AR065666A1 - Metodos e intermediarios para la sintesis de inhibidores selectivos de dpp-iv - Google Patents
Metodos e intermediarios para la sintesis de inhibidores selectivos de dpp-ivInfo
- Publication number
- AR065666A1 AR065666A1 ARP080100973A ARP080100973A AR065666A1 AR 065666 A1 AR065666 A1 AR 065666A1 AR P080100973 A ARP080100973 A AR P080100973A AR P080100973 A ARP080100973 A AR P080100973A AR 065666 A1 AR065666 A1 AR 065666A1
- Authority
- AR
- Argentina
- Prior art keywords
- salt
- formula
- synthesis
- compound
- methods
- Prior art date
Links
- 230000015572 biosynthetic process Effects 0.000 title abstract 3
- 239000003112 inhibitor Substances 0.000 title abstract 3
- 238000000034 method Methods 0.000 title abstract 3
- 238000003786 synthesis reaction Methods 0.000 title abstract 2
- 150000003839 salts Chemical class 0.000 abstract 4
- -1 carboxylate salt Chemical class 0.000 abstract 3
- 150000001875 compounds Chemical class 0.000 abstract 3
- 102000016622 Dipeptidyl Peptidase 4 Human genes 0.000 abstract 2
- 101000930822 Giardia intestinalis Dipeptidyl-peptidase 4 Proteins 0.000 abstract 2
- RVMGCVMWQUXDQQ-WCCKRBBISA-N N1[C@H](C(=O)O)CCC1.[B] Chemical class N1[C@H](C(=O)O)CCC1.[B] RVMGCVMWQUXDQQ-WCCKRBBISA-N 0.000 abstract 2
- 125000002887 hydroxy group Chemical group [H]O* 0.000 abstract 2
- ZOXJGFHDIHLPTG-UHFFFAOYSA-N Boron Chemical group [B] ZOXJGFHDIHLPTG-UHFFFAOYSA-N 0.000 abstract 1
- XBPCUCUWBYBCDP-UHFFFAOYSA-N Dicyclohexylamine Chemical class C1CCCCC1NC1CCCCC1 XBPCUCUWBYBCDP-UHFFFAOYSA-N 0.000 abstract 1
- 229940124639 Selective inhibitor Drugs 0.000 abstract 1
- 229910052796 boron Inorganic materials 0.000 abstract 1
- 150000001768 cations Chemical class 0.000 abstract 1
- 125000004122 cyclic group Chemical group 0.000 abstract 1
- 206010012601 diabetes mellitus Diseases 0.000 abstract 1
- 239000000543 intermediate Substances 0.000 abstract 1
- 125000006239 protecting group Chemical group 0.000 abstract 1
- 159000000000 sodium salts Chemical class 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
- C07F5/00—Compounds containing elements of Groups 3 or 13 of the Periodic Table
- C07F5/02—Boron compounds
- C07F5/025—Boronic and borinic acid compounds
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
- A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
- C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D207/04—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
- C07D207/10—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D207/14—Nitrogen atoms not forming part of a nitro radical
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Diabetes (AREA)
- General Chemical & Material Sciences (AREA)
- Emergency Medicine (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Engineering & Computer Science (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Endocrinology (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Pyrrole Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Abstract
Se proporcionan métodos e intermediarios para la síntesis de inhibidores selectivos de la dipeptidil peptidasa IV (DPP-IV). La union de una sal de carboxilato con un derivado de boro-prolina, provee una forma protegida de un inhibidor de DDP-IV, quepuede desbloquearse para proporcionar el compuesto medicinal. La sal de carboxilato puede ser una forma cristalina de una sal de sodio o una sal de diciclohexilamonio. El inhibidor puede usarse en el tratamiento de la diabetes. Reivindicacion 1:Un método para preparar un compuesto de formula (1) donde cada PG es independientemente un grupo protector de N, y Ra y Rb son cada uno hidroxilo, o una sal de éste, o un grupo que puede convertirse en hidroxilo, o una sal de éste, o Ra y Rb, juntocon un átomo de boro al que están unidos, forman una estructura cíclica que puede convertirse en B(OH)2, o una sal de este caracterizado porque comprende: poner en contacto una sal de carboxilato de formula (2) donde M es un cation y una boro-prolina protegida de formula (3), o una sal de ésta bajo condiciones apropiadas para obtener la formacion de un enlace amida para proporcionar el compuesto de formula (1).
