AR077797A1 - Procedimientos para la sintesis estereoselectiva de heterociclos biciclicos - Google Patents
Procedimientos para la sintesis estereoselectiva de heterociclos biciclicosInfo
- Publication number
- AR077797A1 AR077797A1 ARP100102887A ARP100102887A AR077797A1 AR 077797 A1 AR077797 A1 AR 077797A1 AR P100102887 A ARP100102887 A AR P100102887A AR P100102887 A ARP100102887 A AR P100102887A AR 077797 A1 AR077797 A1 AR 077797A1
- Authority
- AR
- Argentina
- Prior art keywords
- compound
- formula
- reaction
- give
- group
- Prior art date
Links
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
- C07D239/70—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
- C07D239/72—Quinazolines; Hydrogenated quinazolines
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P13/00—Drugs for disorders of the urinary system
- A61P13/08—Drugs for disorders of the urinary system of the prostate
-
- 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
-
- 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
- A61P37/00—Drugs for immunological or allergic disorders
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
- C07D239/70—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D241/00—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings
- C07D241/36—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings condensed with carbocyclic rings or ring systems
- C07D241/38—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings condensed with carbocyclic rings or ring systems with only hydrogen or carbon atoms directly attached to the ring nitrogen atoms
-
- 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
-
- Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
- Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
- Y02P—CLIMATE CHANGE MITIGATION TECHNOLOGIES IN THE PRODUCTION OR PROCESSING OF GOODS
- Y02P20/00—Technologies relating to chemical industry
- Y02P20/50—Improvements relating to the production of bulk chemicals
- Y02P20/55—Design of synthesis routes, e.g. reducing the use of auxiliary or protecting groups
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Diabetes (AREA)
- Urology & Nephrology (AREA)
- Emergency Medicine (AREA)
- Endocrinology (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Pulmonology (AREA)
- Immunology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
- Plural Heterocyclic Compounds (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Steroid Compounds (AREA)
Abstract
Preparacion de un compuesto y de sus sales, en particular sus sales fisiologicamente compatibles con ácidos y bases inorgánicos u orgánicos, las cuales muestran propiedades farmacéuticas valiosas, en particular un efecto inhibidor sobre la transduccion de senales mediadas por tirosinquinasas, a su utilizacion para el tratamiento de enfermedades, en particular enfermedades tumorales, tales como la hiperplasia benigna de prostata (HBP), enfermedades pulmonares y de las vías respiratorias. Reivindicacion 1: Procedimiento para la preparacion estereoselectiva del compuesto de la formula (1A) eventualmente en forma de sus tautomeros, así como eventualmente de sus sales por adicion de ácidos farmacologicamente inocuas, caracterizado porque el procedimiento abarca las etapas de reaccion (A), (B), (V), (X), (R), (S) y (T), significando (A) la reaccion de 1,4-ciclohexanodion-mono-etilencetal para dar un compuesto de la formula (1); (B) la reaccion de un compuesto de la formula (1) para dar el compuesto de la formula (2); (V) la reaccion de un compuesto de la formula (2) con un reactivo protector de grupos para dar el compuesto de la formula (3); (X) la reaccion de un compuesto de la formula (3) para dar el compuesto de la formula (4); (R) la reaccion de un compuesto de la formula (4) con un compuesto de la formula (5) para dar un compuesto