AR092137A2 - Derivados macrociclicos de quinazolina utiles como agentes antiproliferativos - Google Patents
Derivados macrociclicos de quinazolina utiles como agentes antiproliferativosInfo
- Publication number
- AR092137A2 AR092137A2 ARP130102897A ARP130102897A AR092137A2 AR 092137 A2 AR092137 A2 AR 092137A2 AR P130102897 A ARP130102897 A AR P130102897A AR P130102897 A ARP130102897 A AR P130102897A AR 092137 A2 AR092137 A2 AR 092137A2
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- amino
- hydroxy
- optionally substituted
- mono
- 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
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- 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
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- 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
- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Urology & Nephrology (AREA)
- Vascular Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
Abstract
Reivindicación 1: Un compuesto que tiene la fórmula (1), las formas N-óxido, las sales de adición farmacéuticamente aceptables y las formas estereoquímicamente isómeras del mismo, caracterizado porque Z representa O, CH₂, NH o S; Y representa -alquilo C₃₋₉-, -alquenilo C₃₋₉-, -alquinilo C₃₋₉-, -alquil C₃₋₇-CO-NH- opcionalmente sustituido con amino, mono- o di(alquil C₁₋₄)amino o alquil C₁₋₄oxicarbonilamino-, -alquenil C₃₋₇-CO-NH- opcionalmente sustituido con amino, mono- o di(alquil C₁₋₄)amino o alquil C₁₋₄oxicarbonilamino-, -alquinil C₃₋₇-CO-NH- opcionalmente sustituido con amino, mono- o di(alquil C₁₋₄)amino o alquil C₁₋₄oxicarbonilamino-, -alquil C₁₋₅-oxi-alquil C₁₋₅-, -alquil C₁₋₅-NR¹³-alquil C₁₋₅-, -alquil C₁₋₅-NR¹⁴-CO-alquil C₁₋₅-, -alquil C₁₋₅-CO-NR¹⁵-alquil C₁₋₅-, -alquil C₁₋₆-CO-NH-, -alquil C₁₋₆-NH-CO-, -alquil C₁₋₃-NH-CS-Het²⁰-, -alquil C₁₋₃-NH-CO-Het²⁰-, alquil C₁₋₂-CO-Het²¹-CO-, -Het²²-CH₂-CO-NH-alquil C₁₋₃-, -CO-NH-alquil C₁₋₆-, -NH-CO-alquil C₁₋₆-, -CO-alquil C₁₋₇-, -alquil C₁₋₇-CO-, -alquil C₁₋₆-CO-alquil C₁₋₆-, -alquil C₁₋₂-NH-CO-CR¹⁶R¹⁷-NH-, -alquil C₁₋₂-CO-NH-CR¹⁸R¹⁹-CO-, -alquil C₁₋₂-CO-NR²⁰-alquil C₁₋₃-CO-, -alquil C₁₋₂-NR²¹-CH₂-CO-NH-alquil C₁₋₃-, o -NR²²-CO-alquil C₁₋₃-NH-; X¹ representa un enlace directo, O, -O-alquil C₁₋₂-, CO, -CO-alquil C₁₋₂-, NR¹¹, -NR¹¹-alquil C₁₋₂-, -CH₂-, -O-N=CH- o -alquil C₁₋₂-; X² representa un enlace directo, O, -O-alquil C₁₋₂-, CO, -CO-alquil C₁₋₂-, NR¹², -NR¹²-alquil C₁₋₂-, -CH₂-, -O-N=CH- o -alquil C₁₋₂-; R¹ representa hidrógeno, ciano, halo, hidroxi, formilo, alcoxi C₁₋₆-, alquil C₁₋₆-, halo-fenil-carbonilamino-, alcoxi C₁₋₆- sustituido con halo, alquilo C₁₋₄ sustituido con uno o cuando sea posible dos o más sustituyentes seleccionados de hidroxi o halo; R² representa hidrógeno, ciano, halo, hidroxi, hidroxicarbonil-, Het¹⁶-carbonil-, alquil C₁₋₄oxicarbonil-, alquil C₁₋₄carbonil-, aminocarbonil-, mono- o di(alquil C₁₋₄)aminocarbonil-, Het¹, formilo, alquil C₁₋₄-, alquinil C₂₋₆-, cicloalquil C₃₋₆-, cicloalquil