AR092948A1 - Procesos en fase liquida para la elaboracion de depsipeptidos macrociclicos y de intermediarios - Google Patents
Procesos en fase liquida para la elaboracion de depsipeptidos macrociclicos y de intermediariosInfo
- Publication number
- AR092948A1 AR092948A1 ARP130103654A ARP130103654A AR092948A1 AR 092948 A1 AR092948 A1 AR 092948A1 AR P130103654 A ARP130103654 A AR P130103654A AR P130103654 A ARP130103654 A AR P130103654A AR 092948 A1 AR092948 A1 AR 092948A1
- Authority
- AR
- Argentina
- Prior art keywords
- formula
- compound
- salt
- amino acid
- prot
- Prior art date
Links
- 238000000034 method Methods 0.000 title abstract 8
- 239000007791 liquid phase Substances 0.000 title abstract 2
- 108010002156 Depsipeptides Proteins 0.000 title 1
- 150000001875 compounds Chemical class 0.000 abstract 31
- 150000003839 salts Chemical class 0.000 abstract 8
- 229940024606 amino acid Drugs 0.000 abstract 7
- 235000001014 amino acid Nutrition 0.000 abstract 7
- 150000001413 amino acids Chemical class 0.000 abstract 7
- 125000006239 protecting group Chemical group 0.000 abstract 7
- AGPKZVBTJJNPAG-WHFBIAKZSA-N L-isoleucine Chemical compound CC[C@H](C)[C@H](N)C(O)=O AGPKZVBTJJNPAG-WHFBIAKZSA-N 0.000 abstract 3
- ROHFNLRQFUQHCH-YFKPBYRVSA-N L-leucine Chemical compound CC(C)C[C@H](N)C(O)=O ROHFNLRQFUQHCH-YFKPBYRVSA-N 0.000 abstract 3
- KZSNJWFQEVHDMF-BYPYZUCNSA-N L-valine Chemical compound CC(C)[C@H](N)C(O)=O KZSNJWFQEVHDMF-BYPYZUCNSA-N 0.000 abstract 3
- ROHFNLRQFUQHCH-UHFFFAOYSA-N Leucine Natural products CC(C)CC(N)C(O)=O ROHFNLRQFUQHCH-UHFFFAOYSA-N 0.000 abstract 3
- KZSNJWFQEVHDMF-UHFFFAOYSA-N Valine Natural products CC(C)C(N)C(O)=O KZSNJWFQEVHDMF-UHFFFAOYSA-N 0.000 abstract 3
- 125000002252 acyl group Chemical group 0.000 abstract 3
- 229960000310 isoleucine Drugs 0.000 abstract 3
- AGPKZVBTJJNPAG-UHFFFAOYSA-N isoleucine Natural products CCC(C)C(N)C(O)=O AGPKZVBTJJNPAG-UHFFFAOYSA-N 0.000 abstract 3
- 238000002360 preparation method Methods 0.000 abstract 3
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 abstract 3
- 239000004474 valine Substances 0.000 abstract 3
- 125000004209 (C1-C8) alkyl group Chemical group 0.000 abstract 2
- 125000003277 amino group Chemical group 0.000 abstract 2
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 abstract 2
- 125000002887 hydroxy group Chemical group [H]O* 0.000 abstract 2
- 125000004430 oxygen atom Chemical group O* 0.000 abstract 2
- 239000012071 phase Substances 0.000 abstract 2
- 238000007086 side reaction Methods 0.000 abstract 2
- DCXYFEDJOCDNAF-UHFFFAOYSA-N Asparagine Natural products OC(=O)C(N)CC(N)=O DCXYFEDJOCDNAF-UHFFFAOYSA-N 0.000 abstract 1
- DCXYFEDJOCDNAF-REOHCLBHSA-N L-asparagine Chemical compound OC(=O)[C@@H](N)CC(N)=O DCXYFEDJOCDNAF-REOHCLBHSA-N 0.000 abstract 1
- ZDXPYRJPNDTMRX-VKHMYHEASA-N L-glutamine Chemical compound OC(=O)[C@@H](N)CCC(N)=O ZDXPYRJPNDTMRX-VKHMYHEASA-N 0.000 abstract 1
- COLNVLDHVKWLRT-QMMMGPOBSA-N L-phenylalanine Chemical compound OC(=O)[C@@H](N)CC1=CC=CC=C1 COLNVLDHVKWLRT-QMMMGPOBSA-N 0.000 abstract 1
- OUYCCCASQSFEME-QMMMGPOBSA-N L-tyrosine Chemical compound OC(=O)[C@@H](N)CC1=CC=C(O)C=C1 OUYCCCASQSFEME-QMMMGPOBSA-N 0.000 abstract 1
- 125000003172 aldehyde group Chemical group 0.000 abstract 1
- 229960001230 asparagine Drugs 0.000 abstract 1
- 235000009582 asparagine Nutrition 0.000 abstract 1
- 230000015572 biosynthetic process Effects 0.000 abstract 1
- 239000006227 byproduct Substances 0.000 abstract 1
- 125000003917 carbamoyl group Chemical group [H]N([H])C(*)=O 0.000 abstract 1
- 229910052799 carbon Inorganic materials 0.000 abstract 1
- 125000004432 carbon atom Chemical group C* 0.000 abstract 1
