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
- 230000001028 anti-proliverative effect Effects 0.000 title 1
- JWVCLYRUEFBMGU-UHFFFAOYSA-N quinazoline Chemical compound N1=CN=CC2=CC=CC=C21 JWVCLYRUEFBMGU-UHFFFAOYSA-N 0.000 title 1
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 abstract 38
- -1 hydroxy, formyl Chemical group 0.000 abstract 20
- 229910052739 hydrogen Inorganic materials 0.000 abstract 18
- 239000001257 hydrogen Substances 0.000 abstract 18
- 150000002431 hydrogen Chemical group 0.000 abstract 14
- 125000000217 alkyl group Chemical group 0.000 abstract 9
- 125000001475 halogen functional group Chemical group 0.000 abstract 9
- 125000004356 hydroxy functional group Chemical group O* 0.000 abstract 9
- 125000001424 substituent group Chemical group 0.000 abstract 9
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 abstract 8
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 6
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 abstract 4
- 125000006527 (C1-C5) alkyl group Chemical group 0.000 abstract 3
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 abstract 3
- 125000003342 alkenyl group Chemical group 0.000 abstract 3
- 125000000623 heterocyclic group Chemical group 0.000 abstract 3
- 125000006273 (C1-C3) alkyl group Chemical group 0.000 abstract 2
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 2
- QMMFVYPAHWMCMS-UHFFFAOYSA-N Dimethyl sulfide Chemical group CSC QMMFVYPAHWMCMS-UHFFFAOYSA-N 0.000 abstract 2
- ROSDSFDQCJNGOL-UHFFFAOYSA-N Dimethylamine Chemical group CNC ROSDSFDQCJNGOL-UHFFFAOYSA-N 0.000 abstract 2
- 150000001412 amines Chemical group 0.000 abstract 2
- 125000003917 carbamoyl group Chemical group [H]N([H])C(*)=O 0.000 abstract 2
- 125000004093 cyano group Chemical group *C#N 0.000 abstract 2
- 125000002795 guanidino group Chemical group C(N)(=N)N* 0.000 abstract 2
- ORTFAQDWJHRMNX-UHFFFAOYSA-N hydroxidooxidocarbon(.) Chemical group O[C]=O ORTFAQDWJHRMNX-UHFFFAOYSA-N 0.000 abstract 2
- 125000004464 hydroxyphenyl group Chemical group 0.000 abstract 2
- 125000001041 indolyl group Chemical group 0.000 abstract 2
- 125000002757 morpholinyl group Chemical group 0.000 abstract 2
- 125000004193 piperazinyl group Chemical group 0.000 abstract 2
- 125000003386 piperidinyl group Chemical group 0.000 abstract 2
- 125000000719 pyrrolidinyl group Chemical group 0.000 abstract 2
- 150000003573 thiols Chemical group 0.000 abstract 2
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 abstract 1
- 125000000815 N-oxide group Chemical group 0.000 abstract 1
- 125000005037 alkyl phenyl group Chemical group 0.000 abstract 1
- ZADPBFCGQRWHPN-UHFFFAOYSA-N boronic acid Chemical group OBO ZADPBFCGQRWHPN-UHFFFAOYSA-N 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 229920001577 copolymer Chemical group 0.000 abstract 1
- 125000005879 dioxolanyl group Chemical group 0.000 abstract 1
- 125000005883 dithianyl group Chemical group 0.000 abstract 1
- 125000002485 formyl group Chemical group [H]C(*)=O 0.000 abstract 1
- 125000002541 furyl group Chemical group 0.000 abstract 1
- 125000002883 imidazolyl group Chemical group 0.000 abstract 1
- 125000000842 isoxazolyl group Chemical group 0.000 abstract 1
