AR030432A1 - Uso de derivados de quinazolina en la preparacion de un medicamento para ser usado en la inhibicion de la quinasa aurora2, compuestos relacionados, y composicion farmaceutica. - Google Patents
Uso de derivados de quinazolina en la preparacion de un medicamento para ser usado en la inhibicion de la quinasa aurora2, compuestos relacionados, y composicion farmaceutica.Info
- Publication number
- AR030432A1 AR030432A1 ARP010103092A ARP010103092A AR030432A1 AR 030432 A1 AR030432 A1 AR 030432A1 AR P010103092 A ARP010103092 A AR P010103092A AR P010103092 A ARP010103092 A AR P010103092A AR 030432 A1 AR030432 A1 AR 030432A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- alkoxy
- defined above
- represents hydrogen
- hydrogen
- Prior art date
Links
- 150000001875 compounds Chemical class 0.000 title abstract 2
- 230000005764 inhibitory process Effects 0.000 title abstract 2
- 239000008194 pharmaceutical composition Substances 0.000 title abstract 2
- 229940126601 medicinal product Drugs 0.000 title 1
- JWVCLYRUEFBMGU-UHFFFAOYSA-N quinazoline Chemical class N1=CN=CC2=CC=CC=C21 JWVCLYRUEFBMGU-UHFFFAOYSA-N 0.000 title 1
- 125000000217 alkyl group Chemical group 0.000 abstract 20
- 125000006273 (C1-C3) alkyl group Chemical group 0.000 abstract 15
- 229910052739 hydrogen Inorganic materials 0.000 abstract 15
- 239000001257 hydrogen Substances 0.000 abstract 15
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 12
- 125000006274 (C1-C3)alkoxy group Chemical group 0.000 abstract 6
- 229910052757 nitrogen Inorganic materials 0.000 abstract 5
- 229910052717 sulfur Inorganic materials 0.000 abstract 5
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 abstract 4
- 229910052736 halogen Inorganic materials 0.000 abstract 4
- 150000002367 halogens Chemical class 0.000 abstract 4
- 125000004356 hydroxy functional group Chemical group O* 0.000 abstract 4
- 229910052760 oxygen Inorganic materials 0.000 abstract 4
- 125000001424 substituent group Chemical group 0.000 abstract 4
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 abstract 3
- 125000000229 (C1-C4)alkoxy group Chemical group 0.000 abstract 3
- 125000002853 C1-C4 hydroxyalkyl group Chemical group 0.000 abstract 3
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 abstract 3
- 125000000304 alkynyl group Chemical group 0.000 abstract 3
- 229910052799 carbon Inorganic materials 0.000 abstract 3
- 125000005842 heteroatom Chemical group 0.000 abstract 3
- 125000000623 heterocyclic group Chemical group 0.000 abstract 3
- 125000004043 oxo group Chemical group O=* 0.000 abstract 3
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 abstract 2
- 125000003342 alkenyl group Chemical group 0.000 abstract 2
- 125000003545 alkoxy group Chemical group 0.000 abstract 2
- 125000006615 aromatic heterocyclic group Chemical group 0.000 abstract 2
- 125000004093 cyano group Chemical group *C#N 0.000 abstract 2
- LVWZTYCIRDMTEY-UHFFFAOYSA-N metamizole Chemical compound O=C1C(N(CS(O)(=O)=O)C)=C(C)N(C)N1C1=CC=CC=C1 LVWZTYCIRDMTEY-UHFFFAOYSA-N 0.000 abstract 2
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 2
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 abstract 2
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 abstract 2
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 1
- 108090000461 Aurora Kinase A Proteins 0.000 abstract 1
- 102100032311 Aurora kinase A Human genes 0.000 abstract 1
- 125000003282 alkyl amino group Chemical group 0.000 abstract 1
- 150000001408 amides Chemical class 0.000 abstract 1
- 125000004103 aminoalkyl group Chemical group 0.000 abstract 1