- 125000002915 carbonyl group Chemical group [*:2]C([*:1])=O 0.000 abstract 1
- 230000008878 coupling Effects 0.000 abstract 1
- 238000010168 coupling process Methods 0.000 abstract 1
- 238000005859 coupling reaction Methods 0.000 abstract 1
- 125000004122 cyclic group Chemical group 0.000 abstract 1
- 125000000524 functional group Chemical group 0.000 abstract 1
- ZDXPYRJPNDTMRX-UHFFFAOYSA-N glutamine Natural products OC(=O)C(N)CCC(N)=O ZDXPYRJPNDTMRX-UHFFFAOYSA-N 0.000 abstract 1
- 229910052739 hydrogen Inorganic materials 0.000 abstract 1
- 239000001257 hydrogen Substances 0.000 abstract 1
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 abstract 1
- 230000003647 oxidation Effects 0.000 abstract 1
- 238000007254 oxidation reaction Methods 0.000 abstract 1
- COLNVLDHVKWLRT-UHFFFAOYSA-N phenylalanine Natural products OC(=O)C(N)CC1=CC=CC=C1 COLNVLDHVKWLRT-UHFFFAOYSA-N 0.000 abstract 1
- 239000000047 product Substances 0.000 abstract 1
- 239000000376 reactant Substances 0.000 abstract 1
- 125000000547 substituted alkyl group Chemical group 0.000 abstract 1
- 238000003786 synthesis reaction Methods 0.000 abstract 1
- OUYCCCASQSFEME-UHFFFAOYSA-N tyrosine Natural products OC(=O)C(N)CC1=CC=C(O)C=C1 OUYCCCASQSFEME-UHFFFAOYSA-N 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K11/00—Depsipeptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C235/00—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms
- C07C235/70—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups and doubly-bound oxygen atoms bound to the same carbon skeleton
- C07C235/72—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups and doubly-bound oxygen atoms bound to the same carbon skeleton with the carbon atoms of the carboxamide groups bound to acyclic carbon atoms
- C07C235/74—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups and doubly-bound oxygen atoms bound to the same carbon skeleton with the carbon atoms of the carboxamide groups bound to acyclic carbon atoms of a saturated carbon skeleton
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K11/00—Depsipeptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
- C07K11/02—Depsipeptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof cyclic, e.g. valinomycins ; Derivatives thereof
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
- C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
- C07K5/08—Tripeptides
- C07K5/0819—Tripeptides with the first amino acid being acidic
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K7/00—Peptides having 5 to 20 amino acids in a fully defined sequence; Derivatives thereof
- C07K7/04—Linear peptides containing only normal peptide links
- C07K7/06—Linear peptides containing only normal peptide links having 5 to 11 amino acids
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K38/00—Medicinal preparations containing peptides
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Molecular Biology (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Biophysics (AREA)
- General Health & Medical Sciences (AREA)
- Genetics & Genomics (AREA)
- Medicinal Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Biochemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Peptides Or Proteins (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
- Preparation Of Compounds By Using Micro-Organisms (AREA)
- Analytical Chemistry (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201261711284P | 2012-10-09 | 2012-10-09 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR092948A1 true AR092948A1 (es) | 2015-05-06 |
Family
ID=49880854