C₃₋₆oxi-, alcoxi C₁₋₆-, Ar⁵, Ar¹-oxi-, dihidroxiborano, alcoxi C₁₋₆- sustituido con halo, alquilo C₁₋₄ sustituido con uno o cuando sea posible dos o más sustituyentes seleccionados a partir de halo, hidroxi o NR⁵R⁶, alquil C₁₋₄carbonil- en donde dicho alquilo C₁₋₄ está opcionalmente sustituido con uno o cuando sea posible dos o más sustituyentes seleccionados a partir de hidroxi o alquil C₁₋₄-oxi-; R³ representa hidrógeno, alquilo C₁₋₄, o alquilo C₁₋₄ sustituido con uno o más sustituyentes seleccionados a partir de halo, alquil C₁₋₄oxi-, amino-, mono- o di(alquil C₁₋₄)amino-, alquil C₁₋₄-sulfonil- o fenilo; R⁴ representa hidrógeno, hidroxi, Ar³-oxi, Ar⁴-alquil C₁₋₄oxi-, alquil C₁₋₄oxi-, alquenil C₂₋₄oxi- opcionalmente sustituido con Het¹² o R⁴ representa alquil C₁₋₄oxi sustituido con uno o cuando sea posible dos o más sustituyentes seleccionados a partir de alquil C₁₋₄oxi-, hidroxi, halo, Het²-, -NR⁷R⁸, -carbonil-NR⁹R¹⁰ o Het³-carbonil-; R⁵ y R⁶ están cada uno independientemente seleccionados a partir de hidrógeno o alquilo C₁₋₄; R⁷ y R⁸ están cada uno independientemente seleccionados a partir de hidrógeno, alquilo C₁₋₄, Het⁸, aminosulfonil-, mono- o di(alquil C₁₋₄)-aminosulfonil, hidroxi-alquil C₁₋₄-, alquil C₁₋₄-oxi-alquil C₁₋₄-, hidroxicarbonil-alquil C₁₋₄-, cicloalquil C₃₋₆, Het⁹-carbonil-alquil C₁₋₄-, Het¹⁰-carbonil-, polihidroxi-alquil C₁₋₄-, Het¹¹-alquil C₁₋₄- o Ar²-alquil C₁₋₄-; R⁹ y R¹⁰ están cada uno independientemente seleccionados a partir de hidrógeno, alquilo C₁₋₄, cicloalquilo C₃₋₆, Het⁴, hidroxi-alquil C₁₋₄-, alquil C₁₋₄oxialquil C₁₋₄- o polihidroxi-alquil C₁₋₄-; R¹¹ representa hidrógeno, alquilo C₁₋₄, Het⁵, Het⁶-alquil C₁₋₄-, alquenil C₂₋₄carbonil- opcionalmente sustituido con Het⁷-alquil C₁₋₄aminocarbonil-, alquenil C₂₋₄sulfonil-, alquil C₁₋₄oxialquil C₁₋₄- o fenilo opcionalmente sustituido con uno o cuando sea posible dos o más sustituyentes seleccionados a partir de hidrógeno, hidroxi, amino o alquil C₁₋₄oxi-; R¹² representa hidrógeno, alquilo C₁₋₄, alquil C₁₋₄-oxi-carbonil-, Het¹⁸-alquil C₁₋₄-, fenil-alquil C₁₋₄-oxi-carbonil-, Het¹⁷, alquenil C₂₋₄carbonil- opcionalmente sustituido con Het¹⁹-alquil C₁₋₄aminocarbonil-, alquenil C₂₋₄sulfonil-, alquil C₁₋₄oxialquil C₁₋₄- o R¹² representa fenilo opcionalmente sustituido con uno o cuando sea posible dos o más sustituyentes seleccionados a partir de hidrógeno, hidroxi, amino o alquil C₁₋₄oxi-; R¹³ representa hidrógeno, alquilo C₁₋₄, Het¹³, Het¹⁴-alquil C₁₋₄- o fenilo opcionalmente sustituido con uno o cuando sea posible dos o más sustituyentes seleccionados a partir de hidrógeno, hidroxi, amino o alquil C₁₋₄oxi-; R¹⁴ y R¹⁵ están cada uno independientemente seleccionados a partir de hidrógeno, alquilo C₁₋₄, Het¹⁵-alquil C₁₋₄- o alquil C₁₋₄oxialquil C₁₋₄-; R¹⁶ y R¹⁷ cada uno independientemente representa hidrógeno o alquilo C₁₋₄ opcionalmente sustituido con fenilo, indolilo, metilsulfuro, hidroxi, tiol, hidroxifenilo, aminocarbonilo, hidroxicarbonilo, amina, imidazoilo