de la formula (6); (S) la separacion de los grupos protectores del compuesto de la formula (6) para dar un compuesto de la formula (7); y (T) la cloracion del compuesto de la formula (7) y subsiguiente reaccion con 3-cloro-2-fluoroanilina, en donde las etapas (A) a (T) tienen lugar consecutivamente en el orden mencionado, y pudiendo significar el grupo protector Sg1 un radical seleccionado del grupo constituido por bencilo eventualmente sustituido, Cbz y acetilo eventualmente sustituido, pudiendo significar el grupo protector Sg2 bencilo eventualmente sustituido. Reivindicacion 4: Procedimiento para la preparacion estereoselectiva del compuesto de la formula (1B) eventualmente en forma de sus tautomeros, así como eventualmente de sus sales por adicion de ácidos farmacologicamente inocuas, caracterizado porque el procedimiento abarca las etapas de reaccion (A), (B), (Z), (H), (P), (Q), (M), (N) y (O), significando (A) la reaccion de 1,4-ciclohexanodion-mono-etilencetal para dar un compuesto de la formula (1); (B) la reaccion de un compuesto de la formula (1) para dar el compuesto de la formula (2); (Z) la reaccion de un compuesto de la formula (2) para dar el compuesto de la formula (8); (H) la reaccion de un compuesto de la formula (8) para dar el compuesto de la formula (9); (P) la reaccion de un compuesto de la formula (9) con un compuesto de la formula (5) para dar un compuesto de la formula (10); (Q + M) la separacion de los grupos protectores del compuesto de la formula (10) para dar un compuesto de la formula (11); y (N + O) la cloracion del compuesto de la formula (11) y subsiguiente reaccion con 3-cloro-2-fluoroanilina, en donde las etapas (A) a (O) tienen lugar consecutivamente en el orden mencionado; y pudiendo significar el grupo protector Sg1 un radical seleccionado del grupo constituido por bencilo eventualmente sustituido, Cbz y acetilo eventualmente sustituido, pudiendo significar el grupo protector Sg2 bencilo eventualmente sustituido, y el grupo protector Sg3 se selecciona del grupo Boc y aliloxicarbonilo.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP09167393A EP2289881A1 (de) | 2009-08-06 | 2009-08-06 | Verfahren zur stereoselektiven Synthese bicyclischer Heterocyclen |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR077797A1 true AR077797A1 (es) | 2011-09-21 |
Family
ID=41205591
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP100102887A AR077797A1 (es) | 2009-08-06 | 2010-08-05 | Procedimientos para la sintesis estereoselectiva de heterociclos biciclicos |
Country Status (21)
| Country | Link |
|---|---|
| US (2) | US8658790B2 (es) |
| EP (2) | EP2289881A1 (es) |
| JP (1) | JP2013501025A (es) |
| KR (1) | KR20120049248A (es) |
| CN (1) | CN102471288B (es) |
| AR (1) | AR077797A1 (es) |
| AU (1) | AU2010280852B2 (es) |
| BR (1) | BR112012002104A2 (es) |
| CA (1) | CA2767963A1 (es) |
| CL (1) | CL2012000159A1 (es) |
| DK (1) | DK2462126T3 (es) |
| EA (1) | EA023562B1 (es) |
| ES (1) | ES2549770T3 (es) |
| HU (1) | HUE025400T2 (es) |
| IL (1) | IL216969A (es) |
| MX (1) | MX2012001089A (es) |
| NZ (1) | NZ597698A (es) |
| PL (1) | PL2462126T3 (es) |
| TW (1) | TW201120013A (es) |
| UY (1) | UY32830A (es) |
| WO (1) | WO2011015526A1 (es) |
Families Citing this family (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP2289881A1 (de) * | 2009-08-06 | 2011-03-02 | Boehringer Ingelheim International GmbH | Verfahren zur stereoselektiven Synthese bicyclischer Heterocyclen |
| MX2013008870A (es) * | 2011-02-01 | 2013-08-14 | Boehringer Ingelheim Int | Dimaleato de 9-[4-(3-cloro-2-fluoro-fenilamino)-7-metoxi-quinazoli n-6-iloxi]-1,4-diaza-espiro[5.5]undecan-5-ona, su uso como medicamento y su preparacion. |
| EP2812317B1 (de) * | 2012-02-09 | 2016-02-03 | Boehringer Ingelheim International GmbH | Verfahren zur stereoselektiven synthese von 1,4-geschützten 9-hydroxy-5-oxo-1,4-diaza-spiro [5.5]undecane |
