MX2019015095A - Metodo de sintesis para producir compuestos de cis-imidazolina enantiomericamente puros para uso farmaceutico. - Google Patents
Metodo de sintesis para producir compuestos de cis-imidazolina enantiomericamente puros para uso farmaceutico.Info
- Publication number
- MX2019015095A MX2019015095A MX2019015095A MX2019015095A MX2019015095A MX 2019015095 A MX2019015095 A MX 2019015095A MX 2019015095 A MX2019015095 A MX 2019015095A MX 2019015095 A MX2019015095 A MX 2019015095A MX 2019015095 A MX2019015095 A MX 2019015095A
- Authority
- MX
- Mexico
- Prior art keywords
- cis
- synthesis method
- enantiomerically pure
- pharmaceutical use
- pure cis
- Prior art date
Links
- 238000001308 synthesis method Methods 0.000 title 1
- HBAQYPYDRFILMT-UHFFFAOYSA-N 8-[3-(1-cyclopropylpyrazol-4-yl)-1H-pyrazolo[4,3-d]pyrimidin-5-yl]-3-methyl-3,8-diazabicyclo[3.2.1]octan-2-one Chemical class C1(CC1)N1N=CC(=C1)C1=NNC2=C1N=C(N=C2)N1C2C(N(CC1CC2)C)=O HBAQYPYDRFILMT-UHFFFAOYSA-N 0.000 abstract 1
- 206010028980 Neoplasm Diseases 0.000 abstract 1
- 239000002253 acid Substances 0.000 abstract 1
- 230000015572 biosynthetic process Effects 0.000 abstract 1
- 201000011510 cancer Diseases 0.000 abstract 1
- 230000000295 complement effect Effects 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 238000000034 method Methods 0.000 abstract 1
- 239000000203 mixture Substances 0.000 abstract 1
- 230000037361 pathway Effects 0.000 abstract 1
- 239000002243 precursor Substances 0.000 abstract 1
- 238000010956 selective crystallization Methods 0.000 abstract 1
- 230000009758 senescence Effects 0.000 abstract 1
- 238000003786 synthesis reaction Methods 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/06—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P39/00—General protective or antinoxious agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
- C07D233/54—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
- C07D233/54—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
- C07D233/64—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with substituted hydrocarbon radicals attached to ring carbon atoms, e.g. histidine
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Toxicology (AREA)
- Epidemiology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Abstract
Se describe un método para la síntesis enantioselectiva de cis-imidazolinas y estructuras relacionadas a través de la resolución quiral. Se usa un ácido quiral para separar los precursores enantioméricos de las cis-imidazolinas de una mezcla racémica por cristalización selectiva. Ambos enantiómeros pueden ciclarse en la cis-imidazolina deseada por vías complementarias. Los compuestos se pueden sintetizar con un exceso enantiomérico de incluso un 99% y se pueden usar para tratar el cáncer, matar células senescentes o tratar afecciones asociadas a la senescencia.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| PCT/CN2017/088787 WO2018227620A1 (en) | 2017-06-16 | 2017-06-16 | Synthesis method for producing enantiomerically pure cis-imidazoline compounds for pharmaceutical use |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| MX2019015095A true MX2019015095A (es) | 2020-08-17 |
Family
ID=62235319
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| MX2019015095A MX2019015095A (es) | 2017-06-16 | 2017-06-16 | Metodo de sintesis para producir compuestos de cis-imidazolina enantiomericamente puros para uso farmaceutico. |
Country Status (10)
| Country | Link |
|---|---|
| US (3) | US9988368B1 (es) |
| EP (1) | EP3512831A4 (es) |
| JP (1) | JP6848055B2 (es) |
| KR (1) | KR20200035944A (es) |
| CN (1) | CN110088081A (es) |
| AU (1) | AU2017418538B2 (es) |
| CA (1) | CA3033850C (es) |
| MX (1) | MX2019015095A (es) |
| SG (1) | SG11201911909UA (es) |
| WO (1) | WO2018227620A1 (es) |
Families Citing this family (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| KR20200035944A (ko) * | 2017-06-16 | 2020-04-06 | 유니티 바이오테크놀로지, 인크. | 약제학적 용도를 위해 에난티오머적으로 순수한 시스-이미다졸린 화합물을 제조하기 위한 합성 방법 |