o guanidino; R¹⁸ y R¹⁹ cada uno independientemente representa hidrógeno o alquilo C₁₋₄ opcionalmente sustituido con fenilo, indolilo, metilsulfuro, hidroxi, tiol, hidroxifenilo, aminocarbonilo, hidroxicarbonilo, amina, imidazoilo o guanidino; R²⁰ y R²² cada uno independientemente representa hidrógeno o alquilo C₁₋₄ opcionalmente sustituido con hidroxi o alquil C₁₋₄oxi; R²¹ representa hidrógeno, alquilo C₁₋₄, Het²³-alquil C₁₋₄carbonil- o R²¹ representa mono- o di(alquil C₁₋₄)amino-alquil C₁₋₄-carbonil- opcionalmente sustituido con hidroxi, pirimidinilo, dimetilamina o alquil C₁₋₄oxi; Het¹ representa un heterociclo seleccionado a partir de piperidinilo, morfolinilo, piperazinilo, furanilo, pirazolilo, dioxolanilo, tiazolilo, oxazolilo, imidazolilo, isoxazolilo, oxadiazolilo, piridinilo o pirrolidinilo en donde dicho Het¹ está opcionalmente sustituido con amino, alquilo C₁₋₄, hidroxi-alquil C₁₋₄, fenilo, fenil-alquil C₁₋₄-, alquil C₁₋₄-oxi-alquil C₁₋₄-, mono- o di(alquil C₁₋₄)amino- o amino-carbonil-; Het² representa un heterociclo seleccionado a partir de morfolinilo, piperazinilo, piperidinilo, pirrolidinilo, tiomorfolinilo o ditianilo en donde dicho Het² está opcionalmente sustituido con uno o cuando sea posible dos o más sustituyentes seleccionados a partir de hidroxi, halo, amino, alquil C₁₋₄-, hidroxi-alquil C₁₋₄-, alquil C₁₋₄-oxi-alquil C₁₋₄-, hidroxi-alquil C₁₋₄-oxi-alquil C₁₋₄-, mono- o di(alquil C₁₋₄)amino-, mono- o di(alquil C₁₋₄)amino-alquil C₁₋₄-, aminoalquil C₁₋₄-, mono- o di(alquil C₁₋₄)amino-sulfonil-, aminosulfonil-; Het³, Het⁴ y Het⁸ cada uno independientemente representa un heterociclo seleccionado a parti
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP0305723 | 2003-05-27 | ||
| EP0310266 | 2003-09-15 | ||
| EP0351061 | 2003-12-18 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR092137A2 true AR092137A2 (es) | 2015-03-25 |
Family
ID=33493782
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP040101806A AR045687A1 (es) | 2003-05-27 | 2004-05-26 | Macrociclos derivados de la quinazolina, procesos de preparacion y composiciones farmaceuticas que los contienen |
| ARP130102897A AR092137A2 (es) | 2003-05-27 | 2013-08-15 | Derivados macrociclicos de quinazolina utiles como agentes antiproliferativos |
Family Applications Before (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP040101806A AR045687A1 (es) | 2003-05-27 | 2004-05-26 | Macrociclos derivados de la quinazolina, procesos de preparacion y composiciones farmaceuticas que los contienen |
Country Status (32)
| Country | Link |
|---|---|
| US (4) | US7648975B2 (es) |
| EP (2) | EP1633365B1 (es) |
| JP (1) | JP4887151B2 (es) |
| KR (1) | KR101143878B1 (es) |
| CN (1) | CN102718775B (es) |
| AR (2) | AR045687A1 (es) |
| AT (1) | ATE544454T1 (es) |
| AU (1) | AU2004243487B2 (es) |
| BR (1) | BRPI0410714B8 (es) |
| CA (1) | CA2525214C (es) |
| CL (1) | CL2004001267A1 (es) |
| CO (1) | CO5640038A2 (es) |