- 125000001715 oxadiazolyl group Chemical group 0.000 abstract 1
- 125000002971 oxazolyl group Chemical group 0.000 abstract 1
- 125000003226 pyrazolyl group Chemical group 0.000 abstract 1
- 125000004076 pyridyl group Chemical group 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 125000000335 thiazolyl group Chemical group 0.000 abstract 1
- 125000004568 thiomorpholinyl group Chemical group 0.000 abstract 1
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
- 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 (31)
| 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) |
| 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) | TWI468372B (es) |
| UA (1) | UA84010C2 (es) |
| WO (1) | WO2004105765A1 (es) |
Families Citing this family (53)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JO2785B1 (en) * | 2003-05-27 | 2014-03-15 | شركة جانسين فارماسوتيكا ان. في | Quinazoline derivatives |
| US20050267182A1 (en) * | 2003-11-13 | 2005-12-01 | Ambit Biosciences Corporation | Urea derivatives as FLT-3 modulators |
| UA83880C2 (en) | 2003-12-18 | 2008-08-26 | Янссен Фармацевтика Н.В. | 3-cyano-quinoline derivatives with antiproliferative activity |
| JP4936897B2 (ja) | 2003-12-18 | 2012-05-23 | ジヤンセン・フアーマシユーチカ・ナームローゼ・フエンノートシヤツプ | 抗増殖剤としてのピリド−およびピリミドピリミジン誘導体 |
| 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 |
| NI200700147A (es) * | 2004-12-08 | 2019-05-10 | Janssen Pharmaceutica Nv | Derivados de quinazolina inhibidores de cinasas dirigidos a multip |
| 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 |
| CN101341138B (zh) * | 2005-06-30 | 2012-11-14 | 詹森药业有限公司 | 作为gsk-3抑制剂的环状苯胺基-吡啶并三嗪类 |
| 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 |
| CA2662587C (en) * | 2006-09-11 | 2013-08-06 | Curis, Inc. | Quinazoline based egfr inhibitors |
| US7547781B2 (en) | 2006-09-11 | 2009-06-16 | Curis, Inc. | Quinazoline based EGFR inhibitors containing a zinc binding moiety |
| US8604044B2 (en) | 2006-09-11 | 2013-12-10 | Curis, Inc. | Quinazoline based EGFR inhibitors containing a zinc binding moiety |
| BRPI0718061A2 (pt) * | 2006-10-27 | 2013-11-05 | Janssen Pharmaceutica Nv | Inibidores de vegfr3 |
| WO2008049904A2 (en) * | 2006-10-27 | 2008-05-02 | Janssen Pharmaceutica Nv | Use of mtki 1 for treating or preventing bone cancer |
| WO2008049901A1 (en) * | 2006-10-27 | 2008-05-02 | Janssen Pharmaceutica Nv | Use of a mt kinase inhibitor for treating or preventing brain cancer |
| CA2664114A1 (en) * | 2006-10-27 | 2008-05-02 | Janssen Pharmaceutica Nv | A method for profiling kinase inhibitors |
| JPWO2008087736A1 (ja) * | 2007-01-19 | 2010-05-06 | 宇部興産株式会社 | 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 |
| JP5536647B2 (ja) | 2007-07-27 | 2014-07-02 | ジヤンセン・フアーマシユーチカ・ナームローゼ・フエンノートシヤツプ | ピロロピリミジン |
| 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 |
| SI2350075T1 (sl) | 2008-09-22 | 2014-06-30 | Array Biopharma, Inc. | Substituirane imidazo (1,2b)piridazinske spojine kot Trk kinazni inhibitorji |
| ES2900243T3 (es) | 2008-10-22 | 2022-03-16 | Array Biopharma Inc | Compuestos de pirazolo[1,5-a]pirimidina sustituidos como inhibidores de trk quinasa |
| 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 |