| JP2015524400A (ja) * | 2012-07-19 | 2015-08-24 | 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 | ９−［４−（３−クロロ−２−フルオロ−フェニルアミノ）−７−メトキシ−キナゾリン−６−イルオキシ］−１，４−ジアザ−スピロ［５．５］ウンデカン−５−オンのフマル酸塩、その薬物としての使用及び調製 |
| WO2021198188A1 (en) | 2020-03-30 | 2021-10-07 | Enyo Pharma | Quinazolinone derivatives and uses thereof for treating a cancer |
| US11680403B2 (en) * | 2020-09-21 | 2023-06-20 | Amp Ip Llc | Multi-purpose structural panels and systems for assembling structures |
Family Cites Families (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| TWI324597B (en) | 2002-03-28 | 2010-05-11 | Astrazeneca Ab | Quinazoline derivatives |
| BRPI0807234A2 (pt) * | 2007-02-06 | 2014-06-03 | Boehringer Ingelheim Int | Heterociclos bicíclicos, composições farmacêuticas que contêm estes compostos, o uso dos mesmos e processos para a preparação dos mesmos |
| SI2202216T1 (sl) * | 2007-10-26 | 2012-10-30 | Japan Tobacco Inc | Spiro obročna spojina in njena uporaba za medicinske namene |
| KR20100111291A (ko) * | 2008-02-07 | 2010-10-14 | 베링거 인겔하임 인터내셔날 게엠베하 | 스피로사이클릭 헤테로사이클, 상기 화합물을 함유하는 약제, 이의 용도 및 이의 제조 방법 |
| EP2313377B1 (de) * | 2008-08-08 | 2016-01-06 | Boehringer Ingelheim International Gmbh | Verfahren zur stereoselektiven synthese bicyclischer heterocyclen |
| EP2289881A1 (de) * | 2009-08-06 | 2011-03-02 | Boehringer Ingelheim International GmbH | Verfahren zur stereoselektiven Synthese bicyclischer Heterocyclen |
| MX2013008870A (es) * | 2011-02-01 | 2013-08-14 | Boehringer Ingelheim Int | Dimaleato de 9-[4-(3-cloro-2-fluoro-fenilamino)-7-metoxi-quinazoli n-6-iloxi]-1,4-diaza-espiro[5.5]undecan-5-ona, su uso como medicamento y su preparacion. |
| EP2812317B1 (de) * | 2012-02-09 | 2016-02-03 | Boehringer Ingelheim International GmbH | Verfahren zur stereoselektiven synthese von 1,4-geschützten 9-hydroxy-5-oxo-1,4-diaza-spiro [5.5]undecane |
-
2009
- 2009-08-06 EP EP09167393A patent/EP2289881A1/de not_active Withdrawn
-
2010
- 2010-07-30 KR KR1020127003126A patent/KR20120049248A/ko not_active Withdrawn
- 2010-07-30 WO PCT/EP2010/061096 patent/WO2011015526A1/de not_active Ceased
- 2010-07-30 NZ NZ597698A patent/NZ597698A/en not_active IP Right Cessation
- 2010-07-30 BR BR112012002104A patent/BR112012002104A2/pt not_active IP Right Cessation
- 2010-07-30 AU AU2010280852A patent/AU2010280852B2/en not_active Ceased
- 2010-07-30 HU HUE10737572A patent/HUE025400T2/en unknown
- 2010-07-30 MX MX2012001089A patent/MX2012001089A/es active IP Right Grant
- 2010-07-30 US US12/846,943 patent/US8658790B2/en active Active
- 2010-07-30 PL PL10737572T patent/PL2462126T3/pl unknown
- 2010-07-30 CA CA2767963A patent/CA2767963A1/en not_active Abandoned
- 2010-07-30 EP EP10737572.7A patent/EP2462126B1/de not_active Not-in-force
- 2010-07-30 CN CN201080034450.2A patent/CN102471288B/zh not_active Expired - Fee Related
- 2010-07-30 ES ES10737572.7T patent/ES2549770T3/es active Active
- 2010-07-30 DK DK10737572.7T patent/DK2462126T3/en active
- 2010-07-30 JP JP2012523298A patent/JP2013501025A/ja not_active Ceased
- 2010-07-30 EA EA201200219A patent/EA023562B1/ru not_active IP Right Cessation
- 2010-08-05 TW TW099126149A patent/TW201120013A/zh unknown
- 2010-08-05 AR ARP100102887A patent/AR077797A1/es unknown
- 2010-08-05 UY UY0001032830A patent/UY32830A/es not_active Application Discontinuation
-
2011
- 2011-12-14 IL IL216969A patent/IL216969A/en not_active IP Right Cessation
-
2012
- 2012-01-19 CL CL2012000159A patent/CL2012000159A1/es unknown
-
2014
- 2014-01-14 US US14/154,441 patent/US8993753B2/en active Active
Also Published As
| Publication number | Publication date |
|---|---|
| PL2462126T3 (pl) | 2015-11-30 |
| US8993753B2 (en) | 2015-03-31 |
| UY32830A (es) | 2011-03-31 |
