AR085052A1 - Metodos para producir un compuesto profarmaco inhibidor de la union al vih e intermediarios - Google Patents
Metodos para producir un compuesto profarmaco inhibidor de la union al vih e intermediariosInfo
- Publication number
- AR085052A1 AR085052A1 ARP120100313A ARP120100313A AR085052A1 AR 085052 A1 AR085052 A1 AR 085052A1 AR P120100313 A ARP120100313 A AR P120100313A AR P120100313 A ARP120100313 A AR P120100313A AR 085052 A1 AR085052 A1 AR 085052A1
- Authority
- AR
- Argentina
- Prior art keywords
- compound
- formula
- produce
- converting
- propharm
- Prior art date
Links
- 150000001875 compounds Chemical class 0.000 title abstract 32
- 230000002401 inhibitory effect Effects 0.000 title 1
- NAWXUBYGYWOOIX-SFHVURJKSA-N (2s)-2-[[4-[2-(2,4-diaminoquinazolin-6-yl)ethyl]benzoyl]amino]-4-methylidenepentanedioic acid Chemical compound C1=CC2=NC(N)=NC(N)=C2C=C1CCC1=CC=C(C(=O)N[C@@H](CC(=C)C(O)=O)C(O)=O)C=C1 NAWXUBYGYWOOIX-SFHVURJKSA-N 0.000 abstract 2
- 229910002651 NO3 Inorganic materials 0.000 abstract 1
- NHNBFGGVMKEFGY-UHFFFAOYSA-N Nitrate Chemical compound [O-][N+]([O-])=O NHNBFGGVMKEFGY-UHFFFAOYSA-N 0.000 abstract 1
- 125000003277 amino group Chemical group 0.000 abstract 1
- 125000002619 bicyclic group Chemical group 0.000 abstract 1
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 abstract 1
- 125000001425 triazolyl group Chemical group 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/04—Ortho-condensed systems
-
- 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
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/4353—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
- A61K31/437—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
- A61P31/14—Antivirals for RNA viruses
- A61P31/18—Antivirals for RNA viruses for HIV
-
- 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
- C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
- C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
- C07F9/02—Phosphorus compounds
- C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
- C07F9/6561—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing systems of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring or ring system, with or without other non-condensed hetero rings
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Veterinary Medicine (AREA)
- Molecular Biology (AREA)
- Public Health (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Biochemistry (AREA)
- Virology (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Communicable Diseases (AREA)
- Tropical Medicine & Parasitology (AREA)
- Engineering & Computer Science (AREA)
- Oncology (AREA)
- AIDS & HIV (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
Abstract
También reivindica los compuestos intermediarios de fórmulas (11), (12), (13), (14).Reivindicación 1: Un método para obtener el compuesto de la fórmula (16) caracterizado porque comprende: (a) bromar el compuesto de fórmula (1) para obtener el compuesto de fórmula (2); y (b) nitrar el compuesto de fórmula (2) para obtener el compuesto de fórmula (3); y (c) convertir el grupo amina del compuesto de fórmula (3) en un grupo metoxi para obtener el compuesto de fórmula (4); y (d) luego, convertir el compuesto de fórmula (4) en el compuesto de fórmula (5); y (e) convertir el compuesto de fórmula (5) en el compuesto de fórmula (6); y (f) formar una estructura bicíclica a partir del compuesto de fórmula (6) para obtener el compuesto de fórmula (7); y (g) luego, clorar el compuesto de fórmula (7) para producir el compuesto de fórmula (8); y (h) posteriormente, agregar una porción de triazolilo al compuesto de fórmula (8) para obtener el compuesto de fórmula (9); y (i) convertir el compuesto de fórmula (9) en la estructura de fórmula (10); y (j) modificar el compuesto de fórmula (10) para obtener el compuesto de fórmula (11); y (k) hacer reaccionar el compuesto de fórmula (11) para producir el compuesto de fórmula (12); y (l) luego, convertir el compuesto de fórmula (12) en el compuesto de fórmula (13); (m) luego, convertir el compuesto de fórmula (13) en el compuesto de fórmula (14); y (n) luego, hacer reaccionar el compuesto de fórmula (14) para producir el compuesto de fórmula (15); y (o) luego, convertir el compuesto de fórmula (15) en el compuesto de la fórmula (16).