| CY (1) | CY1113002T1 (es) |
| DK (1) | DK1633365T3 (es) |
| EA (1) | EA009064B1 (es) |
| ES (1) | ES2381976T3 (es) |
| HK (1) | HK1176350A1 (es) |
| HR (1) | HRP20120351T1 (es) |
| IL (3) | IL172154A0 (es) |
| IS (1) | IS3030B (es) |
| JO (1) | JO2785B1 (es) |
| MX (1) | MXPA05012762A (es) |
| MY (1) | MY148633A (es) |
| NO (1) | NO334209B1 (es) |
| NZ (1) | NZ544154A (es) |
| PA (1) | PA8603801A1 (es) |
| PL (1) | PL1633365T3 (es) |
| PT (1) | PT1633365E (es) |
| SI (1) | SI1633365T1 (es) |
| TW (3) | TWI468397B (es) |
| UA (1) | UA84010C2 (es) |
| WO (1) | WO2004105765A1 (es) |
Families Citing this family (51)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JO2785B1 (en) * | 2003-05-27 | 2014-03-15 | شركة جانسين فارماسوتيكا ان. في | Quinazoline derivatives |
| WO2005048948A2 (en) * | 2003-11-13 | 2005-06-02 | Ambit Biosciences Corporation | Urea derivatives as kinase modulators |
| CA2549728C (en) | 2003-12-18 | 2015-07-21 | Janssen Pharmaceutica N.V. | 3-cyano-quinoline derivatives with antiproliferative activity |
| UA83881C2 (en) | 2003-12-18 | 2008-08-26 | Янссен Фармацевтика Н.В. | Pyrido- and pyrimidopyrimidine derivatives as anti-proliferative agents |
| NI200700147A (es) | 2004-12-08 | 2019-05-10 | Janssen Pharmaceutica Nv | Derivados de quinazolina inhibidores de cinasas dirigidos a multip |
| JO3088B1 (ar) * | 2004-12-08 | 2017-03-15 | Janssen Pharmaceutica Nv | مشتقات كوينازولين كبيرة الحلقات و استعمالها بصفتها موانع كينيز متعددة الاهداف |
| MY169441A (en) | 2004-12-08 | 2019-04-11 | Janssen Pharmaceutica Nv | 2,4, (4,6) pyrimidine derivatives |
| PT1854789E (pt) | 2005-02-23 | 2013-10-23 | Shionogi & Co | Derivado de quinazolina possuindo actividade inibidora de tirosina-cinase |
| GB0509227D0 (en) * | 2005-05-05 | 2005-06-15 | Chroma Therapeutics Ltd | Intracellular enzyme inhibitors |
| ES2330789T3 (es) * | 2005-06-30 | 2009-12-15 | Janssen Pharmaceutica Nv | Anilino-piridinotriazinas ciclicas como inhibidores de gsk-3. |
| MX2009000456A (es) * | 2006-07-13 | 2009-01-27 | Janssen Pharmaceutica Nv | Derivados de quinazolina mtki. |
| 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 |
| US7977347B2 (en) * | 2006-09-11 | 2011-07-12 | Curis, Inc. | Quinazoline based EGFR inhibitors |
| CN101535279B (zh) | 2006-09-11 | 2015-05-20 | 柯瑞斯公司 | 含锌结合基的喹唑啉基egfr抑制剂 |
| EA200970420A1 (ru) * | 2006-10-27 | 2009-12-30 | Янссен Фармацевтика Нв | Применение mtki 1 для лечения или предупреждения рака кости |
| WO2008049930A2 (en) * | 2006-10-27 | 2008-05-02 | Janssen Pharmaceutica Nv | A method for profiling kinase inhibitors |
| AU2007310843A1 (en) * | 2006-10-27 | 2008-05-02 | Janssen Pharmaceutica Nv | Macrocyclic quinazoline derivatives as VEGFR3 inhibitors |
| EA200970418A1 (ru) * | 2006-10-27 | 2009-10-30 | Янссен Фармацевтика Нв | Применение мультитаргетного ингибитора киназ для лечения или предупреждения рака головного мозга |
| WO2008087736A1 (ja) * | 2007-01-19 | 2008-07-24 | Ube Industries, Ltd. | アラルキルオキシ又はヘテロアラルキルオキシ基を有する芳香族アミンの製法 |
