JP2015503582A5 - - Google Patents
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- JP2015503582A5 JP2015503582A5 JP2014551231A JP2014551231A JP2015503582A5 JP 2015503582 A5 JP2015503582 A5 JP 2015503582A5 JP 2014551231 A JP2014551231 A JP 2014551231A JP 2014551231 A JP2014551231 A JP 2014551231A JP 2015503582 A5 JP2015503582 A5 JP 2015503582A5
- Authority
- JP
- Japan
- Prior art keywords
- composition
- biguanide compound
- metformin
- optionally substituted
- 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.)
- Withdrawn
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- 239000000203 mixture Substances 0.000 claims description 112
- 229940123208 Biguanide Drugs 0.000 claims description 46
- -1 biguanide compound Chemical class 0.000 claims description 46
- XZWYZXLIPXDOLR-UHFFFAOYSA-N metformin Chemical compound CN(C)C(=N)NC(N)=N XZWYZXLIPXDOLR-UHFFFAOYSA-N 0.000 claims description 36
- 229910052757 nitrogen Inorganic materials 0.000 claims description 28
- 125000000217 alkyl group Chemical group 0.000 claims description 22
- 229960003105 metformin Drugs 0.000 claims description 22
- 125000005119 alkyl cycloalkyl group Chemical group 0.000 claims description 18
- 125000004433 nitrogen atom Chemical group N* 0.000 claims description 18
- 125000000753 cycloalkyl group Chemical group 0.000 claims description 17
- 238000000034 method Methods 0.000 claims description 17
- OETHQSJEHLVLGH-UHFFFAOYSA-N metformin hydrochloride Chemical compound Cl.CN(C)C(=N)N=C(N)N OETHQSJEHLVLGH-UHFFFAOYSA-N 0.000 claims description 16
- 229960004329 metformin hydrochloride Drugs 0.000 claims description 14
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims description 12
- 239000012729 immediate-release (IR) formulation Substances 0.000 claims description 11
- 125000003226 pyrazolyl group Chemical group 0.000 claims description 11
- 125000000168 pyrrolyl group Chemical group 0.000 claims description 11
- 125000005213 alkyl heteroaryl group Chemical group 0.000 claims description 9
- 125000001072 heteroaryl group Chemical group 0.000 claims description 9
- 150000003839 salts Chemical class 0.000 claims description 9
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- 125000004426 substituted alkynyl group Chemical group 0.000 claims description 8
- 125000002877 alkyl aryl group Chemical group 0.000 claims description 7
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- 125000005017 substituted alkenyl group Chemical group 0.000 claims description 7
- 125000000547 substituted alkyl group Chemical group 0.000 claims description 7
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- 239000003112 inhibitor Substances 0.000 claims description 6
- 230000036470 plasma concentration Effects 0.000 claims description 6
- NOWKCMXCCJGMRR-UHFFFAOYSA-N Aziridine Chemical compound C1CN1 NOWKCMXCCJGMRR-UHFFFAOYSA-N 0.000 claims description 5
- 108010067722 Dipeptidyl Peptidase 4 Proteins 0.000 claims description 5
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- 125000002252 acyl group Chemical group 0.000 claims description 5
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- 125000002883 imidazolyl group Chemical group 0.000 claims description 5
- 125000003387 indolinyl group Chemical group N1(CCC2=CC=CC=C12)* 0.000 claims description 5
- 125000001041 indolyl group Chemical group 0.000 claims description 5
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- DHHVAGZRUROJKS-UHFFFAOYSA-N phentermine Chemical group CC(C)(N)CC1=CC=CC=C1 DHHVAGZRUROJKS-UHFFFAOYSA-N 0.000 claims 6
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- SWLAMJPTOQZTAE-UHFFFAOYSA-N 4-[2-[(5-chloro-2-methoxybenzoyl)amino]ethyl]benzoic acid Chemical class COC1=CC=C(Cl)C=C1C(=O)NCCC1=CC=C(C(O)=O)C=C1 SWLAMJPTOQZTAE-UHFFFAOYSA-N 0.000 claims 1
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| EP2629609A4 (en) | 2010-10-19 | 2014-08-27 | Elcelyx Therapeutics Inc | THERAPIES BASED ON CHEMOSOUS RECEPTOR LIGANDS |
| US8796338B2 (en) | 2011-01-07 | 2014-08-05 | Elcelyx Therapeutics, Inc | Biguanide compositions and methods of treating metabolic disorders |
| US9480663B2 (en) | 2011-01-07 | 2016-11-01 | Elcelyx Therapeutics, Inc. | Biguanide compositions and methods of treating metabolic disorders |
| WO2012094636A2 (en) | 2011-01-07 | 2012-07-12 | Elcelyx Therapeutics, Inc. | Chemosensory receptor ligand-based therapies |
| US9211263B2 (en) | 2012-01-06 | 2015-12-15 | Elcelyx Therapeutics, Inc. | Compositions and methods of treating metabolic disorders |
| US9572784B2 (en) | 2011-01-07 | 2017-02-21 | Elcelyx Therapeutics, Inc. | Compositions comprising statins, biguanides and further agents for reducing cardiometabolic risk |
| US11974971B2 (en) | 2011-01-07 | 2024-05-07 | Anji Pharmaceuticals Inc. | Compositions and methods for treating metabolic disorders |
| CN102188429A (zh) * | 2011-05-20 | 2011-09-21 | 吴四清 | 一种治疗糖尿病的药物组合物 |
| CN102357088A (zh) | 2011-10-26 | 2012-02-22 | 河北山姆士药业有限公司 | 盐酸二甲双胍肠溶片 |
| BR112014016808B1 (pt) | 2012-01-06 | 2022-01-11 | Anji Pharma (Us) Llc | Uso de um composto de biguanida para a fabricação de um medicamento para baixar os níveis de glicose no sangue e para o tratamento de um distúrbio do metabolismo de glicose |
| CN104349773A (zh) | 2012-01-06 | 2015-02-11 | 埃尔舍利克斯治疗公司 | 用于治疗代谢性病症的组合物和方法 |
| EP2941245B1 (en) | 2013-01-05 | 2024-06-26 | Anji Pharmaceuticals Inc. | Delayed-release composition comprising biguanide |
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2012
- 2012-07-11 BR BR112014016808-3A patent/BR112014016808B1/pt active IP Right Grant
- 2012-07-11 EA EA201491335A patent/EA201491335A1/ru unknown
- 2012-07-11 KR KR1020147021875A patent/KR102035879B1/ko active Active
- 2012-07-11 KR KR1020197030360A patent/KR20190120430A/ko not_active Ceased
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- 2012-07-11 AU AU2012363873A patent/AU2012363873B2/en active Active
- 2012-07-11 CN CN201280070968.0A patent/CN104254325A/zh active Pending
- 2012-07-11 JP JP2014551231A patent/JP2015503582A/ja not_active Withdrawn
- 2012-07-11 WO PCT/US2012/046335 patent/WO2013103384A1/en not_active Ceased
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- 2012-07-11 CN CN201910957458.9A patent/CN110693868A/zh active Pending
- 2012-07-11 KR KR1020237020116A patent/KR20230095124A/ko not_active Ceased
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- 2021-07-21 JP JP2021120385A patent/JP2021169522A/ja active Pending
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