BRPI0410714A - derivados de quinazolina - Google Patents
derivados de quinazolinaInfo
- Publication number
- BRPI0410714A BRPI0410714A BRPI0410714-4A BRPI0410714A BRPI0410714A BR PI0410714 A BRPI0410714 A BR PI0410714A BR PI0410714 A BRPI0410714 A BR PI0410714A BR PI0410714 A BRPI0410714 A BR PI0410714A
- Authority
- BR
- Brazil
- Prior art keywords
- alkyl
- independently represent
- het
- represent hydrogen
- optionally substituted
- Prior art date
Links
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
- C07D498/06—Peri-condensed systems
-
- 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
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C229/00—Compounds containing amino and carboxyl groups bound to the same carbon skeleton
- C07C229/02—Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton
- C07C229/04—Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being acyclic and saturated
- C07C229/06—Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being acyclic and saturated having only one amino and one carboxyl group bound to the carbon skeleton
- C07C229/10—Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being acyclic and saturated having only one amino and one carboxyl group bound to the carbon skeleton the nitrogen atom of the amino group being further bound to acyclic carbon atoms or to carbon atoms of rings other than six-membered aromatic rings
- C07C229/16—Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being acyclic and saturated having only one amino and one carboxyl group bound to the carbon skeleton the nitrogen atom of the amino group being further bound to acyclic carbon atoms or to carbon atoms of rings other than six-membered aromatic rings to carbon atoms of hydrocarbon radicals substituted by amino or carboxyl groups, e.g. ethylenediamine-tetra-acetic acid, iminodiacetic acids
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C229/00—Compounds containing amino and carboxyl groups bound to the same carbon skeleton
- C07C229/40—Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino groups bound to carbon atoms of at least one six-membered aromatic ring and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton
-
- 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
- C07D239/86—Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in position 4
- C07D239/88—Oxygen atoms
-
- 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
- C07D239/86—Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in position 4
- C07D239/93—Sulfur atoms
-
- 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
- C07D239/86—Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in position 4
- C07D239/94—Nitrogen atoms
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Engineering & Computer Science (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Heart & Thoracic Surgery (AREA)
- Cardiology (AREA)
- Vascular Medicine (AREA)
- Urology & Nephrology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
Abstract