| US8642067B2 (en) | 2007-04-02 | 2014-02-04 | Allergen, Inc. | Methods and compositions for intraocular administration to treat ocular conditions |
| EP2185562B1 (en) | 2007-07-27 | 2015-12-02 | Janssen Pharmaceutica, N.V. | Pyrrolopyrimidines useful for the treatment of proliferative diseases |
| US8119616B2 (en) | 2007-09-10 | 2012-02-21 | Curis, Inc. | Formulation of quinazoline based EGFR inhibitors containing a zinc binding moiety |
| CL2008003384A1 (es) * | 2007-11-14 | 2009-12-11 | Enanta Pharm Inc | Compuestos derivados de quinoxalina macrocíclica, inhibidores de serina proteasa; composicion farmaceutica que los comprende; y su uso en el tratamiento de la hepatitis c. |
| US8426430B2 (en) | 2008-06-30 | 2013-04-23 | Hutchison Medipharma Enterprises Limited | Quinazoline derivatives |
| CN103965200B (zh) | 2008-09-22 | 2016-06-08 | 阵列生物制药公司 | 作为trk激酶抑制剂的取代的咪唑并[1,2-b]哒嗪化合物 |
| LT3372605T (lt) | 2008-10-22 | 2022-02-10 | Array Biopharma, Inc. | Pakeistieji pirazolo[1,5-a]pirimidino junginiai, kaip trk kinazės inhibitoriai |
| WO2010085597A1 (en) * | 2009-01-23 | 2010-07-29 | Incyte Corporation | Macrocyclic compounds and their use as kinase inhibitors |
| AR077468A1 (es) | 2009-07-09 | 2011-08-31 | Array Biopharma Inc | Compuestos de pirazolo (1,5 -a) pirimidina sustituidos como inhibidores de trk- quinasa |
| TWI406853B (zh) * | 2010-04-07 | 2013-09-01 | Dev Center Biotechnology | Ｅｇｆｒ與ｖｅｇｆｒ－２雙重抑制劑及其用途與製法 |
| KR102132405B1 (ko) * | 2010-05-20 | 2020-07-09 | 어레이 바이오파마 인크. | Trk 키나제 저해제로서의 매크로시클릭 화합물 |
| WO2013126015A1 (en) | 2012-02-23 | 2013-08-29 | N. V. Nutricia | Composition comprising non- digestible oligosaccharides |
| DK2822953T5 (en) * | 2012-03-06 | 2017-09-11 | Pfizer | Macrocyclic derivatives for the treatment of proliferative diseases |
| CN104513253A (zh) * | 2013-10-01 | 2015-04-15 | 南京波尔泰药业科技有限公司 | 用于治疗增殖性疾病的大环化合物 |
| JP6382997B2 (ja) * | 2014-02-07 | 2018-08-29 | エクセセーラ ファーマシューティカルズ インコーポレイテッド | 治療用化合物および組成物 |
| 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 |
| RS64122B1 (sr) | 2014-11-16 | 2023-05-31 | Array Biopharma Inc | Kristalni oblik (s)-n-(5-((r)-2-(2,5-difluorofenil)-pirolidin-1-il)-pirazolo[1,5-a]pirimidin-3-il)-3-hidroksipirolidin-1-karboksamid hidrogensulfata |
| CN108473435A (zh) | 2015-10-05 | 2018-08-31 | 纽约市哥伦比亚大学理事会 | 自噬潮和磷脂酶d的活化剂以及包括tau的蛋白聚集体的清除和蛋白质病的治疗 |
| BR112018008357A2 (pt) | 2015-10-26 | 2018-11-27 | Array Biopharma Inc | mutações de ponto em câncer resistente a inibidor de trk e métodos relacionados às mesmas |
| EP3423113B1 (en) | 2016-02-29 | 2020-09-02 | Oncodesign S.A. | Radiolabeled macrocyclic egfr inhibitor |
| US10045991B2 (en) | 2016-04-04 | 2018-08-14 | Loxo Oncology, Inc. | Methods of treating pediatric cancers |
| AU2017246554B2 (en) | 2016-04-04 | 2022-08-18 | Loxo Oncology, Inc. | Liquid formulations of (S)-N-(5-((R)-2-(2,5-difluorophenyl)-pyrrolidin-1-yl)-pyrazolo(1,5-a)pyrimidin-3-yl)-3-hydroxypyrrolidine-1-carboxamide |