Applications Claiming Priority (4)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US89384207P | 2007-03-08 | 2007-03-08 | |
| US95922607P | 2007-07-12 | 2007-07-12 | |
| US2348708P | 2008-01-25 | 2008-01-25 | |
| US2950608P | 2008-02-18 | 2008-02-18 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR065666A1 true AR065666A1 (es) | 2009-06-24 |
Family
ID=39711954
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP080100973A AR065666A1 (es) | 2007-03-08 | 2008-03-07 | Metodos e intermediarios para la sintesis de inhibidores selectivos de dpp-iv |
Country Status (7)
| Country | Link |
|---|---|
| EP (1) | EP2173709A2 (es) |
| CN (1) | CN101679238A (es) |
| AR (1) | AR065666A1 (es) |
| CA (1) | CA2680133A1 (es) |
| MX (1) | MX2009009575A (es) |
| TW (1) | TW200843784A (es) |
| WO (1) | WO2008109681A2 (es) |
Families Citing this family (13)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP1919485A4 (en) | 2005-08-01 | 2011-03-23 | Phenomix Corp | METHOD FOR PRODUCING HETEROCYCLIC BORONIC ACIDS AND ITS DERIVATIVES |
| CL2007002499A1 (es) | 2006-08-30 | 2008-03-14 | Phenomix Corp | Sales citrato y tartrato de compuestos derivados de acido pirrolidinilaminoacetilpirrolidinboronico, inhibidores de dpp-iv; metodo de preparacion; forma solida; combinacion farmaceutica, util para el tratamiento de diabetes. |
| UY32030A (es) | 2008-08-06 | 2010-03-26 | Boehringer Ingelheim Int | "tratamiento para diabetes en pacientes inapropiados para terapia con metformina" |
| JP5906086B2 (ja) | 2008-08-15 | 2016-04-20 | 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 | Ｆａｂ関連疾患の治療に用いるためのプリン誘導体 |
| TW201036975A (en) | 2009-01-07 | 2010-10-16 | Boehringer Ingelheim Int | Treatment for diabetes in patients with inadequate glycemic control despite metformin therapy |
| TWI466672B (zh) | 2009-01-29 | 2015-01-01 | Boehringer Ingelheim Int | 小兒科病人糖尿病之治療 |
| CN106177958A (zh) | 2009-02-13 | 2016-12-07 | 勃林格殷格翰国际有限公司 | 包含dpp‑4抑制剂(利拉列汀)任选地组合其它抗糖尿病药的抗糖尿病药物 |
| JP2013512229A (ja) | 2009-11-27 | 2013-04-11 | 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 | 遺伝子型が同定された糖尿病患者のリナグリプチン等のｄｄｐ−ｉｖ阻害薬による治療 |
| 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 |
| NZ602921A (en) | 2010-05-05 | 2016-01-29 | Boehringer Ingelheim Int | Combination therapy comprising the administration of a glp-1 receptor agonist and a ddp-4 inhibitor |
| MX2012014247A (es) | 2010-06-24 | 2013-01-18 | Boehringer Ingelheim Int | Terapia para la diabetes. |
| 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 |
| CN111533675B (zh) * | 2019-11-29 | 2021-09-28 | 杭州华东医药集团新药研究院有限公司 | 杂环硼酸化合物的杂质及其控制方法 |
Family Cites Families (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US7317109B2 (en) * | 2003-11-12 | 2008-01-08 | Phenomix Corporation | Pyrrolidine compounds and methods for selective inhibition of dipeptidyl peptidase-IV |
| EP1919485A4 (en) * | 2005-08-01 | 2011-03-23 | Phenomix Corp | METHOD FOR PRODUCING HETEROCYCLIC BORONIC ACIDS AND ITS DERIVATIVES |
-
2008
- 2008-03-05 MX MX2009009575A patent/MX2009009575A/es not_active Application Discontinuation
- 2008-03-05 CA CA002680133A patent/CA2680133A1/en not_active Abandoned
- 2008-03-05 CN CN200880015066A patent/CN101679238A/zh active Pending
- 2008-03-05 EP EP08743692A patent/EP2173709A2/en not_active Withdrawn
- 2008-03-05 WO PCT/US2008/055927 patent/WO2008109681A2/en active Application Filing
- 2008-03-07 TW TW097108175A patent/TW200843784A/zh unknown
- 2008-03-07 AR ARP080100973A patent/AR065666A1/es not_active Application Discontinuation
Also Published As
| Publication number | Publication date |
|---|---|
| WO2008109681A2 (en) | 2008-09-12 |
| WO2008109681A3 (en) | 2008-11-13 |
| MX2009009575A (es) | 2009-11-12 |
| CN101679238A (zh) | 2010-03-24 |
| EP2173709A2 (en) | 2010-04-14 |
| CA2680133A1 (en) | 2008-09-12 |
| TW200843784A (en) | 2008-11-16 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FA | Abandonment or withdrawal |