- 150000001721 carbon Chemical group 0.000 abstract 1
- 125000002915 carbonyl group Chemical group [*:2]C([*:1])=O 0.000 abstract 1
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 abstract 1
- 125000004122 cyclic group Chemical group 0.000 abstract 1
- 125000000113 cyclohexyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])C1([H])[H] 0.000 abstract 1
- 125000001511 cyclopentyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 abstract 1
- 239000003814 drug Substances 0.000 abstract 1
- 150000002148 esters Chemical class 0.000 abstract 1
- 125000001475 halogen functional group Chemical group 0.000 abstract 1
- 125000001072 heteroaryl group Chemical group 0.000 abstract 1
- 125000005113 hydroxyalkoxy group Chemical group 0.000 abstract 1
- AQYSYJUIMQTRMV-UHFFFAOYSA-N hypofluorous acid Chemical compound FO AQYSYJUIMQTRMV-UHFFFAOYSA-N 0.000 abstract 1
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 abstract 1
- 125000002294 quinazolinyl group Chemical class N1=C(N=CC2=CC=CC=C12)* 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
Classifications
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/517—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
- C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
- C07D409/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
- C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Epidemiology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Abstract
El uso de derivados de quinazolina de formula (1) o una sal, éster o amida del mismo; en la cual X es O, o S, S(O) o S(O)2, o NR6 donde R6 es hidrogeno o alquilo C1-6; R5 es un anillo heteroaromático de 5 miembros opcionalmente sustituido, R1, R2, R3, R4 están independientemente seleccionados entre halo, ciano, nitro, trifluormetilo, alquilo C1-3, NR7R8 (donde R7 y R8 que pueden ser iguales o diferentes, representan cada uno hidrogeno o alquilo C1-3), o -X1R9 (donde X1 representa un enlace directo, -O-, -CH2-, -OCO-, carbonilo, -S-, -SO-, -SO2-, -NR10CO-, -CONR11-, -SO2NR12-, -NR13SO2-, o NR14 - (donde R10, R11, R12, R13 y R14 representa cada uno independientemente hidrogeno, alquilo C1-3 o alcoxi C1-3 alquilo C2-3), y R9 está seleccionado entre uno de los siguientes grupos: 1) hidrogeno o alquilo C1-5 que puede estar no sustituido o puede estar sustituido con uno o más grupos seleccionados de hidroxi, fluor o amino, 2) alquilo C1-5X2COR15 (donde X2 representa -O- o -NR16- (en el cual R15 representa hidrogeno, alquilo C1-3 o alcoxi C1-3 alquilo C2-3 y R16 representa alquilo C1-3, -NR17R18 o -OR19 (donde R17, R18 y R19, que pueden ser iguales o diferentes, representan cada uno hidrogeno, alquilo C1-3 o alcoxi C1-3 alquilo C2-3)); 3) alquilo C1-5X3R20 (donde X3 representa -O-, -S-, -SO-, -SO2-, -OCO-, -NR21CO-, -CONR22-, -SO2NR23-, -NR24SO2- o -NR25- (donde R21, R22, R23, R24 y R25 representa cada uno independientemente hidrogeno, alquilo C1-3 o alcoxi C1-3 alquilo C2-3) y R20 representa hidrogeno, alquilo C1-3, ciclopentilo, ciclohexilo o un grupo heterocíclico saturado de 5-6 miembros con 1-2 heteroátomos, seleccionados independientemente de O, S y N, donde el grupo alquilo C1-3 puede ser portador de 1 o 2 sustituyentes seleccionados de oxo, hidroxi, halogeno y alcoxi C1-4 y donde el grupo cíclico puede ser portador de uno o dos sustituyentes seleccionados de oxo, hidroxi, halogeno, alquilo C1-4, hidroxialquilo C1-4, y alcoxi C1-4; 4) alquilo C1-5 X4 alquilo C1-5 X5R26 (donde X4 y X5, que pueden ser iguales o diferentes, son cada uno -O-, -S-, -SO-, -SO2-, -NR27CO-, -CONR28-, -SO2NR29-, -NR30SO2- o -NR31- (donde R27, R28, R29, R30 y R31 cada uno independientemente