| MX2012013467A (es) | 2010-05-20 | 2013-04-29 | Array Biopharma Inc | Compuestos macrociclicos como inhibidores de trk cinasa. |
| WO2013126015A1 (en) | 2012-02-23 | 2013-08-29 | N. V. Nutricia | Composition comprising non- digestible oligosaccharides |
| BR112014022106B1 (pt) * | 2012-03-06 | 2022-08-02 | Pfizer Inc | Derivados macrocíclicos, combinação, composição e usos na fabricação de um medicamento para o tratamento de doenças |
| 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 |
| CN108892661B (zh) * | 2014-02-07 | 2023-03-14 | 艾克赛特赫拉制药有限责任公司 | 治疗化合物和组合物 |
| 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 |
| US10799505B2 (en) | 2014-11-16 | 2020-10-13 | Array Biopharma, Inc. | Crystalline form of (S)-N-(5-((R)-2-(2,5-difluorophenyl)-pyrrolidin-1-yl)-pyrazolo[1,5-A]pyrimidin-3-yl)-3-hydroxypyrrolidine-1-carboxamide hydrogen sulfate |
| KR20180086187A (ko) | 2015-10-05 | 2018-07-30 | 더 트러스티이스 오브 콜롬비아 유니버시티 인 더 시티 오브 뉴욕 | 자가포식 유동의 활성체 및 포스포리파제 d 및 타우를 포함하는 단백질 응집물의 클리어런스 및 단백질질환의 치료 |
| EP3368039A1 (en) | 2015-10-26 | 2018-09-05 | The Regents of The University of Colorado, A Body Corporate | Point mutations in trk inhibitor-resistant cancer and methods relating to the same |
| ES2833959T3 (es) * | 2016-02-29 | 2021-06-16 | Oncodesign Sa | Inhibidor del EGFR macrocíclico radiomarcado |
| HUE068971T2 (hu) | 2016-04-04 | 2025-02-28 | Loxo Oncology Inc | (S)-N-(5-((R)-2-(2,5-difluorofenil)-pirrolidin-1-il)-pirazolo[1,5-A]pirimidin-3-il) -3-hidroxipirrolidin-1-karboxamid folyékony készítményei |
| US10045991B2 (en) | 2016-04-04 | 2018-08-14 | Loxo Oncology, Inc. | Methods of treating pediatric cancers |
| PT3800189T (pt) | 2016-05-18 | 2023-07-27 | Array Biopharma Inc | Preparação de (s)-n-(5-((r)-2-(2,5- difluoropenil)pirrolidin-1-il)pirazolo[1,5-a]pirimidin-3- il)-3-hidroxipirrolidina-1-carboxamida |
| 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 |
| DK3720438T3 (da) | 2017-12-07 | 2023-10-02 | Amplyx Pharmaceuticals Inc | Svampedræbende midler, der er afledt af heterocyklus-substitueret pyridin |
| US11771688B2 (en) | 2018-06-25 | 2023-10-03 | Amplyx Pharmaceuticals, Inc. | Pyridine derivatives substituted by heterocyclic ring and amino group |
| CN115698020B (zh) * | 2020-01-31 | 2025-02-25 | 昂科迪塞恩精密医药公司(Opm) | 大环rip2-激酶抑制剂 |
| 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 |
| WO2026008023A1 (zh) * | 2024-07-04 | 2026-01-08 | 正大天晴药业集团股份有限公司 | 哒嗪胺类化合物及其医药用途 |
Family Cites Families (14)
| 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 |
| US4160836A (en) | 1976-05-17 | 1979-07-10 | Janssen Pharmaceutica N.V. | Antiemetic 1-(benzothiazolylalkyl)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 |
| GEP20012442B (en) * | 1996-04-12 | 2001-05-25 | Warner Lambert Co | Irreversible Inhibitors of Tyrosine Kinases |
| GB9718972D0 (en) * | 1996-09-25 | 1997-11-12 | Zeneca Ltd | Chemical compounds |
| DE69905264T2 (de) | 1998-10-01 | 2003-12-11 | Astrazeneca Ab, Soedertaelje | Chinolin- und chinazolin derivate und ihre verwendung als inhibitoren von krankheiten, bei denen cytokine beteiligt wird |
| 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 |
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