| HRP20230704T1 (hr) | 2016-05-18 | 2023-10-27 | Loxo Oncology, Inc. | Priprava (s)-n-(5-((r)-2-(2,5-difluorfenil)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 |
| WO2019113542A1 (en) * | 2017-12-07 | 2019-06-13 | Amplyx Pharmaceuticals, Inc. | Heterocycle substituted pyridine derivative antifungal agents |
| CA3104653A1 (en) | 2018-06-25 | 2020-01-02 | Amplyx Pharmaceuticals, Inc. | Pyridine derivatives substituted by heterocyclic ring and amino group |
| WO2021216440A1 (en) * | 2020-04-20 | 2021-10-28 | Tenova Pharmaceuticals Inc. | Novel protein kinase inhibitors |
| WO2023114809A1 (en) | 2021-12-16 | 2023-06-22 | Kinnate Biopharma Inc. | Inhibitors of met kinase |
| WO2024017258A1 (zh) * | 2022-07-19 | 2024-01-25 | 百极弘烨(南通)医药科技有限公司 | Egfr小分子抑制剂、含其的药物组合物及其用途 |
Family Cites Families (15)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| BE558251A (es) | 1956-06-11 | |||
| DE2423536A1 (de) * | 1974-05-15 | 1975-11-27 | Bayer Ag | 3-amino-phenylessigsaeure-derivate, verfahren zu ihrer herstellung sowie ihre verwendung als herbizide |
| US4066772A (en) * | 1975-07-21 | 1978-01-03 | Janssen Pharmaceutica N.V. | 1,3-Dihydro-1-[3-(1-piperidinyl)propyl]-2H-benzimidazol-2-ones and related compounds |
| NZ181256A (en) | 1975-07-21 | 1978-04-28 | Janssen Pharmaceutica Nv | 1-(w-benzazol-11-ylalkyl)-piperidine derivatives and pharmaceutical compositions containing certain of these derivatives |
| US4126687A (en) | 1976-05-17 | 1978-11-21 | Janssen Pharmaceutica N.V. | Antiemetic, 1-(benzimidazolyl-alkyl)-piperidine derivatives |
| US5721237A (en) | 1991-05-10 | 1998-02-24 | Rhone-Poulenc Rorer Pharmaceuticals Inc. | Protein tyrosine kinase aryl and heteroaryl quinazoline compounds having selective inhibition of HER-2 autophosphorylation properties |
| GB9510757D0 (en) * | 1994-09-19 | 1995-07-19 | Wellcome Found | Therapeuticaly active compounds |
| GB9508538D0 (en) | 1995-04-27 | 1995-06-14 | Zeneca Ltd | Quinazoline derivatives |
| RO121900B1 (ro) * | 1996-04-12 | 2008-07-30 | Warner-Lambert Company | Compuşi inhibitori, ireversibili, ai tirozin kinazelor, compoziţie farmaceutică care îi conţine şi utilizarea acestora |
| GB9718972D0 (en) * | 1996-09-25 | 1997-11-12 | Zeneca Ltd | Chemical compounds |
| CN1158266C (zh) | 1998-10-01 | 2004-07-21 | 阿斯特拉曾尼卡有限公司 | 化合物 |
| FR2809400B1 (fr) * | 2000-05-25 | 2004-04-09 | Inst Francais Du Petrole | Materiaux comportant des groupements organiques contenant du soufre et du phosphore lie par l'intermediaire d'atomes d'oxygenes a un oxyde mineral |
| JO2785B1 (en) * | 2003-05-27 | 2014-03-15 | شركة جانسين فارماسوتيكا ان. في | Quinazoline derivatives |
| JO3088B1 (ar) * | 2004-12-08 | 2017-03-15 | Janssen Pharmaceutica Nv | مشتقات كوينازولين كبيرة الحلقات و استعمالها بصفتها موانع كينيز متعددة الاهداف |
| GB2446974B (en) * | 2006-04-13 | 2009-01-14 | Siemens Magnet Technology Ltd | A solenoidal magnet structure |
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