representa hidrogeno, alquilo C1-3 y alcoxi C1-3 alquilo C2-3) y R26 representa hidrogeno o alquilo C1-3); 5) R32 (donde R32 es un grupo heterocíclilo saturado de 5-6 miembros (ligado a través de carbono o nitrogeno) con 1-2 heteroátomos, seleccionados independientemente de O, S y N, donde el grupo heterocíclico puede ser portador de uno o dos sustituyentes seleccionados de oxo, hidroxi, halogeno, alquilo C1-4, hidroxialquilo C1-4, alcoxi C1-4, alcoxi C1-4 alquilo C1-4 y alquilsulfonil C1-4 alquilo C1-4); 6) alquilo C1-5 R32 (donde R32 es tal como se ha definido anteriormente); 7) alquenilo C2-5 R32 (donde R32 es tal como se ha definido anteriormente); 8) alquinilo C2-5R32 (donde R32 es tal como se ha definido anteriormente); 9) R33 (donde R33 representa un grupo piridona, fenilo o un grupo heterocíclico aromático de 5-6 miembros (ligado a través de carbono o nitrogeno) con 1-3 heterátomos seleccionados de O, N y S, donde el grupo piridona, fenilo o heterocíclico aromático puede ser portador de hasta 5 sustituyentes sobre un átomo de carbono asequible, seleccionados de hidroxi, halogeno, amino, alquilo C1-4, alcoxi C1-4, hidroxialquilo C1-4, aminoalquilo C1-4, alquilamino C1-4, hidroxialcoxi C1-4, carboxi, trifluormetilo, ciano, -CONR34R35 y -NR36COR37 (donde R34, R35,R36 y R37, que pueden ser iguales o diferentes, representa cada uno hidrogeno, alquilo C1-4 o alcoxi C1-3 alquilo C2-3)); 10) alquilo C1-5R33 (donde R33 es tal como se ha definido anteriormente); 11) alquenilo C2-5 R33(donde R33 es tal como se ha definido anteriormente); 12) alquinilo C2-5R33 (donde R33 es tal como se ha definido anteriormente); 13) alquilo C1-5X6R33 (donde X6 representa -O-, -S-, -SO2-, -NR38CO-, -CONR39-, -SO2NR40-, -NR41SO2- o -NR42- (donde R38, R39, R40, R41 y R42 representa cada uno independientemente hidrogeno, alquilo C1-3 o alcoxi C1-3 alquilo C2-3) y R33 es tal como se ha definido anteriormente); 14) alquenilo C2-5X7R33 (donde X7 representa -O-, -S-, -SO-, -SO2-, -NR43CO-, -CONR44-, -SO2NR45, -NR46SO2-, o -NR47- (donde R43, R44, R45, R46 y R47 cada uno independientemente representa hidrogeno, alquilo C1-3 o alcoxi C1-3 alquilo C2-3) y R33 es tal como se ha definido anteriormente); 15) alquinilo C2-5X8R33 (donde X8 representa -O-, -S-, -SO-, -SO2-, -NR48CO-, -CONR49-, -SO2NR50-, -NR51SO2- o -NR52- (donde R48, R49, R50, R51 y R52 cada uno independientemente representa hidrogeno, alquilo C1-3 o alcoxi C1-3 alquilo C2-3) y R33 es tal como se ha definido anteriormente); 16) alquilo C1-3X9 alquilo C1-3R33 (donde X9 representa -O-, -S-, -SO-, -SO2-, -NR53CO-, -CONR54-, -SO2NR55-, -NR56SO2- o -NR57- (donde R53, R54, R55, R56 y R57 cada uno de los cuales representa independientemente hidrogeno, alquilo C1-3 o alcoxi C1-3 alquilo C2-3) y R33 es tal como se ha definido anteriormente) y 17) alquilo C1-3X9 alquilo C1-3R32 (donde X9 y R28 son tal como se han definido anteriormente); que se usa en la preparacion de un medicamento para ser usado en la inhibicion de la quinasa aurora2, compuestos relacionados, y composicion farmacéutica.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP00401842 | 2000-06-28 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR030432A1 true AR030432A1 (es) | 2003-08-20 |
Family
ID=8173742
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP010103092A AR030432A1 (es) | 2000-06-28 | 2001-06-28 | Uso de derivados de quinazolina en la preparacion de un medicamento para ser usado en la inhibicion de la quinasa aurora2, compuestos relacionados, y composicion farmaceutica. |
Country Status (26)
| Country | Link |
|---|---|
| US (2) | US6919338B2 (es) |
