JP2010516715A5 - - Google Patents
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- Publication number
- JP2010516715A5 JP2010516715A5 JP2009546627A JP2009546627A JP2010516715A5 JP 2010516715 A5 JP2010516715 A5 JP 2010516715A5 JP 2009546627 A JP2009546627 A JP 2009546627A JP 2009546627 A JP2009546627 A JP 2009546627A JP 2010516715 A5 JP2010516715 A5 JP 2010516715A5
- Authority
- JP
- Japan
- Prior art keywords
- optionally substituted
- alkyl
- phenyl
- halogens
- halogen
- 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
- 229910052736 halogen Inorganic materials 0.000 claims 48
- 150000002367 halogens Chemical class 0.000 claims 44
- 125000000217 alkyl group Chemical group 0.000 claims 43
- 125000001424 substituent group Chemical group 0.000 claims 16
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 15
- 150000001875 compounds Chemical class 0.000 claims 13
- 150000003839 salts Chemical class 0.000 claims 9
- 125000005843 halogen group Chemical group 0.000 claims 4
- NOESYZHRGYRDHS-UHFFFAOYSA-N insulin Chemical compound N1C(=O)C(NC(=O)C(CCC(N)=O)NC(=O)C(CCC(O)=O)NC(=O)C(C(C)C)NC(=O)C(NC(=O)CN)C(C)CC)CSSCC(C(NC(CO)C(=O)NC(CC(C)C)C(=O)NC(CC=2C=CC(O)=CC=2)C(=O)NC(CCC(N)=O)C(=O)NC(CC(C)C)C(=O)NC(CCC(O)=O)C(=O)NC(CC(N)=O)C(=O)NC(CC=2C=CC(O)=CC=2)C(=O)NC(CSSCC(NC(=O)C(C(C)C)NC(=O)C(CC(C)C)NC(=O)C(CC=2C=CC(O)=CC=2)NC(=O)C(CC(C)C)NC(=O)C(C)NC(=O)C(CCC(O)=O)NC(=O)C(C(C)C)NC(=O)C(CC(C)C)NC(=O)C(CC=2NC=NC=2)NC(=O)C(CO)NC(=O)CNC2=O)C(=O)NCC(=O)NC(CCC(O)=O)C(=O)NC(CCCNC(N)=N)C(=O)NCC(=O)NC(CC=3C=CC=CC=3)C(=O)NC(CC=3C=CC=CC=3)C(=O)NC(CC=3C=CC(O)=CC=3)C(=O)NC(C(C)O)C(=O)N3C(CCC3)C(=O)NC(CCCCN)C(=O)NC(C)C(O)=O)C(=O)NC(CC(N)=O)C(O)=O)=O)NC(=O)C(C(C)CC)NC(=O)C(CO)NC(=O)C(C(C)O)NC(=O)C1CSSCC2NC(=O)C(CC(C)C)NC(=O)C(NC(=O)C(CCC(N)=O)NC(=O)C(CC(N)=O)NC(=O)C(NC(=O)C(N)CC=1C=CC=CC=1)C(C)C)CC1=CN=CN1 NOESYZHRGYRDHS-UHFFFAOYSA-N 0.000 claims 4
- 102000007399 Nuclear hormone receptor Human genes 0.000 claims 3
- 108020005497 Nuclear hormone receptor Proteins 0.000 claims 3
- 125000003118 aryl group Chemical group 0.000 claims 3
- 229910052739 hydrogen Inorganic materials 0.000 claims 3
- 239000003112 inhibitor Substances 0.000 claims 3
- -1 substituted Chemical class 0.000 claims 3
- SNICXCGAKADSCV-JTQLQIEISA-N (-)-Nicotine Chemical compound CN1CCC[C@H]1C1=CC=CN=C1 SNICXCGAKADSCV-JTQLQIEISA-N 0.000 claims 2
- 101100516563 Caenorhabditis elegans nhr-6 gene Proteins 0.000 claims 2
- 102000016622 Dipeptidyl Peptidase 4 Human genes 0.000 claims 2
- 101000930822 Giardia intestinalis Dipeptidyl-peptidase 4 Proteins 0.000 claims 2