| EA201200219A1 (ru) | 2012-11-30 |
| CN102471288A (zh) | 2012-05-23 |
| US8658790B2 (en) | 2014-02-25 |
| HUE025400T2 (en) | 2016-02-29 |
| ES2549770T3 (es) | 2015-11-02 |
| EP2462126B1 (de) | 2015-07-15 |
| US20140135495A1 (en) | 2014-05-15 |
| EP2289881A1 (de) | 2011-03-02 |
| KR20120049248A (ko) | 2012-05-16 |
| TW201120013A (en) | 2011-06-16 |
| AU2010280852B2 (en) | 2015-04-02 |
| CA2767963A1 (en) | 2011-02-10 |
| EA023562B1 (ru) | 2016-06-30 |
| NZ597698A (en) | 2014-03-28 |
| IL216969A (en) | 2015-06-30 |
| MX2012001089A (es) | 2012-02-28 |
| AU2010280852A1 (en) | 2012-02-09 |
| CN102471288B (zh) | 2014-10-22 |
| BR112012002104A2 (pt) | 2015-09-15 |
| EP2462126A1 (de) | 2012-06-13 |
| US20110183987A1 (en) | 2011-07-28 |
| JP2013501025A (ja) | 2013-01-10 |
| DK2462126T3 (en) | 2015-09-07 |
| IL216969A0 (en) | 2012-02-29 |
| WO2011015526A1 (de) | 2011-02-10 |
| CL2012000159A1 (es) | 2012-08-31 |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| AR077797A1 (es) | Procedimientos para la sintesis estereoselectiva de heterociclos biciclicos | |
| CY1124742T1 (el) | 4'-φθορο-νουκλεοσιδια, 4'-φθορο-νουκλοεοτιδια και αναλογα αυτων για τη θεραπευτικη αγωγη toy hcv | |
| EP2598138A4 (en) | ARYLIC CARBON RECEPTOR MODIFIERS AS A NEW CANCER THERAPEUTICS | |
| BR112013028430A2 (pt) | composto, composição farmacêutica, método para tratar uma doença ou condição mediada por tirosina quinase do baço (syk), e, uso de uma quantidade terapeuticamente eficiente do composto | |
| Wang et al. | Synthesis and evaluation of novel alkannin and shikonin oxime derivatives as potent antitumor agents | |
| MX2020006460A (es) | Compuestos de anillo 5,5 fusionado sustituido con diarilo como inhibidores de c5ar. | |
| EA201001143A1 (ru) | Активаторы прокаспаз "исполнителей" 3, 6 и 7 | |
| CY1113269T1 (el) | Παραγωγα ινδαζολυλ αμιδιου για τη θεραπευτικη αγωγη διαταραχων διαμεσολαβουμενων υπο υποδοχεα γλυκοκορτικοειδων | |
| GT200900294A (es) | Compuestos amino-heterocíclicos | |
| BR112019024747A2 (pt) | formulações de dose fixa | |
| BR112013001753A2 (pt) | método para preparar uma composição d einter-alfa-inibidor (iaip) eriquecida de plasma, solução aquosa de iaip, e, método para tratar uma doença ou distúrbio associado com disfunção de iaip e associado com atividadede protease de serina no plasma aumentada. | |
| EP2400847A4 (en) | SPECIFIC DIARYLHYDANTOIN AND DIARYLTHIOHYDANTOINE COMPOUNDS | |
| UY33889A (es) | Dimaleato de 9-[4-(3-cloro-2-fluoro-fenilamino)-7-metoxiquinazolin-6-iloxi]-1,4-diaza-espiro[5 .5]undecan-5-ona, su uso como medicamento y su preparación | |
| MX384293B (es) | Inhibidores de dopamina-b-hidroxilasa penetrantes de la barrera hematoencefálica | |
| TN2018000393A1 (en) | Pegylated carfilzomib compounds | |
| UY32622A (es) | Nuevos compuestos para el tratamiento de patologías relacionadas con ab(beta) | |
| DOP2018000115A (es) | Compuestos de imidazo[4,5-c]quinolin-2-ona y su uso en el tratamiento del cáncer | |
| ECSP10010328A (es) | Heterociclos espirocíclicos, medicamentos que contienen a estos compuestos, su uso y procedimiento para su preparación. | |
| CY1114140T1 (el) | Ενωσεις 4-πυριδινονης και η χρηση αυτων για τον καρκινο | |
| CY1113759T1 (el) | Ταχεως διασπομενοι ανταγωνιστες υποδοχεα ντοπαμινης 2 | |
| TR201819805T4 (tr) | Flavaglin türevleri̇. | |
| MX394367B (es) | Moléculas tipo esfingolípidos sintéticas, fármacos, métodos de su síntesis y usos de los mismos. | |
| CL2020001461A1 (es) | Inhibidores de dopamina–b–hidroxilasa. | |
| MX2009007610A (es) | Heterociclicos biciclicos, medicamentos que contienen estos compuestos, su utilizacion y procedimientos para su preparacion. | |
| BR112015013350A2 (pt) | compostos de triazolona e usos dos mesmos |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FB | Suspension of granting procedure |