"DERIVADOS DE QUINAZOLINA". A presente invenção se refere a compostos da fórmula: as formas de N-óxido, os sais de adição farmaceuticamente aceitáveis e as formas estereoquimicamente isoméricas do mesmo, em que: Z representa NH; Y representa -C~ 3-9~ alquila-, -C~ 2-9~ alquenila-, -C~ 3-7~alquil-CO-NH opcionalmente substituída por amino, mono - ou di(C~ 1-4~alquil)amino ou C~ 1-4~ alquilóxicarbonilamino-, -C~ 3-7~alquenil-CO-NH- opcionalmente substituído por amino, mono- ou di(C~ 1~-4~alquil)amino- ou C~ 1-4~ alquilóxicarbonilamino-, C~ 1-5~alquil-NR~ 13~-C~ 1-5~ alquila-, C~ 1-5~alquil-NR¬ 14¬-CO-C~ 1-5~ alquila-, -C~ 1-6~alquil-CO-NH-, -C~ 1-5~alquil-CO NR¬ 15¬-C~ 1-5~ alquila-, -C~ 1-3~alquil-NH-CO-Het¬ 20¬-, -C~ 1-2~alquil-CO-Het¬ 21¬CO-, -C~ 1-2~alquil-NH-CO-CR¬ 16¬R¬ 17¬-NH-, -C~ 1-2~alquiL-CO-NH-CR¬ 18¬R¬ 19¬-CO-, -C~ 1-2~alquiL-CO-Nr¬ 20¬-C~ 1-3~alquil-CO- ou -NR¬ 22¬-CO-C~ 1-3~alquil-NH-; X¬ 1¬ representa uma ligação direta, O ou -O-C~ 1-2~ alquila-; X¬ 2¬ representa uma ligação direta, -CO-C~ 1-2~ alquila-, NR¬ 12¬,-NR¬ 12¬-C~ 1-2~ alquila-, -O-N=CH- ou -C~ 1-2~ alquila-; R¬ 1¬ e R¬ 2¬ representam, cada um independentemente, hidrogênio ou halo; R¬ 3¬ representa hidrogênio; R¬ 4¬ representa hidrogênio ou C~ 1-4~ alquilóxi; R¬ 12¬ e R¬ 13¬ representam, cada um independentemente, hidrogênio OU C~ 1-4~ alquila; R¬ 14¬ e R¬ 15¬ representa hidrogênio; R¬ 16¬ e R~ 17¬ representam, cada um independentemente, hidrogênio ou C~ 1-4~ alquila; R¬ 18¬ e R¬ 19¬ representam, cada um independentemente, hidrogênio ou C~ 1-4~ alquila opcionalmente substituída por fenila ou hidróxi; R¬ 20¬ e R¬ 21¬ representam, cada um independentemente, hidrogênio OU C~ 1-4~ alquila opcionalmente substituída por C~ 1-4~ alquilóxi; Het¬ 20¬, Het¬ 21¬ e Het¬ 22¬ representam, cada um independentemente, um heterociclo selecionado do grupo consistindo de pirrolidinila, 2-pirrolidinonila ou piperidinila opcionalmente substituída por hidróxi.
Applications Claiming Priority (7)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
EPPCT/EP03/05723 | 2003-05-27 | ||
EP0305723 | 2003-05-27 | ||
EPPCT/EP03/10266 | 2003-09-15 | ||
EP0310266 | 2003-09-15 | ||
EPPCT/EP03/51061 | 2003-12-18 | ||
EP0351061 | 2003-12-18 | ||
PCT/EP2004/005621 WO2004105765A1 (en) | 2003-05-27 | 2004-05-25 | Macrocyclic quinazoline derivatives as antiproliferative agents |
Publications (3)
Publication Number | Publication Date |
---|---|
BRPI0410714A true BRPI0410714A (pt) | 2006-06-13 |
BRPI0410714B1 BRPI0410714B1 (pt) | 2019-09-24 |
BRPI0410714B8 BRPI0410714B8 (pt) | 2021-05-25 |
Family
ID=33493782
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
BRPI0410714A BRPI0410714B8 (pt) | 2003-05-27 | 2004-05-25 | derivados de quinazolina macrocíclicos, seu processo de preparação, composição farmacêutica que os compreende e uso |
Country Status (32)
Country | Link |
---|---|
US (4) | US7648975B2 (pt) |
EP (2) | EP2305687A1 (pt) |
JP (1) | JP4887151B2 (pt) |
KR (1) | KR101143878B1 (pt) |
CN (1) | CN102718775B (pt) |
AR (2) | AR045687A1 (pt) |
AT (1) | ATE544454T1 (pt) |
AU (1) | AU2004243487B2 (pt) |
BR (1) | BRPI0410714B8 (pt) |
CA (1) | CA2525214C (pt) |
CL (1) | CL2004001267A1 (pt) |
CO (1) | CO5640038A2 (pt) |
CY (1) | CY1113002T1 (pt) |
DK (1) | DK1633365T3 (pt) |
EA (1) | EA009064B1 (pt) |
ES (1) | ES2381976T3 (pt) |
HK (1) | HK1176350A1 (pt) |
HR (1) | HRP20120351T1 (pt) |
IL (3) | IL172154A0 (pt) |
IS (1) | IS3030B (pt) |
JO (1) | JO2785B1 (pt) |
MX (1) | MXPA05012762A (pt) |