- DTHNMHAUYICORS-KTKZVXAJSA-N Glucagon-like peptide 1 Chemical compound C([C@@H](C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](C)C(=O)N[C@@H](CC=1C2=CC=CC=C2NC=1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](CCCNC(N)=N)C(N)=O)NC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@H](CCC(N)=O)NC(=O)CNC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC=1C=CC(O)=CC=1)NC(=O)[C@H](CO)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](CC(O)=O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](CC=1C=CC=CC=1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](C)NC(=O)[C@@H](N)CC=1N=CNC=1)[C@@H](C)O)[C@@H](C)O)C(C)C)C1=CC=CC=C1 DTHNMHAUYICORS-KTKZVXAJSA-N 0.000 claims 2
- 102000004877 Insulin Human genes 0.000 claims 2
- 108090001061 Insulin Proteins 0.000 claims 2
- 102000023984 PPAR alpha Human genes 0.000 claims 2
- 229910052799 carbon Inorganic materials 0.000 claims 2
- 239000003937 drug carrier Substances 0.000 claims 2
- 125000001072 heteroaryl group Chemical group 0.000 claims 2
- 125000005842 heteroatom Chemical group 0.000 claims 2
- 229940125396 insulin Drugs 0.000 claims 2
- 238000000034 method Methods 0.000 claims 2
- 229910052757 nitrogen Inorganic materials 0.000 claims 2
- 229910052760 oxygen Inorganic materials 0.000 claims 2
- 108091008725 peroxisome proliferator-activated receptors alpha Proteins 0.000 claims 2
- 239000008194 pharmaceutical composition Substances 0.000 claims 2
- 229910052717 sulfur Inorganic materials 0.000 claims 2
- 208000001072 type 2 diabetes mellitus Diseases 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
- DGENZVKCTGIDRZ-UHFFFAOYSA-N 3-[4-[(3-phenoxyphenyl)methylamino]phenyl]propanoic acid Chemical compound C1=CC(CCC(=O)O)=CC=C1NCC1=CC=CC(OC=2C=CC=CC=2)=C1 DGENZVKCTGIDRZ-UHFFFAOYSA-N 0.000 claims 1
- MVQVNTPHUGQQHK-UHFFFAOYSA-N 3-pyridinemethanol Chemical compound OCC1=CC=CN=C1 MVQVNTPHUGQQHK-UHFFFAOYSA-N 0.000 claims 1
- 229940077274 Alpha glucosidase inhibitor Drugs 0.000 claims 1
- 229940123208 Biguanide Drugs 0.000 claims 1
- XNCOSPRUTUOJCJ-UHFFFAOYSA-N Biguanide Chemical compound NC(N)=NC(N)=N XNCOSPRUTUOJCJ-UHFFFAOYSA-N 0.000 claims 1
- 101001078593 Caenorhabditis elegans 3beta-hydroxysteroid dehydrogenase/Delta(5)-Delta(4) isomerase 1 Proteins 0.000 claims 1
- 229940122502 Cholesterol absorption inhibitor Drugs 0.000 claims 1
- 101710198884 GATA-type zinc finger protein 1 Proteins 0.000 claims 1
- 229940125827 GPR40 agonist Drugs 0.000 claims 1
- 229940122904 Glucagon receptor antagonist Drugs 0.000 claims 1
- 229940121710 HMGCoA reductase inhibitor Drugs 0.000 claims 1
- 101000618112 Homo sapiens Sperm-associated antigen 8 Proteins 0.000 claims 1
- 229940077672 Ileal bile acid transport inhibitor Drugs 0.000 claims 1
- 206010028980 Neoplasm Diseases 0.000 claims 1
- 229940122054 Peroxisome proliferator-activated receptor delta agonist Drugs 0.000 claims 1
- 229940080774 Peroxisome proliferator-activated receptor gamma agonist Drugs 0.000 claims 1
- 102100040918 Pro-glucagon Human genes 0.000 claims 1
- 102100021913 Sperm-associated antigen 8 Human genes 0.000 claims 1
- 102000001494 Sterol O-Acyltransferase Human genes 0.000 claims 1
- 108010054082 Sterol O-acyltransferase Proteins 0.000 claims 1