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP130103654A AR092948A1 (es) | 2012-10-09 | 2013-10-09 | Procesos en fase liquida para la elaboracion de depsipeptidos macrociclicos y de intermediarios |
Country Status (14)
| Country | Link |
|---|---|
| US (2) | US9067978B2 (https=) |
| EP (1) | EP2906585A2 (https=) |
| JP (1) | JP2015533156A (https=) |
| KR (1) | KR20150065709A (https=) |
| CN (1) | CN104703997A (https=) |
| AR (1) | AR092948A1 (https=) |
| AU (1) | AU2013328284B2 (https=) |
| BR (1) | BR112015007196A2 (https=) |
| CA (1) | CA2884393A1 (https=) |
| EA (1) | EA201590698A1 (https=) |
| IN (1) | IN2015DN01811A (https=) |
| MX (1) | MX2015004629A (https=) |
| TW (1) | TW201418278A (https=) |
| WO (1) | WO2014057418A2 (https=) |
Families Citing this family (11)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| MY151973A (en) | 2007-08-17 | 2014-07-31 | Novartis Ag | Cyclic depsipeptides |
| US8680054B2 (en) | 2011-04-20 | 2014-03-25 | Novartis Ag | Suspension type topical formulations comprising cyclic depsipeptide |
| US8614289B2 (en) | 2011-04-20 | 2013-12-24 | Novartis Ag | Processes for the manufacture of macrocyclic depsipeptides and new intermediates |
| US8987413B2 (en) * | 2012-10-09 | 2015-03-24 | Novartis Ag | Aldehyde acetal based processes for the manufacture of macrocyclic depsipeptides and new intermediates |
| US9067978B2 (en) | 2012-10-09 | 2015-06-30 | Novartis Ag | Solution phase processes for the manufacture of macrocyclic depsipeptides and new intermediates |
| KR102337328B1 (ko) | 2015-12-21 | 2021-12-10 | 텍사스 테크 유니버시티 시스템 | 용액상 gap 펩타이드 합성을 위한 시스템 및 방법 |
| WO2019217116A1 (en) * | 2018-05-06 | 2019-11-14 | Gap Peptides Llc | Method for solution-phase peptide synthesis |
| US12024537B2 (en) | 2018-05-31 | 2024-07-02 | Sederma | Compositions and methods for chemical synthesis |
| US11643438B2 (en) | 2018-07-20 | 2023-05-09 | The Board Of Regents Of The University Of Oklahoma | Antimicrobial peptides and methods of use |
| EP3917937A4 (en) | 2019-02-01 | 2022-11-23 | Sederma | SYNTHETIC STRATEGY FOR A SPLIT PROTECTION GROUP |
| JP7162853B1 (ja) * | 2021-07-02 | 2022-10-31 | ペプチスター株式会社 | 液相ペプチド合成用担体結合ペプチドの分析方法 |
Family Cites Families (25)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE3043252C2 (de) | 1980-11-15 | 1982-12-02 | Degussa Ag, 6000 Frankfurt | Cyclische Acetale von N-Acylglutaminsäure -γ- semialdehyden, Verfahren zu deren Herstellung und ihre Verwendung |
| US5595756A (en) | 1993-12-22 | 1997-01-21 | Inex Pharmaceuticals Corporation | Liposomal compositions for enhanced retention of bioactive agents |
| DE4421113A1 (de) | 1994-06-16 | 1995-12-21 | Biotechnolog Forschung Gmbh | Chondramide, Gewinnungsverfahren, Mittel mit Chondramiden und Mischkultur zur Chondramid-Gewinnung |
| DE19828043A1 (de) | 1998-06-24 | 1999-12-30 | Bayer Ag | Ektoparasitizide Mittel |
| JP2000154198A (ja) | 1998-11-20 | 2000-06-06 | Nisshin Flour Milling Co Ltd | 環状デプシペプチドの固相合成方法及びその中間体 |
| GB0108234D0 (en) | 2001-04-02 | 2001-05-23 | Pharma Mar Sa | Process for producing trunkamide A compounds |
| US20040110228A1 (en) | 2002-04-01 | 2004-06-10 | Mcalpine Shelli R. | Combinatorial organic synthesis of unique biologically active compounds |
| KR101205257B1 (ko) | 2003-06-06 | 2012-11-27 | 아렉시스 악티에볼라그 | 피부 상태 또는 암 치료를 위한 ｓｃｃｅ 저해제로서의 융합된 헤테로사이클 화합물의 용도 |
| GB0322140D0 (en) | 2003-09-22 | 2003-10-22 | Pfizer Ltd | Combinations |
| EP1716248A1 (en) | 2004-02-03 | 2006-11-02 | Bayer HealthCare AG | Diagnostics and therapeutics for diseases associated with kallikrein 7 (klk7) |
| CA2651796A1 (en) | 2006-02-27 | 2007-09-07 | Arizona Board Of Regents For And On Behalf Of Arizona State University | Identification and use of novopeptides for the treatment of cancer |