MY (1) | MY148633A (pt) |
NO (1) | NO334209B1 (pt) |
NZ (1) | NZ544154A (pt) |
PA (1) | PA8603801A1 (pt) |
PL (1) | PL1633365T3 (pt) |
PT (1) | PT1633365E (pt) |
SI (1) | SI1633365T1 (pt) |
TW (3) | TWI468397B (pt) |
UA (1) | UA84010C2 (pt) |
WO (1) | WO2004105765A1 (pt) |
Families Citing this family (51)
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JO2785B1 (en) * | 2003-05-27 | 2014-03-15 | شركة جانسين فارماسوتيكا ان. في | Quinazoline derivatives |
EP1684762A4 (en) * | 2003-11-13 | 2009-06-17 | Ambit Biosciences Corp | UREA DERIVATIVES AS MODULATORS OF KINASE |
UA83881C2 (en) | 2003-12-18 | 2008-08-26 | Янссен Фармацевтика Н.В. | Pyrido- and pyrimidopyrimidine derivatives as anti-proliferative agents |
KR101158440B1 (ko) * | 2003-12-18 | 2012-07-06 | 얀센 파마슈티카 엔.브이. | 항증식활성을 지닌 3-시아노-퀴놀린 유도체 |
JO3088B1 (ar) * | 2004-12-08 | 2017-03-15 | Janssen Pharmaceutica Nv | مشتقات كوينازولين كبيرة الحلقات و استعمالها بصفتها موانع كينيز متعددة الاهداف |
NI200700147A (es) | 2004-12-08 | 2019-05-10 | Janssen Pharmaceutica Nv | Derivados de quinazolina inhibidores de cinasas dirigidos a multip |
MY169441A (en) | 2004-12-08 | 2019-04-11 | Janssen Pharmaceutica Nv | 2,4, (4,6) pyrimidine derivatives |
ES2431843T3 (es) | 2005-02-23 | 2013-11-28 | Shionogi & Co., Ltd. | Derivado de quinazolina que tiene actividad inhibidora de tirosina quinasa |
GB0509227D0 (en) | 2005-05-05 | 2005-06-15 | Chroma Therapeutics Ltd | Intracellular enzyme inhibitors |
UA92608C2 (en) * | 2005-06-30 | 2010-11-25 | Янссен Фармацевтика Н.В. | Cyclic anilino - pyridinotriazines as gsk-3 inhibitors |
DK2044084T3 (en) * | 2006-07-13 | 2016-05-09 | Janssen Pharmaceutica Nv | MTKI-quinazoline derivatives |
JP2009242240A (ja) * | 2006-08-04 | 2009-10-22 | Mebiopharm Co Ltd | 含ホウ素キナゾリン誘導体 |
US7547781B2 (en) | 2006-09-11 | 2009-06-16 | Curis, Inc. | Quinazoline based EGFR inhibitors containing a zinc binding moiety |
SG174774A1 (en) | 2006-09-11 | 2011-10-28 | Curis Inc | Quinazoline based egfr inhibitors containing a zinc binding moiety |
EP2061469B8 (en) * | 2006-09-11 | 2014-02-26 | Curis, Inc. | Quinazoline based egfr inhibitors |
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BRPI0718021A2 (pt) * | 2006-10-27 | 2013-11-12 | Janssen Pharmaceutica Nv | Uso de mtki 1 para tratar ou prevenir câncer ósseo |
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TWI577680B (zh) | 2008-10-22 | 2017-04-11 | 亞雷生物製藥股份有限公司 | 作為TRK激酶抑制劑之經取代吡唑并〔1,5-a〕嘧啶化合物 |
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NZ604708A (en) * | 2010-05-20 | 2015-05-29 | Array Biopharma Inc | Macrocyclic compounds as trk kinase inhibitors |
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RU2020131276A (ru) * | 2014-02-07 | 2020-11-03 | Экзитера Фармасьютикалз Инк. | Терапевтические соединения и композиции |
MA39822A (fr) | 2014-04-03 | 2018-02-06 | Janssen Pharmaceutica Nv | Dérivés de pyrimidine bicycle |
MA39823A (fr) | 2014-04-03 | 2018-01-09 | Janssen Pharmaceutica Nv | Dérivés de pyridine macrocyclique |
IL290905B2 (en) | 2014-11-16 | 2023-09-01 | Array Biopharma Inc | Crystal form of (s)–n-(5–)–2–(r))5,2-difluorophenyl)-pyrrolidine-1-yl)-pyrazolo[5,1-a]pyrimidine-3-yl)-3 -Hydroxypyrrolidine-1-carboxamide hydrogen sulfate |