- 229940100389 Sulfonylurea Drugs 0.000 claims 1
- 125000002252 acyl group Chemical group 0.000 claims 1
- 239000000556 agonist Substances 0.000 claims 1
- 239000003888 alpha glucosidase inhibitor Substances 0.000 claims 1
- 230000001548 androgenic effect Effects 0.000 claims 1
- 239000002260 anti-inflammatory agent Substances 0.000 claims 1
- 229940124599 anti-inflammatory drug Drugs 0.000 claims 1
- 230000003579 anti-obesity Effects 0.000 claims 1
- 239000003613 bile acid Substances 0.000 claims 1
- 201000011510 cancer Diseases 0.000 claims 1
- 239000002738 chelating agent Substances 0.000 claims 1
- 239000003795 chemical substances by application Substances 0.000 claims 1
- 239000003354 cholesterol ester transfer protein inhibitor Substances 0.000 claims 1
- 229940125881 cholesteryl ester transfer protein inhibitor Drugs 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 229940125542 dual agonist Drugs 0.000 claims 1
- 239000002471 hydroxymethylglutaryl coenzyme A reductase inhibitor Substances 0.000 claims 1
- 125000000842 isoxazolyl group Chemical group 0.000 claims 1
- 150000002632 lipids Chemical class 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 229960002715 nicotine Drugs 0.000 claims 1
- SNICXCGAKADSCV-UHFFFAOYSA-N nicotine Natural products CN1CCCC1C1=CC=CN=C1 SNICXCGAKADSCV-UHFFFAOYSA-N 0.000 claims 1
- 229960004738 nicotinyl alcohol Drugs 0.000 claims 1
- 125000001715 oxadiazolyl group Chemical group 0.000 claims 1
- 125000002971 oxazolyl group Chemical group 0.000 claims 1
- 239000004031 partial agonist Substances 0.000 claims 1
- 239000002530 phenolic antioxidant Substances 0.000 claims 1
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 1
- 125000003373 pyrazinyl group Chemical group 0.000 claims 1
- 125000002098 pyridazinyl 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
- YROXIXLRRCOBKF-UHFFFAOYSA-N sulfonylurea Chemical class OC(=N)N=S(=O)=O YROXIXLRRCOBKF-UHFFFAOYSA-N 0.000 claims 1
- 125000001113 thiadiazolyl 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
- 125000001425 triazolyl group Chemical group 0.000 claims 1
- 0 B[C@@]12C(C([C@](*=CC)F)F)C(C)(C3)[C@]3C(CC(CCC*)*N(C)C(C)C)C(C)[C@]1C2 Chemical compound B[C@@]12C(C([C@](*=CC)F)F)C(C)(C3)[C@]3C(CC(CCC*)*N(C)C(C)C)C(C)[C@]1C2 0.000 description 4
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US89770007P | 2007-01-26 | 2007-01-26 | |
| US60/897,700 | 2007-01-26 | ||
| PCT/CA2008/000172 WO2008089581A1 (en) | 2007-01-26 | 2008-01-24 | Fused aromatic ptp-1b inhibitors |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2010516715A JP2010516715A (ja) | 2010-05-20 |
| JP2010516715A5 true JP2010516715A5 (enExample) | 2011-02-03 |
| JP5570223B2 JP5570223B2 (ja) | 2014-08-13 |
Family
ID=39644072
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2009546627A Expired - Fee Related JP5570223B2 (ja) | 2007-01-26 | 2008-01-24 | タンパク質チロシンホスファターゼ１ｂ（ｐｔｐ−１ｂ）阻害剤としての縮合芳香族ジフルオロメタンホスホネート |
