JP2010514829A5 - - Google Patents
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- JP2010514829A5 JP2010514829A5 JP2009544448A JP2009544448A JP2010514829A5 JP 2010514829 A5 JP2010514829 A5 JP 2010514829A5 JP 2009544448 A JP2009544448 A JP 2009544448A JP 2009544448 A JP2009544448 A JP 2009544448A JP 2010514829 A5 JP2010514829 A5 JP 2010514829A5
- Authority
- JP
- Japan
- Prior art keywords
- pharmaceutically acceptable
- acceptable salt
- compound
- compound according
- table below
- 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.)
- Pending
Links
- 150000003839 salts Chemical class 0.000 claims 36
- 150000001875 compounds Chemical class 0.000 claims 35
- 125000000217 alkyl group Chemical group 0.000 claims 7
- 229910052739 hydrogen Inorganic materials 0.000 claims 6
- 239000001257 hydrogen Substances 0.000 claims 6
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 6
- 239000003814 drug Substances 0.000 claims 5
- -1 n- propyl Chemical group 0.000 claims 5
- 150000002431 hydrogen Chemical class 0.000 claims 4
- 201000010099 disease Diseases 0.000 claims 3
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 3
- 125000004356 hydroxy functional group Chemical group O* 0.000 claims 3
- 229940124597 therapeutic agent Drugs 0.000 claims 3
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 2
- 125000001309 chloro group Chemical group Cl* 0.000 claims 2
- 125000001153 fluoro group Chemical group F* 0.000 claims 2
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims 2
- 208000024891 symptom Diseases 0.000 claims 2
- 125000000954 2-hydroxyethyl group Chemical group [H]C([*])([H])C([H])([H])O[H] 0.000 claims 1
- 208000002705 Glucose Intolerance Diseases 0.000 claims 1
- 102100033839 Glucose-dependent insulinotropic receptor Human genes 0.000 claims 1
- 101000996752 Homo sapiens Glucose-dependent insulinotropic receptor Proteins 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
- 208000001145 Metabolic Syndrome Diseases 0.000 claims 1
- 208000008589 Obesity Diseases 0.000 claims 1
- 201000000690 abdominal obesity-metabolic syndrome Diseases 0.000 claims 1
- 206010012601 diabetes mellitus Diseases 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 125000005843 halogen group Chemical group 0.000 claims 1
- 208000006575 hypertriglyceridemia Diseases 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 238000000034 method Methods 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
- 230000036186 satiety Effects 0.000 claims 1
- 235000019627 satiety Nutrition 0.000 claims 1
- 208000011580 syndromic disease Diseases 0.000 claims 1
- 125000000999 tert-butyl group Chemical group [H]C([H])([H])C(*)(C([H])([H])[H])C([H])([H])[H] 0.000 claims 1
Applications Claiming Priority (4)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| GB0700124A GB0700124D0 (en) | 2007-01-04 | 2007-01-04 | GPCR agonists |
| GB0708740A GB0708740D0 (en) | 2007-05-08 | 2007-05-08 | Gpcr agonists |
| GB0719762A GB0719762D0 (en) | 2007-10-10 | 2007-10-10 | GPCR agonists |
| PCT/GB2008/050011 WO2008081205A1 (en) | 2007-01-04 | 2008-01-04 | Piperidine gpcr agonists |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2010514829A JP2010514829A (ja) | 2010-05-06 |
| JP2010514829A5 true JP2010514829A5 (enExample) | 2011-02-24 |
Family
ID=39203222
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2009544448A Pending JP2010514829A (ja) | 2007-01-04 | 2008-01-04 | ピペリジンgpcrアゴニスト |
Country Status (27)
| Country | Link |
|---|---|
| US (1) | US20100022591A1 (enExample) |
| EP (2) | EP2383270A1 (enExample) |
| JP (1) | JP2010514829A (enExample) |
| KR (1) | KR20090104092A (enExample) |
| CN (1) | CN101627036A (enExample) |
| AR (1) | AR064736A1 (enExample) |
| AT (1) | ATE531710T1 (enExample) |
| AU (1) | AU2008203673A1 (enExample) |