| GB0715750D0 (en) | 2007-08-13 | 2007-09-19 | Karus Therapeutics Ltd | Chemical compounds |
| WO2009024528A1 (en) | 2007-08-17 | 2009-02-26 | Novartis Ag | Use of cyclic depsipeptides to inhibit kallikrein 7 |
| MY151973A (en) * | 2007-08-17 | 2014-07-31 | Novartis Ag | Cyclic depsipeptides |
| DE102007052391A1 (de) | 2007-10-31 | 2009-05-07 | Henkel Ag & Co. Kgaa | Mattwachs |
| US20110112121A1 (en) | 2009-07-06 | 2011-05-12 | Joerg Berghausen | Pharmaceutical Compositions and Solid Forms |
| KR101004362B1 (ko) | 2010-03-19 | 2010-12-28 | 가톨릭대학교 산학협력단 | 자가 면역 질환 예방 및 치료용 ＴＮＦ－α와 ＴＷＥＡＫ 이중 길항제 |
| US20120064136A1 (en) | 2010-09-10 | 2012-03-15 | Nanobio Corporation | Anti-aging and wrinkle treatment methods using nanoemulsion compositions |
| WO2012035468A2 (en) | 2010-09-14 | 2012-03-22 | Trima - Israel Pharmaceutical Products Maabarot Ltd. | Foamable topical composition |
| EP2667854B1 (en) | 2011-01-24 | 2019-01-16 | Anterios, Inc. | Nanoparticle compositions |
| KR20140005998A (ko) | 2011-01-24 | 2014-01-15 | 안테리오스, 인코퍼레이티드 | 나노입자 조성물, 이의 제형, 및 그의 용도 |
| US8614289B2 (en) * | 2011-04-20 | 2013-12-24 | Novartis Ag | Processes for the manufacture of macrocyclic depsipeptides and new intermediates |
| US8680054B2 (en) | 2011-04-20 | 2014-03-25 | Novartis Ag | Suspension type topical formulations comprising cyclic depsipeptide |
| US9067978B2 (en) | 2012-10-09 | 2015-06-30 | Novartis Ag | Solution phase processes for the manufacture of macrocyclic depsipeptides and new intermediates |
| US8987413B2 (en) * | 2012-10-09 | 2015-03-24 | Novartis Ag | Aldehyde acetal based processes for the manufacture of macrocyclic depsipeptides and new intermediates |
-
2013
- 2013-10-04 US US14/045,844 patent/US9067978B2/en active Active
- 2013-10-08 IN IN1811DEN2015 patent/IN2015DN01811A/en unknown
- 2013-10-08 BR BR112015007196A patent/BR112015007196A2/pt not_active IP Right Cessation
- 2013-10-08 CA CA2884393A patent/CA2884393A1/en not_active Abandoned
- 2013-10-08 EA EA201590698A patent/EA201590698A1/ru unknown
- 2013-10-08 WO PCT/IB2013/059196 patent/WO2014057418A2/en not_active Ceased
- 2013-10-08 CN CN201380051965.7A patent/CN104703997A/zh active Pending
- 2013-10-08 KR KR1020157008834A patent/KR20150065709A/ko not_active Withdrawn
- 2013-10-08 AU AU2013328284A patent/AU2013328284B2/en not_active Ceased
- 2013-10-08 EP EP13812092.8A patent/EP2906585A2/en not_active Withdrawn
- 2013-10-08 JP JP2015536260A patent/JP2015533156A/ja active Pending
- 2013-10-08 MX MX2015004629A patent/MX2015004629A/es unknown
- 2013-10-08 TW TW102136392A patent/TW201418278A/zh unknown
- 2013-10-09 AR ARP130103654A patent/AR092948A1/es unknown
-
2015
- 2015-04-15 US US14/686,899 patent/US9493512B2/en not_active Expired - Fee Related
Also Published As
| Publication number | Publication date |
|---|---|
| BR112015007196A2 (pt) | 2017-07-04 |
| US9493512B2 (en) | 2016-11-15 |
| JP2015533156A (ja) | 2015-11-19 |
| US20150218224A1 (en) | 2015-08-06 |
| WO2014057418A2 (en) | 2014-04-17 |
| IN2015DN01811A (https=) | 2015-05-29 |
| WO2014057418A3 (en) | 2014-07-10 |
| AU2013328284A1 (en) | 2015-03-12 |
| US9067978B2 (en) | 2015-06-30 |
| EP2906585A2 (en) | 2015-08-19 |
| CN104703997A (zh) | 2015-06-10 |
| AU2013328284B2 (en) | 2016-07-14 |
| EA201590698A1 (ru) | 2015-07-30 |
| KR20150065709A (ko) | 2015-06-15 |
| CA2884393A1 (en) | 2014-04-17 |
| US20140100355A1 (en) | 2014-04-10 |
| TW201418278A (zh) | 2014-05-16 |
| MX2015004629A (es) | 2015-07-14 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FB | Suspension of granting procedure |