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)
- Pulmonology (AREA)
- Emergency Medicine (AREA)
- Endocrinology (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Urology & Nephrology (AREA)
- Immunology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Steroid Compounds (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Plural Heterocyclic Compounds (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (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 (5)
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 |
AP3531A (en) * | 2011-02-01 | 2016-01-13 | Boehringer Ingelheim Int | 9-[4-(3-chlor-2-fluor-phenylamino)-7-methoxy-quinazolin-6-yloxy]-1,4-diaza-spiro[5.5]undecan-5-one dimaleate, use thereof as a drug, and production thereof |
AU2013218119A1 (en) * | 2012-02-09 | 2014-07-17 | Boehringer Ingelheim International Gmbh | Method for stereoselective synthesis of 1,4-protected 9-hydroxy-5-oxo-1,4-diaza-spiro [5.5] undecanes |
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 |
EP4126847A1 (en) | 2020-03-30 | 2023-02-08 | ENYO Pharma | Quinazolinone derivatives and uses thereof for treating a cancer |
Family Cites Families (8)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
TW200813014A (en) | 2002-03-28 | 2008-03-16 | Astrazeneca Ab | Quinazoline derivatives |
KR20090116782A (ko) * | 2007-02-06 | 2009-11-11 | 베링거 인겔하임 인터내셔날 게엠베하 | 바이사이클릭 헤테로사이클, 당해 화합물을 함유하는 약물, 이의 용도 및 이의 제조방법 |
ME02338B (me) * | 2007-10-26 | 2013-02-28 | Japan Tobacco Inc | Spiro-ciklično jedinjenje i njegova upotreba u medicinske svrhe |
DK2245026T3 (da) * | 2008-02-07 | 2012-10-15 | Boehringer Ingelheim Int | Spirocycliske heterocycler, lægemiddel indeholdende disse forbindelser, deres anvendelse og fremgangsmåde til deres fremstilling |
WO2010015524A1 (de) * | 2008-08-08 | 2010-02-11 | 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 |
AP3531A (en) | 2011-02-01 | 2016-01-13 | Boehringer Ingelheim Int | 9-[4-(3-chlor-2-fluor-phenylamino)-7-methoxy-quinazolin-6-yloxy]-1,4-diaza-spiro[5.5]undecan-5-one dimaleate, use thereof as a drug, and production thereof |
AU2013218119A1 (en) * | 2012-02-09 | 2014-07-17 | Boehringer Ingelheim International Gmbh | Method for stereoselective synthesis of 1,4-protected 9-hydroxy-5-oxo-1,4-diaza-spiro [5.5] undecanes |
-
2009
- 2009-08-06 EP EP09167393A patent/EP2289881A1/de not_active Withdrawn
-
2010
- 2010-07-30 US US12/846,943 patent/US8658790B2/en active Active
- 2010-07-30 NZ NZ597698A patent/NZ597698A/en not_active IP Right Cessation
- 2010-07-30 AU AU2010280852A patent/AU2010280852B2/en not_active Ceased
- 2010-07-30 BR BR112012002104A patent/BR112012002104A2/pt not_active IP Right Cessation
- 2010-07-30 WO PCT/EP2010/061096 patent/WO2011015526A1/de active Application Filing
- 2010-07-30 DK DK10737572.7T patent/DK2462126T3/en active
- 2010-07-30 HU HUE10737572A patent/HUE025400T2/en unknown
- 2010-07-30 ES ES10737572.7T patent/ES2549770T3/es active Active
- 2010-07-30 CN CN201080034450.2A patent/CN102471288B/zh not_active Expired - Fee Related
- 2010-07-30 KR KR1020127003126A patent/KR20120049248A/ko unknown
- 2010-07-30 MX MX2012001089A patent/MX2012001089A/es active IP Right Grant
- 2010-07-30 EA EA201200219A patent/EA023562B1/ru not_active IP Right Cessation
- 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 JP JP2012523298A patent/JP2013501025A/ja not_active Ceased
- 2010-07-30 PL PL10737572T patent/PL2462126T3/pl unknown
- 2010-08-05 UY UY0001032830A patent/UY32830A/es not_active Application Discontinuation
- 2010-08-05 AR ARP100102887A patent/AR077797A1/es unknown