| BR (1) | BRPI0806468A2 (enExample) |
| CA (1) | CA2674093A1 (enExample) |
| CL (1) | CL2008000017A1 (enExample) |
| DK (1) | DK2114931T3 (enExample) |
| EA (1) | EA015805B9 (enExample) |
| ES (1) | ES2376015T3 (enExample) |
| HR (1) | HRP20110964T1 (enExample) |
| IL (1) | IL199680A0 (enExample) |
| MA (1) | MA31084B1 (enExample) |
| MX (1) | MX2009007180A (enExample) |
| NZ (1) | NZ578144A (enExample) |
| PE (1) | PE20081849A1 (enExample) |
| PL (1) | PL2114931T3 (enExample) |
| PT (1) | PT2114931E (enExample) |
| RS (1) | RS52168B (enExample) |
| SA (1) | SA08280756B1 (enExample) |
| SI (1) | SI2114931T1 (enExample) |
| TW (1) | TWI380818B (enExample) |
| WO (1) | WO2008081205A1 (enExample) |
Families Citing this family (64)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US7407955B2 (en) | 2002-08-21 | 2008-08-05 | Boehringer Ingelheim Pharma Gmbh & Co., Kg | 8-[3-amino-piperidin-1-yl]-xanthines, the preparation thereof and their use as pharmaceutical compositions |
| US7501426B2 (en) | 2004-02-18 | 2009-03-10 | Boehringer Ingelheim International Gmbh | 8-[3-amino-piperidin-1-yl]-xanthines, their preparation and their use as pharmaceutical compositions |
| DE102004054054A1 (de) | 2004-11-05 | 2006-05-11 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | Verfahren zur Herstellung chiraler 8-(3-Amino-piperidin-1-yl)-xanthine |
| NZ556017A (en) * | 2004-12-24 | 2009-10-30 | Prosidion Ltd | G-protein coupled receptor (gpr116) agonists and use thereof for treating obesity and diabetes |
| EP2308840A1 (en) * | 2005-06-30 | 2011-04-13 | Prosidion Limited | GPCR agonists |
| DE102005035891A1 (de) | 2005-07-30 | 2007-02-08 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | 8-(3-Amino-piperidin-1-yl)-xanthine, deren Herstellung und deren Verwendung als Arzneimittel |
| MX2008014024A (es) | 2006-05-04 | 2008-11-14 | Boehringer Ingelheim Int | Formas poliformas. |
| EP1852108A1 (en) | 2006-05-04 | 2007-11-07 | Boehringer Ingelheim Pharma GmbH & Co.KG | DPP IV inhibitor formulations |
| PE20110235A1 (es) | 2006-05-04 | 2011-04-14 | Boehringer Ingelheim Int | Combinaciones farmaceuticas que comprenden linagliptina y metmorfina |
| AR064735A1 (es) * | 2007-01-04 | 2009-04-22 | Prosidion Ltd | Agonistas de gpcr y composicion farmaceutica en base al compuesto |
| EP2200609A1 (en) | 2007-09-10 | 2010-06-30 | Prosidion Limited | Compounds for the treatment of metabolic disorders |
| AU2008309589B2 (en) | 2007-10-10 | 2012-07-05 | Novartis Ag | Spiropyrrolidines and their use against HCV and HIV infection |
| PE20140960A1 (es) | 2008-04-03 | 2014-08-15 | Boehringer Ingelheim Int | Formulaciones que comprenden un inhibidor de dpp4 |
| GB0812642D0 (en) * | 2008-07-10 | 2008-08-20 | Prosidion Ltd | Compounds |
| GB0812648D0 (en) * | 2008-07-10 | 2008-08-20 | Prosidion Ltd | Compounds |
| GB0812649D0 (en) * | 2008-07-10 | 2008-08-20 | Prosidion Ltd | Compounds |
| BRPI0915867A2 (pt) * | 2008-07-11 | 2017-06-20 | Irm Llc | 4-fenoximetilpiperidinas como moduladores de atividade de gpr119 |
| KR20200118243A (ko) | 2008-08-06 | 2020-10-14 | 베링거 인겔하임 인터내셔날 게엠베하 | 메트포르민 요법이 부적합한 환자에서의 당뇨병 치료 |
| UY32030A (es) | 2008-08-06 | 2010-03-26 | Boehringer Ingelheim Int | "tratamiento para diabetes en pacientes inapropiados para terapia con metformina" |
| CN102149407A (zh) | 2008-09-10 | 2011-08-10 | 贝林格尔.英格海姆国际有限公司 | 治疗糖尿病和相关病症的组合疗法 |
| US20200155558A1 (en) | 2018-11-20 | 2020-05-21 | Boehringer Ingelheim International Gmbh | Treatment for diabetes in patients with insufficient glycemic control despite therapy with an oral antidiabetic drug |
| CN107011345A (zh) | 2008-12-23 | 2017-08-04 | 勃林格殷格翰国际有限公司 | 有机化合物的盐形式 |
| TW201036975A (en) | 2009-01-07 | 2010-10-16 | Boehringer Ingelheim Int | Treatment for diabetes in patients with inadequate glycemic control despite metformin therapy |