JP6740354B2 (ja) | 2015-10-05 | 2020-08-12 | ザ トラスティーズ オブ コロンビア ユニバーシティー イン ザ シティー オブ ニューヨーク | オートファジーの流れ及びホスホリパーゼd及びタウを含むタンパク質凝集体のクリアランスの活性化剤ならびにタンパク質症の治療方法 |
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CR20180501A (es) | 2016-04-04 | 2019-04-05 | Loxo Oncology Inc | Formulaciones liquidas de (s)-n-(5-((r)-2(2,5-difluorofenil)-pirrolidin-1-il)-pirazolo[1,5-a] pirimidin-3-il)-3-hidroxipirrolidina-1-carboxamida |
US10045991B2 (en) | 2016-04-04 | 2018-08-14 | Loxo Oncology, Inc. | Methods of treating pediatric cancers |
SI3458456T1 (sl) | 2016-05-18 | 2021-04-30 | Loxo Oncology, Inc. | Priprava (S)-N-(5-((R)-2-(2,5-difluorofenil) pirolidin-1-il) pirazolo (1,5-A) pirimidin-3-il)-3-hidroksipirolidin-1-karboksamida |
JOP20190092A1 (ar) | 2016-10-26 | 2019-04-25 | Array Biopharma Inc | عملية لتحضير مركبات بيرازولو[1، 5-a]بيريميدين وأملاح منها |
JOP20190213A1 (ar) | 2017-03-16 | 2019-09-16 | Array Biopharma Inc | مركبات حلقية ضخمة كمثبطات لكيناز ros1 |
JP7292299B2 (ja) * | 2017-12-07 | 2023-06-16 | アンプリックス ファーマシューティカルズ,インク. | 複素環式の置換ピリジン誘導体である抗真菌薬 |
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2004
- 2004-05-24 JO JO200466A patent/JO2785B1/en active
- 2004-05-24 PA PA20048603801A patent/PA8603801A1/es unknown
- 2004-05-25 MX MXPA05012762A patent/MXPA05012762A/es active IP Right Grant
- 2004-05-25 PL PL04739341T patent/PL1633365T3/pl unknown
- 2004-05-25 CA CA2525214A patent/CA2525214C/en not_active Expired - Lifetime
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- 2004-05-25 AT AT04739341T patent/ATE544454T1/de active
- 2004-05-25 WO PCT/EP2004/005621 patent/WO2004105765A1/en active Application Filing
- 2004-05-25 DK DK04739341.8T patent/DK1633365T3/da active
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- 2004-05-25 UA UAA200510181A patent/UA84010C2/ru unknown
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- 2004-05-25 KR KR1020057022189A patent/KR101143878B1/ko active IP Right Grant
- 2004-05-25 CN CN201210144221.7A patent/CN102718775B/zh not_active Expired - Lifetime
- 2004-05-25 JP JP2006529915A patent/JP4887151B2/ja not_active Expired - Lifetime
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- 2004-05-25 US US10/558,007 patent/US7648975B2/en active Active
- 2004-05-25 SI SI200431864T patent/SI1633365T1/sl unknown
- 2004-05-25 BR BRPI0410714A patent/BRPI0410714B8/pt not_active Application Discontinuation
- 2004-05-25 EP EP10192741A patent/EP2305687A1/en not_active Withdrawn
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- 2004-05-26 AR ARP040101806A patent/AR045687A1/es active IP Right Grant
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2005
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- 2005-12-27 NO NO20056196A patent/NO334209B1/no unknown
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2009
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2012
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2013
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- 2013-03-12 HK HK13103104.2A patent/HK1176350A1/zh not_active IP Right Cessation
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2014
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2016
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