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201161437821P | 2011-01-31 | 2011-01-31 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR085052A1 true AR085052A1 (es) | 2013-08-07 |
Family
ID=45688987
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP120100313A AR085052A1 (es) | 2011-01-31 | 2012-01-31 | Metodos para producir un compuesto profarmaco inhibidor de la union al vih e intermediarios |
Country Status (25)
| Country | Link |
|---|---|
| US (1) | US8436168B2 (es) |
| EP (1) | EP2670751B1 (es) |
| JP (1) | JP6006236B2 (es) |
| KR (1) | KR101848533B1 (es) |
| CN (1) | CN103339130B (es) |
| AR (1) | AR085052A1 (es) |
| AU (1) | AU2012212508B2 (es) |
| BR (1) | BR112013018159A2 (es) |
| CA (1) | CA2826260C (es) |
| CY (1) | CY1116505T1 (es) |
| DK (1) | DK2670751T3 (es) |
| EA (1) | EA021726B1 (es) |
| ES (1) | ES2539908T3 (es) |
| HR (1) | HRP20150616T1 (es) |
| HU (1) | HUE026880T2 (es) |
| IL (1) | IL227302A (es) |
| MX (1) | MX2013008371A (es) |
| PL (1) | PL2670751T3 (es) |
| PT (1) | PT2670751E (es) |
| RS (1) | RS54055B1 (es) |
| SG (1) | SG191841A1 (es) |
| SI (1) | SI2670751T1 (es) |
| SM (1) | SMT201500169B (es) |
| TW (1) | TW201309692A (es) |
| WO (1) | WO2012106189A1 (es) |
Families Citing this family (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US7745625B2 (en) * | 2004-03-15 | 2010-06-29 | Bristol-Myers Squibb Company | Prodrugs of piperazine and substituted piperidine antiviral agents |
| WO2010085456A1 (en) | 2009-01-20 | 2010-07-29 | Guided Delivery Systems Inc. | Anchor deployment devices and related methods |
| CN104080785B (zh) | 2012-02-08 | 2016-08-31 | 百时美施贵宝公司 | 用于制备hiv附着抑制剂哌嗪前药化合物的方法 |
| JP6693891B2 (ja) * | 2014-06-23 | 2020-05-13 | フリー フォーム ファイバーズ リミテッド ライアビリティ カンパニー | 核燃料構造体及び核燃料構造体を作製する方法 |
| RU2017123259A (ru) | 2014-12-18 | 2019-01-21 | ВАЙВ ХЕЛТКЕР ЮКей (N4) ЛИМИТЕД | Способ получения галогенированных азаиндольных соединений с использованием бороксина |
| AU2015364535A1 (en) | 2014-12-18 | 2017-07-06 | Viiv Healthcare Uk (No. 4) Limited | A process for preparing halogenated azaindole compounds using PyBroP |
| EP4292551A3 (en) | 2015-03-05 | 2024-01-31 | Ancora Heart, Inc. | Devices of visualizing and determining depth of penetration in cardiac tissue |
| WO2020148679A1 (en) | 2019-01-17 | 2020-07-23 | ViiV Healthcare UK (No.4) Limited | Process for preparing fostemsavir |
Family Cites Families (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20040110785A1 (en) | 2001-02-02 | 2004-06-10 | Tao Wang | Composition and antiviral activity of substituted azaindoleoxoacetic piperazine derivatives |
| US7745625B2 (en) * | 2004-03-15 | 2010-06-29 | Bristol-Myers Squibb Company | Prodrugs of piperazine and substituted piperidine antiviral agents |
| US7776863B2 (en) | 2004-03-24 | 2010-08-17 | Bristol-Myers Squibb Company | Methods of treating HIV infection |
| US7601715B2 (en) * | 2005-06-22 | 2009-10-13 | Bristol-Myers Squibb Company | Process for preparing triazole substituted azaindoleoxoacetic piperazine derivatives and novel salt forms produced therein |