Country Status (16)
| Country | Link |
|---|---|
| US (4) | US8168815B2 (enExample) |
| EP (1) | EP2114971B1 (enExample) |
| JP (1) | JP5570223B2 (enExample) |
| KR (1) | KR101568799B1 (enExample) |
| CN (1) | CN102317296B (enExample) |
| AU (1) | AU2008209296B2 (enExample) |
| BR (1) | BRPI0806789B8 (enExample) |
| CA (1) | CA2675142C (enExample) |
| DK (1) | DK2114971T3 (enExample) |
| ES (1) | ES2547386T3 (enExample) |
| IL (1) | IL199742A (enExample) |
| MX (1) | MX2009007911A (enExample) |
| NZ (2) | NZ600947A (enExample) |
| RU (1) | RU2462469C2 (enExample) |
| WO (1) | WO2008089581A1 (enExample) |
| ZA (1) | ZA200904679B (enExample) |
Families Citing this family (15)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CA2675142C (en) * | 2007-01-26 | 2014-08-19 | Merck Frosst Canada Ltd. | Fused aromatic difluoromethanephosphonates as protein tyrosine phosphatase 1b (ptp-1b) inhibitors |
| WO2011107494A1 (de) | 2010-03-03 | 2011-09-09 | Sanofi | Neue aromatische glykosidderivate, diese verbindungen enthaltende arzneimittel und deren verwendung |
| 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 |
| TW201221505A (en) | 2010-07-05 | 2012-06-01 | Sanofi Sa | Aryloxyalkylene-substituted hydroxyphenylhexynoic acids, process for preparation thereof and use thereof as a medicament |
| 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 |
| TW201215388A (en) | 2010-07-05 | 2012-04-16 | Sanofi Sa | (2-aryloxyacetylamino)phenylpropionic acid derivatives, processes for preparation thereof and use thereof as medicaments |
| 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 |
| MX2014012465A (es) | 2012-04-16 | 2015-01-12 | Kaneq Pharma Inc | Derivados de fosfonato aromaticos fusionados como precursores de inhibidores de tirosina fosfatasa de proteina 1b. |
| WO2014141110A2 (en) * | 2013-03-14 | 2014-09-18 | Curadev Pharma Pvt. Ltd. | Aminonitriles as kynurenine pathway inhibitors |
| US9828399B2 (en) * | 2014-02-28 | 2017-11-28 | The Royal Institution For The Advancement Of Learning/Mcgill University | TC-PTP inhibitors as APC activators for immunotherapy |
| CN108159069A (zh) * | 2018-01-26 | 2018-06-15 | 广东省微生物研究所（广东省微生物分析检测中心） | 灰树花多糖f2在制备治疗高脂血症药物、预防或延缓动脉粥样硬化药物中的应用 |
| WO2023220833A1 (en) * | 2022-05-19 | 2023-11-23 | Kanyr Pharma Inc. | Combined inhibition of tyrosine phosphatases tcptp and ptp1b and pd-1 blockage immunotherapy in the treatment of cancer |
| EP4630001A1 (en) * | 2022-12-05 | 2025-10-15 | Merck Sharp & Dohme LLC | Substituted quinazoline derivatives and methods of use thereof |
Family Cites Families (12)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| FI83421C (fi) * | 1989-06-21 | 1991-07-10 | Huhtamaeki Oy | Foerfarande foer framstaellning av farmakologiskt anvaendbara metylenbisfosfonsyraderivat. |
| AU1856997A (en) | 1996-02-02 | 1997-08-22 | Merck & Co., Inc. | Method for raising hdl cholesterol levels |