Family Cites Families (16)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JPS6112651A (ja) * | 1984-06-29 | 1986-01-21 | Kazuhiko Saigo | 光学活性１，２―ジフェニルエチレンジアミンの製造方法 |
| JP2002128745A (ja) * | 2000-10-18 | 2002-05-09 | Mitsui Chemicals Inc | 光学活性１，２−ビス（２，４，６−トリメチルフェニル）−１，２−エタンジアミンの製造方法 |
| DE60225719T2 (de) * | 2001-12-18 | 2009-04-23 | F. Hoffmann-La Roche Ag | Cis-2,4,5- triphenyl-imidazoline und ihre verwendung bei der behandlung von tumoren |
| DE60227108D1 (de) | 2001-12-18 | 2008-07-24 | Hoffmann La Roche | Cis-imidazoline als mdm2-hemmer |
| US7893278B2 (en) | 2004-06-17 | 2011-02-22 | Hoffman-La Roche Inc. | CIS-imidazolines |
| CN101103004A (zh) * | 2004-06-17 | 2008-01-09 | 霍夫曼-拉罗奇有限公司 | 新型顺式-咪唑啉类化合物 |
| EP2130822A1 (en) | 2005-12-01 | 2009-12-09 | F. Hoffmann-La Roche AG | 2,4,5-triphenyl imidazoline derivatives as inhibitors of the interaction between p53 and mdm2 proteins for use as anticancer agents |
| KR101015073B1 (ko) | 2006-01-18 | 2011-02-16 | 에프. 호프만-라 로슈 아게 | Ｍｄｍ2 억제제로서의시스-4,5-비아릴-2-헤테로시클릭-이미다졸린 |
| WO2008065068A2 (en) * | 2006-11-27 | 2008-06-05 | Novartis Ag | Substituted dihydroimidazoles and their use in the treatment of tumors |
| US8889863B2 (en) * | 2010-07-16 | 2014-11-18 | Vanderbilt University | Stereoselective methods, catalysts and intermediates for the synthesis of (−)-Nutlin-3 and related compounds |
| WO2012047587A2 (en) | 2010-09-27 | 2012-04-12 | Serrata, Llc | Mdm2 inhibitors for treatment of ocular conditions |
| US9993472B2 (en) | 2014-01-28 | 2018-06-12 | Unity Biotechnology, Inc. | Treatment for osteoarthritis in a joint by administering a means for inhibiting MDM2 |
| WO2015116735A1 (en) | 2014-01-28 | 2015-08-06 | Mayo Foundation For Medical Education And Research | Methods and combinations for killing senescent cells and for treating senescence-associated diseases and disorders |
| CN103923067B (zh) | 2014-04-29 | 2016-08-24 | 湖北工业大学 | 一种MdmX/Mdm2的小分子抑制剂及制备方法和应用 |
| WO2015184383A1 (en) * | 2014-05-29 | 2015-12-03 | St. Jude Children's Research Hospital | Aryl-substituted imidazoles and methods of making and using same |
| KR20200035944A (ko) * | 2017-06-16 | 2020-04-06 | 유니티 바이오테크놀로지, 인크. | 약제학적 용도를 위해 에난티오머적으로 순수한 시스-이미다졸린 화합물을 제조하기 위한 합성 방법 |
-
2017
- 2017-06-16 KR KR1020207001176A patent/KR20200035944A/ko not_active Application Discontinuation
- 2017-06-16 WO PCT/CN2017/088787 patent/WO2018227620A1/en unknown
- 2017-06-16 MX MX2019015095A patent/MX2019015095A/es unknown
- 2017-06-16 CN CN201780060930.8A patent/CN110088081A/zh active Pending
- 2017-06-16 SG SG11201911909UA patent/SG11201911909UA/en unknown
- 2017-06-16 EP EP17913630.4A patent/EP3512831A4/en not_active Withdrawn
- 2017-06-16 CA CA3033850A patent/CA3033850C/en not_active Expired - Fee Related
- 2017-06-16 JP JP2019518436A patent/JP6848055B2/ja active Active
- 2017-06-16 AU AU2017418538A patent/AU2017418538B2/en not_active Ceased
- 2017-08-31 US US15/693,061 patent/US9988368B1/en active Active
-
2018
- 2018-04-17 US US15/955,474 patent/US10329279B2/en not_active Expired - Fee Related
-
2019
- 2019-05-17 US US16/415,862 patent/US20190270726A1/en not_active Abandoned
Also Published As
| Publication number | Publication date |
|---|---|
| CN110088081A (zh) | 2019-08-02 |
| CA3033850A1 (en) | 2018-12-20 |
| SG11201911909UA (en) | 2020-01-30 |
| JP6848055B2 (ja) | 2021-03-24 |
| US9988368B1 (en) | 2018-06-05 |
| AU2017418538B2 (en) | 2021-10-21 |
| US20190270726A1 (en) | 2019-09-05 |
| AU2017418538A1 (en) | 2020-01-16 |
| KR20200035944A (ko) | 2020-04-06 |
| US10329279B2 (en) | 2019-06-25 |
| EP3512831A1 (en) | 2019-07-24 |
| EP3512831A4 (en) | 2019-07-31 |
| JP2019531304A (ja) | 2019-10-31 |
| US20180362510A1 (en) | 2018-12-20 |
| WO2018227620A1 (en) | 2018-12-20 |
| CA3033850C (en) | 2020-02-11 |
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