| GB0904284D0 (en) | 2009-03-12 | 2009-04-22 | Prosidion Ltd | Compounds for the treatment of metabolic disorders |
| GB0904285D0 (en) | 2009-03-12 | 2009-04-22 | Prosidion Ltd | Compounds for the treatment of metabolic disorders |
| GB0904287D0 (en) | 2009-03-12 | 2009-04-22 | Prosidion Ltd | Compounds for the treatment of metabolic disorders |
| TW201113269A (en) | 2009-06-24 | 2011-04-16 | Boehringer Ingelheim Int | New compounds, pharmaceutical composition and methods relating thereto |
| NZ596445A (en) | 2009-06-24 | 2013-04-26 | Boehringer Ingelheim Int | New compounds, pharmaceutical composition and methods relating thereto |
| US8552022B2 (en) | 2009-08-13 | 2013-10-08 | Merck Sharp & Dohme Corp. | Substituted cyclopropyl compounds, compositions containing such compounds and methods of treatment |
| EP2504002B1 (en) | 2009-11-27 | 2019-10-09 | Boehringer Ingelheim International GmbH | Treatment of genotyped diabetic patients with dpp-iv inhibitors such as linagliptin |
| WO2011107494A1 (de) | 2010-03-03 | 2011-09-09 | Sanofi | Neue aromatische glykosidderivate, diese verbindungen enthaltende arzneimittel und deren verwendung |
| WO2011113947A1 (en) | 2010-03-18 | 2011-09-22 | Boehringer Ingelheim International Gmbh | Combination of a gpr119 agonist and the dpp-iv inhibitor linagliptin for use in the treatment of diabetes and related conditions |
| GB201006167D0 (en) | 2010-04-14 | 2010-05-26 | Prosidion Ltd | Compounds for the treatment of metabolic disorders |
| GB201006166D0 (en) | 2010-04-14 | 2010-05-26 | Prosidion Ltd | Compounds for the treatment of metabolic disorders |
| ITMI20100770A1 (it) | 2010-05-03 | 2011-11-04 | Dipharma Francis Srl | Procedimento per la preparazione di 3-(4-piridinil)-propanolo e suoi intermedi |
| KR101927068B1 (ko) | 2010-05-05 | 2018-12-10 | 베링거 인겔하임 인터내셔날 게엠베하 | 체중 감소 치료에 후속하는 dpp-4 억제제에 의한 순차적 병용 요법 |
| TW201209054A (en) | 2010-05-28 | 2012-03-01 | Prosidion Ltd | Novel compounds |
| ITMI20100984A1 (it) | 2010-05-31 | 2011-12-01 | Dipharma Francis Srl | Procedimento per la preparazione di ossadiazoli |
| 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 |
| KR20200028498A (ko) | 2010-06-24 | 2020-03-16 | 베링거 인겔하임 인터내셔날 게엠베하 | 당뇨병 요법 |
| 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 |
| TW201215388A (en) | 2010-07-05 | 2012-04-16 | Sanofi Sa | (2-aryloxyacetylamino)phenylpropionic acid derivatives, processes for preparation thereof and use thereof as medicaments |
| AR083878A1 (es) | 2010-11-15 | 2013-03-27 | Boehringer Ingelheim Int | Terapia antidiabetica vasoprotectora y cardioprotectora, linagliptina, metodo de tratamiento |
| GB201114389D0 (en) | 2011-08-22 | 2011-10-05 | Prosidion Ltd | Novel compounds |
| AR083904A1 (es) | 2010-11-18 | 2013-04-10 | Prosidion Ltd | Derivados de 1,4-pirrolidinas disustituidos y 3-il-aminas y sus usos en el tratamiento de desordenes metabolicos |
| WO2012138845A1 (en) * | 2011-04-08 | 2012-10-11 | Merck Sharp & Dohme Corp. | Substituted cyclopropyl compounds, compositions containing such compounds and methods of treatment |
| WO2012170867A1 (en) | 2011-06-09 | 2012-12-13 | Rhizen Pharmaceuticals Sa | Novel compounds as modulators of gpr-119 |
| EP2720544B1 (en) | 2011-06-16 | 2016-12-21 | Merck Sharp & Dohme Corp. | Substituted cyclopropyl compounds, compositions containing such compounds, and methods of treatment |
| HUE061596T2 (hu) | 2011-07-15 | 2023-07-28 | Boehringer Ingelheim Int | Szubsztituált dimer kinazolin származék, annak elõállítása és alkalmazása az I. és II. típusú cukorbetegség kezelésére szolgáló gyógyszerkészítményekben |
| 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 |