- 2010-08-05 TW TW099126149A patent/TW201120013A/zh unknown
-
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 |
---|---|
EP2462126B1 (de) | 2015-07-15 |
JP2013501025A (ja) | 2013-01-10 |
MX2012001089A (es) | 2012-02-28 |
US8993753B2 (en) | 2015-03-31 |
EP2289881A1 (de) | 2011-03-02 |
US20140135495A1 (en) | 2014-05-15 |
DK2462126T3 (en) | 2015-09-07 |
NZ597698A (en) | 2014-03-28 |
US8658790B2 (en) | 2014-02-25 |
KR20120049248A (ko) | 2012-05-16 |
BR112012002104A2 (pt) | 2015-09-15 |
EA201200219A1 (ru) | 2012-11-30 |
CL2012000159A1 (es) | 2012-08-31 |
WO2011015526A1 (de) | 2011-02-10 |
TW201120013A (en) | 2011-06-16 |
AU2010280852B2 (en) | 2015-04-02 |
ES2549770T3 (es) | 2015-11-02 |
EA023562B1 (ru) | 2016-06-30 |
CA2767963A1 (en) | 2011-02-10 |
AU2010280852A1 (en) | 2012-02-09 |
HUE025400T2 (en) | 2016-02-29 |
CN102471288A (zh) | 2012-05-23 |
CN102471288B (zh) | 2014-10-22 |
EP2462126A1 (de) | 2012-06-13 |
US20110183987A1 (en) | 2011-07-28 |
UY32830A (es) | 2011-03-31 |
IL216969A0 (en) | 2012-02-29 |
IL216969A (en) | 2015-06-30 |
PL2462126T3 (pl) | 2015-11-30 |
Similar Documents
Publication | Publication Date | Title |
---|---|---|
CY1124742T1 (el) | 4'-φθορο-νουκλεοσιδια, 4'-φθορο-νουκλοεοτιδια και αναλογα αυτων για τη θεραπευτικη αγωγη toy hcv | |
CY1122808T1 (el) | Ενωσεις ετεροαρυλιου χρησιμες ως αναστολεις toy ενζυμου ενεργοποιησης της sumo | |
AR077797A1 (es) | Procedimientos para la sintesis estereoselectiva de heterociclos biciclicos | |
BR112019024747A2 (pt) | formulações de dose fixa | |
EA201001143A1 (ru) | Активаторы прокаспаз "исполнителей" 3, 6 и 7 | |
GT200900294A (es) | Compuestos amino-heterocíclicos | |
CY1121137T1 (el) | Φαρμακευτικα σκευασματα που περιλαμβανουν ανταγωνιστες ccr3 | |
CO2018004933A2 (es) | Compuestos de imidazo[4,5-c]quinolin-2-ona y su uso en el tratamiento del cáncer | |
Wang et al. | Synthesis and evaluation of novel alkannin and shikonin oxime derivatives as potent antitumor agents | |
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 | |
UY30282A1 (es) | Compuestos quimicos | |
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. | |
ECSP10010328A (es) | Heterociclos espirocíclicos, medicamentos que contienen a estos compuestos, su uso y procedimiento para su preparación. | |
PH12019500569A1 (en) | Blood-brain barrier-penetrant dopamine-b-hydroxylase inhibitors | |
CY1113759T1 (el) | Ταχεως διασπομενοι ανταγωνιστες υποδοχεα ντοπαμινης 2 | |
TN2018000393A1 (en) | Pegylated carfilzomib compounds | |
MX2009007610A (es) | Heterociclicos biciclicos, medicamentos que contienen estos compuestos, su utilizacion y procedimientos para su preparacion. | |
CL2008003672A1 (es) | Compuestos derivados de 3-carbopropil-aminotetralina; procedimiento de preparación; composición farmacéutica que los comprende; y sus usos para tratar disfunciones intestinales inducidas por opioides. | |
TR201819805T4 (tr) | Flavaglin türevleri̇. | |
SV2011003839A (es) | Agentes antifungicos | |
PH12019500858A1 (en) | Combination therapy with a phosphoinositide 3-kinase inhibitor with a zinc binding moiety | |
MX2017015375A (es) | Variantes de oxintomodulina pegilada. | |
CL2020001461A1 (es) | Inhibidores de dopamina–b–hidroxilasa. | |
AR061890A1 (es) | Sal xinafoato del etil ester de la 1-[[5-(1s)-aminoetil)-2-[8-metoxi-2(trifluorometil)-5-quinolil]-4-oxazolil]carbonil]-(4r)-[(ciclopropil-carbonil)amino]-l-prolina. | |
Mai et al. | Synthesis of febrifuginol analogues and evaluation of their biological activities |
Legal Events
Date | Code | Title | Description |
---|---|---|---|
FB | Suspension of granting procedure |