| US7851476B2 (en) * | 2005-12-14 | 2010-12-14 | Bristol-Myers Squibb Company | Crystalline forms of 1-benzoyl-4-[2-[4-methoxy-7-(3-methyl-1H-1,2,4-triazol-1-YL)-1-[(phosphonooxy)methyl]-1H-pyrrolo[2,3-C]pyridin-3-YL]-1,2-dioxoethyl]-piperazine |
-
2012
- 2012-01-27 SI SI201230225T patent/SI2670751T1/sl unknown
- 2012-01-27 CA CA2826260A patent/CA2826260C/en not_active Expired - Fee Related
- 2012-01-27 JP JP2013551361A patent/JP6006236B2/ja active Active
- 2012-01-27 DK DK12704960.9T patent/DK2670751T3/en active
- 2012-01-27 PL PL12704960T patent/PL2670751T3/pl unknown
- 2012-01-27 RS RS20150388A patent/RS54055B1/en unknown
- 2012-01-27 PT PT127049609T patent/PT2670751E/pt unknown
- 2012-01-27 SG SG2013051560A patent/SG191841A1/en unknown
- 2012-01-27 MX MX2013008371A patent/MX2013008371A/es active IP Right Grant
- 2012-01-27 HU HUE12704960A patent/HUE026880T2/en unknown
- 2012-01-27 WO PCT/US2012/022851 patent/WO2012106189A1/en active Application Filing
- 2012-01-27 AU AU2012212508A patent/AU2012212508B2/en not_active Ceased
- 2012-01-27 ES ES12704960.9T patent/ES2539908T3/es active Active
- 2012-01-27 EP EP20120704960 patent/EP2670751B1/en active Active
- 2012-01-27 BR BR112013018159A patent/BR112013018159A2/pt not_active Application Discontinuation
- 2012-01-27 CN CN201280007153.8A patent/CN103339130B/zh not_active Expired - Fee Related
- 2012-01-27 EA EA201391123A patent/EA021726B1/ru not_active IP Right Cessation
- 2012-01-27 US US13/359,708 patent/US8436168B2/en active Active
- 2012-01-27 KR KR1020137022709A patent/KR101848533B1/ko active Active
- 2012-01-31 TW TW101103123A patent/TW201309692A/zh unknown
- 2012-01-31 AR ARP120100313A patent/AR085052A1/es not_active Application Discontinuation
-
2013
- 2013-07-02 IL IL227302A patent/IL227302A/en active IP Right Grant
-
2015
- 2015-06-08 HR HRP20150616TT patent/HRP20150616T1/hr unknown
- 2015-07-14 SM SM201500169T patent/SMT201500169B/xx unknown
- 2015-07-17 CY CY20151100631T patent/CY1116505T1/el unknown
Also Published As
| Publication number | Publication date |
|---|---|
| JP6006236B2 (ja) | 2016-10-12 |
| TW201309692A (zh) | 2013-03-01 |
| JP2014503594A (ja) | 2014-02-13 |
| CN103339130B (zh) | 2015-05-06 |
| KR20140014154A (ko) | 2014-02-05 |
| IL227302A0 (en) | 2013-09-30 |
| CY1116505T1 (el) | 2017-03-15 |
| SI2670751T1 (sl) | 2015-07-31 |
| ES2539908T3 (es) | 2015-07-07 |
| EA201391123A1 (ru) | 2013-12-30 |
| AU2012212508A1 (en) | 2013-09-19 |
| AU2012212508B2 (en) | 2016-01-14 |
| EA021726B1 (ru) | 2015-08-31 |
| IL227302A (en) | 2016-10-31 |
| PL2670751T3 (pl) | 2015-09-30 |
| RS54055B1 (en) | 2015-10-30 |
| DK2670751T3 (en) | 2015-07-20 |
| KR101848533B1 (ko) | 2018-04-12 |
| PT2670751E (pt) | 2015-07-29 |
| EP2670751A1 (en) | 2013-12-11 |
| SG191841A1 (en) | 2013-08-30 |
| HRP20150616T1 (hr) | 2015-07-03 |
| HUE026880T2 (en) | 2016-08-29 |
| EP2670751B1 (en) | 2015-04-22 |
| US20130030178A1 (en) | 2013-01-31 |
| CA2826260C (en) | 2018-09-04 |
| SMT201500169B (it) | 2015-09-07 |
| BR112013018159A2 (pt) | 2018-09-11 |
| WO2012106189A1 (en) | 2012-08-09 |
| US8436168B2 (en) | 2013-05-07 |
| CN103339130A (zh) | 2013-10-02 |
| CA2826260A1 (en) | 2012-08-09 |
| MX2013008371A (es) | 2013-08-12 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FA | Abandonment or withdrawal |