| EP2760855B1 (en) | 2011-09-30 | 2017-03-15 | Merck Sharp & Dohme Corp. | Substituted cyclopropyl compounds, compositions containing such compounds as well as their use in treating type-2 diabetes |
| WO2013062838A1 (en) * | 2011-10-24 | 2013-05-02 | Merck Sharp & Dohme Corp. | Substituted piperidinyl compounds useful as gpr119 agonists |
| AU2012339870B2 (en) | 2011-11-15 | 2017-06-29 | Merck Sharp & Dohme Corp. | Substituted cyclopropyl compounds useful as GPR119 agonists |
| US9555001B2 (en) | 2012-03-07 | 2017-01-31 | Boehringer Ingelheim International Gmbh | Pharmaceutical composition and uses thereof |
| ES2929025T3 (es) | 2012-05-14 | 2022-11-24 | Boehringer Ingelheim Int | Linagliptina, un derivado de xantina como inhibidor de dpp-4, para su uso en el tratamiento del SRIS y/o de la septicemia |
| US20130303462A1 (en) | 2012-05-14 | 2013-11-14 | Boehringer Ingelheim International Gmbh | Use of a dpp-4 inhibitor in podocytes related disorders and/or nephrotic syndrome |
| WO2013174767A1 (en) | 2012-05-24 | 2013-11-28 | Boehringer Ingelheim International Gmbh | A xanthine derivative as dpp -4 inhibitor for use in modifying food intake and regulating food preference |
| EP3110449B1 (en) | 2014-02-28 | 2023-06-28 | Boehringer Ingelheim International GmbH | Medical use of a dpp-4 inhibitor |
| KR101726819B1 (ko) * | 2014-10-27 | 2017-04-13 | 동아에스티 주식회사 | Gpr119 작용 활성을 갖는 화합물, 이의 제조방법 및 이를 유효성분으로 함유하는 약제학적 조성물 |
| BR112018072401A2 (pt) | 2016-06-10 | 2019-02-19 | Boehringer Ingelheim International Gmbh | combinações de linagliptina e metformina |
| EP3421455B1 (en) * | 2017-06-29 | 2019-03-27 | F.I.S.- Fabbrica Italiana Sintetici S.p.A. | Improved process for the preparation of chiral 3-amino-piperidins, useful intermediates for the preparation of tofacitinib |
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-
2008
- 2008-01-03 PE PE2008000085A patent/PE20081849A1/es not_active Application Discontinuation
- 2008-01-03 CL CL200800017A patent/CL2008000017A1/es unknown
- 2008-01-03 AR ARP080100018A patent/AR064736A1/es not_active Application Discontinuation
- 2008-01-04 EA EA200900796A patent/EA015805B9/ru not_active IP Right Cessation
- 2008-01-04 DK DK08700184.8T patent/DK2114931T3/da active
- 2008-01-04 US US12/522,018 patent/US20100022591A1/en not_active Abandoned
- 2008-01-04 EP EP11172885A patent/EP2383270A1/en not_active Withdrawn
- 2008-01-04 KR KR1020097016214A patent/KR20090104092A/ko not_active Withdrawn
- 2008-01-04 ES ES08700184T patent/ES2376015T3/es active Active
- 2008-01-04 NZ NZ578144A patent/NZ578144A/en not_active IP Right Cessation
- 2008-01-04 CA CA002674093A patent/CA2674093A1/en not_active Abandoned
- 2008-01-04 JP JP2009544448A patent/JP2010514829A/ja active Pending
- 2008-01-04 EP EP08700184A patent/EP2114931B1/en active Active
- 2008-01-04 HR HR20110964T patent/HRP20110964T1/hr unknown
- 2008-01-04 WO PCT/GB2008/050011 patent/WO2008081205A1/en not_active Ceased
- 2008-01-04 MX MX2009007180A patent/MX2009007180A/es active IP Right Grant
- 2008-01-04 BR BRPI0806468-7A patent/BRPI0806468A2/pt not_active IP Right Cessation
- 2008-01-04 AU AU2008203673A patent/AU2008203673A1/en not_active Abandoned
- 2008-01-04 CN CN200880007091A patent/CN101627036A/zh active Pending
- 2008-01-04 PT PT08700184T patent/PT2114931E/pt unknown
- 2008-01-04 RS RS20120031A patent/RS52168B/sr unknown
- 2008-01-04 TW TW097100419A patent/TWI380818B/zh not_active IP Right Cessation
- 2008-01-04 PL PL08700184T patent/PL2114931T3/pl unknown
- 2008-01-04 AT AT08700184T patent/ATE531710T1/de active
- 2008-01-04 SI SI200830517T patent/SI2114931T1/sl unknown
- 2008-01-05 SA SA8280756A patent/SA08280756B1/ar unknown
-
2009
- 2009-07-02 IL IL199680A patent/IL199680A0/en unknown
- 2009-07-03 MA MA32072A patent/MA31084B1/fr unknown
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