetes and related conditions with combination therapy and compositions containing such compounds |
| US20110021570A1 (en) | 2009-07-23 | 2011-01-27 | Nancy-Ellen Haynes | Pyridone glucokinase activators |
| WO2011107494A1 (de) | 2010-03-03 | 2011-09-09 | Sanofi | Neue aromatische glykosidderivate, diese verbindungen enthaltende arzneimittel und deren verwendung |
| JP5909482B2 (ja) | 2010-03-31 | 2016-04-26 | ザ スクリプス リサーチ インスティテュート | 細胞の再プログラム |
| ES2559209T3 (es) * | 2010-04-14 | 2016-02-11 | Bristol-Myers Squibb Company | Nuevos activadores de la glucocinasa y métodos de uso de los mismos |
| US8178689B2 (en) | 2010-06-17 | 2012-05-15 | Hoffman-La Roche Inc. | Tricyclic compounds |
| EP2582709B1 (de) | 2010-06-18 | 2018-01-24 | Sanofi | Azolopyridin-3-on-derivate als inhibitoren von lipasen und phospholipasen |
| 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 |
| TW201215388A (en) | 2010-07-05 | 2012-04-16 | Sanofi Sa | (2-aryloxyacetylamino)phenylpropionic acid derivatives, processes for preparation thereof and use thereof as medicaments |
| 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 |
| TW201221505A (en) | 2010-07-05 | 2012-06-01 | Sanofi Sa | Aryloxyalkylene-substituted hydroxyphenylhexynoic acids, process for preparation thereof and use thereof as a medicament |
| JP2013544787A (ja) | 2010-10-13 | 2013-12-19 | タケダ カリフォルニア インコーポレイテッド | アザインダゾール誘導体の調製方法 |
| CN103841975A (zh) | 2011-04-01 | 2014-06-04 | 基因泰克公司 | Akt抑制剂化合物和厄洛替尼的组合以及使用方法 |
| CN103841976A (zh) | 2011-04-01 | 2014-06-04 | 基因泰克公司 | Akt和mek抑制剂化合物的组合及其使用方法 |
| 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 |
| KR20140092721A (ko) * | 2013-01-16 | 2014-07-24 | 주식회사유한양행 | 신규의 헤테로아릴을 포함하는 페녹시벤즈아마이드 글루코키나제 활성화제 및 그의 제조방법 |
| PL3828173T3 (pl) | 2014-03-07 | 2022-12-19 | Biocryst Pharmaceuticals, Inc. | Podstawiane pirazole jako inhibitory ludzkiej kalikreiny osoczowej |
| TWI656121B (zh) | 2014-08-04 | 2019-04-11 | 德商拜耳製藥公司 | ２－（嗎啉－４－基）－１，７－萘啶 |
| US20170327457A1 (en) | 2014-09-09 | 2017-11-16 | Bristol-Myers Squibb Company | Phenyl-(aza)cycloalkyl carboxylic acid gpr120 modulators |
| CN106632298B (zh) * | 2015-11-03 | 2021-06-01 | 上海科胜药物研发有限公司 | 一种泰地唑胺的制备方法及其中间体 |
| WO2018017910A1 (en) | 2016-07-22 | 2018-01-25 | Bristol-Myers Squibb Company | Glucokinase activators and methods of using same |
| GB201714777D0 (en) | 2017-09-14 | 2017-11-01 | Univ London Queen Mary | Agent |
| DK3804716T3 (da) * | 2018-05-31 | 2025-03-03 | Hua Medicine Shanghai Ltd | Farmaceutisk kombination, sammensætning og kombinationspræparat omfattende glucokinase-aktivator og sglt-2-inhibitor og fremgangsmåder til fremstilling og anvendelser deraf |
| WO2020016335A1 (en) | 2018-07-19 | 2020-01-23 | Astrazeneca Ab | Methods of treating hfpef employing dapagliflozin and compositions comprising the same |
| TW202220672A (zh) | 2020-07-27 | 2022-06-01 | 瑞典商阿斯特捷利康公司 | 用達格列淨治療慢性腎臟病之方法 |
| SI4188389T1 (sl) | 2020-07-27 | 2025-11-28 | Astrazeneca Ab | Dapagliflozin za uporabo pri postopkih zdravljenja kronične ledvične bolezni |
| CN113461635A (zh) * | 2021-07-07 | 2021-10-01 | 上海毕得医药科技股份有限公司 | 4-（2-氯乙基）噻唑-2-羧酸乙酯及其制备方法和应用 |
| US20250108065A1 (en) | 2022-01-26 | 2025-04-03 | Astrazeneca Ab | Methods of treating prediabetes or reducing the risk of developing type 2 diabetes with dapagliflozin |
| CN120202188A (zh) | 2022-11-15 | 2025-06-24 | 日本农药株式会社 | 酰胺化合物或其盐、含有所述化合物的用于农业和园艺的杀菌剂、及其使用方法 |
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| GB0218014D0 (en) | 2002-08-02 | 2002-09-11 | Eisai London Res Lab Ltd | Process |
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