| US6174874B1 (en) * | 1998-09-21 | 2001-01-16 | Merck Frosst Canada & Co. | Phosphonic acids derivatives as inhibitors of protein tyrosine phosphate 1B (PTP-1B) |
| US6486142B2 (en) * | 1999-12-22 | 2002-11-26 | Merck Frosst Canada & Co. | Phosphonic acid derivatives as inhibitors of protein tyrosine phosphatase 1B (PTP-1B) |
| US6465444B2 (en) * | 2000-03-22 | 2002-10-15 | Merck Frosst Canada & Co. | Aryldifluoromethylphosphonic acids with sulfur-containing substituents as PTP-1B inhibitors |
| ATE362468T1 (de) | 2000-07-25 | 2007-06-15 | Merck & Co Inc | N-substituierte indole mit anwendung in der behandlung von diabetes |
| AU2003265681A1 (en) | 2002-08-29 | 2004-03-19 | Merck And Co., Inc. | Indoles having anti-diabetic activity |
| ES2336009T3 (es) * | 2004-01-30 | 2010-04-07 | Medivir Ab | Inhibidores de la ns-3 serina proteasa del vhc. |
| WO2005100298A1 (en) | 2004-04-13 | 2005-10-27 | Merck & Co., Inc. | Cetp inhibitors |
| DOP2005000123A (es) | 2004-07-02 | 2011-07-15 | Merck Sharp & Dohme | Inhibidores de cetp |
| CA2586363A1 (en) | 2004-11-15 | 2006-05-26 | Ceptyr, Inc. | Protein tyrosine phosphatase inhibitors and methods of use thereof |
| CA2675142C (en) * | 2007-01-26 | 2014-08-19 | Merck Frosst Canada Ltd. | Fused aromatic difluoromethanephosphonates as protein tyrosine phosphatase 1b (ptp-1b) inhibitors |
-
2008
- 2008-01-24 CA CA2675142A patent/CA2675142C/en not_active Expired - Fee Related
- 2008-01-24 EP EP08706319.4A patent/EP2114971B1/en not_active Not-in-force
- 2008-01-24 JP JP2009546627A patent/JP5570223B2/ja not_active Expired - Fee Related
- 2008-01-24 RU RU2009132092/04A patent/RU2462469C2/ru not_active IP Right Cessation
- 2008-01-24 DK DK08706319.4T patent/DK2114971T3/en active
- 2008-01-24 CN CN200880010110.9A patent/CN102317296B/zh not_active Expired - Fee Related
- 2008-01-24 MX MX2009007911A patent/MX2009007911A/es active IP Right Grant
- 2008-01-24 KR KR1020097017809A patent/KR101568799B1/ko not_active Expired - Fee Related
- 2008-01-24 NZ NZ600947A patent/NZ600947A/xx not_active IP Right Cessation
- 2008-01-24 WO PCT/CA2008/000172 patent/WO2008089581A1/en not_active Ceased
- 2008-01-24 NZ NZ578296A patent/NZ578296A/en not_active IP Right Cessation
- 2008-01-24 AU AU2008209296A patent/AU2008209296B2/en not_active Ceased
- 2008-01-24 BR BRPI0806789A patent/BRPI0806789B8/pt not_active IP Right Cessation
- 2008-01-24 ES ES08706319.4T patent/ES2547386T3/es active Active
- 2008-01-24 US US12/518,899 patent/US8168815B2/en active Active
-
2009
- 2009-07-03 ZA ZA200904679A patent/ZA200904679B/xx unknown
- 2009-07-07 IL IL199742A patent/IL199742A/en active IP Right Grant
-
2012
- 2012-03-13 US US13/418,956 patent/US8481742B2/en not_active Expired - Fee Related
-
2013
- 2013-05-21 US US13/898,947 patent/US8927526B2/en active Active
-
2014
- 2014-10-28 US US14/525,396 patent/US9334295B2/en active Active