| EP (1) | EP1299381B1 (es) |
| JP (1) | JP2004501914A (es) |
| KR (1) | KR20030014411A (es) |
| CN (1) | CN1267431C (es) |
| AR (1) | AR030432A1 (es) |
| AT (1) | ATE394102T1 (es) |
| AU (1) | AU2001266505A1 (es) |
| BG (1) | BG107376A (es) |
| BR (1) | BR0111754A (es) |
| CA (1) | CA2412592A1 (es) |
| CZ (1) | CZ20024120A3 (es) |
| DE (1) | DE60133897D1 (es) |
| EE (1) | EE200200715A (es) |
| ES (1) | ES2305081T3 (es) |
| HU (1) | HUP0301236A2 (es) |
| IL (1) | IL153246A0 (es) |
| IS (1) | IS6656A (es) |
| MX (1) | MXPA02011974A (es) |
| NO (1) | NO20026010D0 (es) |
| NZ (1) | NZ522696A (es) |
| PL (1) | PL360439A1 (es) |
| RU (1) | RU2283311C2 (es) |
| SK (1) | SK18102002A3 (es) |
| WO (1) | WO2002000649A1 (es) |
| ZA (1) | ZA200209412B (es) |
Families Citing this family (103)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US7361678B2 (en) * | 2002-03-05 | 2008-04-22 | Transtech Pharma, Inc. | Azole derivatives and fused bicyclic azole derivatives as therapeutic agents |
| US6660731B2 (en) * | 2000-09-15 | 2003-12-09 | Vertex Pharmaceuticals Incorporated | Pyrazole compounds useful as protein kinase inhibitors |
| WO2002022607A1 (en) * | 2000-09-15 | 2002-03-21 | Vertex Pharmaceuticals Incorporated | Pyrazole compounds useful as protein kinase inhibitors |
| US7473691B2 (en) * | 2000-09-15 | 2009-01-06 | Vertex Pharmaceuticals Incorporated | Pyrazole compounds useful as protein kinase inhibitors |
| MXPA03005609A (es) * | 2000-12-21 | 2003-10-06 | Vertex Pharma | Compuestos de pirazol utiles como inhibidores de la proteina cinasa. |
| US7402585B2 (en) * | 2001-12-24 | 2008-07-22 | Astrazeneca Ab | Substituted quinazoline derivatives as inhibitors of aurora kinases |
| WO2003066629A2 (en) * | 2002-02-06 | 2003-08-14 | Vertex Pharmaceuticals Incorporated | Heteroaryl compounds useful as inhibitors of gsk-3 |
| AU2003218215A1 (en) * | 2002-03-15 | 2003-09-29 | Vertex Pharmaceuticals, Inc. | Azolylaminoazines as inhibitors of protein kinases |
| RU2004135386A (ru) * | 2002-05-06 | 2005-07-20 | Вертекс Фармасьютикалз Инкорпорейтед (Us) | Тиадиазолы или оксадиазолы и их применение в качестве ингибиторов протеинкиназы jak |
| MY141867A (en) | 2002-06-20 | 2010-07-16 | Vertex Pharma | Substituted pyrimidines useful as protein kinase inhibitors |
| EP2280003B1 (en) | 2002-07-15 | 2014-04-02 | Symphony Evolution, Inc. | Process for preparing receptor-type kinase modulators |
| CN1319968C (zh) * | 2002-08-02 | 2007-06-06 | 沃泰克斯药物股份有限公司 | 用作gsk－3的抑制剂的吡唑组合物 |
| GB0221245D0 (en) * | 2002-09-13 | 2002-10-23 | Astrazeneca Ab | Chemical process |
| UA86470C2 (ru) * | 2002-12-24 | 2009-04-27 | Астразенека Аб | Производные фосфонооксихиназолина и их фармацевтическое применение |
| SI1578755T1 (sl) * | 2002-12-24 | 2007-12-31 | Astrazeneca Ab | Fosfonooksi kinazolinski derivati in njihova farmacevtska uporaba |
| JP2006516138A (ja) * | 2002-12-24 | 2006-06-22 | アストラゼネカ アクチボラグ | キナゾリン化合物 |
| US7601718B2 (en) * | 2003-02-06 | 2009-10-13 | Vertex Pharmaceuticals Incorporated | Compositions useful as inhibitors of protein kinases |
| RU2005135337A (ru) * | 2003-04-16 | 2006-06-10 | Астразенека Аб (Se) | Производные хиназолина для лечения злокачественного новообразования |
| EP1635823A1 (en) * | 2003-05-20 | 2006-03-22 | TransTech Pharma Inc. | Rage antagonists as agents to reverse amyloidosis and diseases associated therewith |
| ATE401080T1 (de) * | 2003-06-02 | 2008-08-15 | Astrazeneca Ab | (3-((chinazolin-4-yl)amino)-1h-pyrazol-1- yl)acetamid derivate und verwandte verbindungen als aurora kinase inhibitoren zur behandlung von proliferativen erkrankungen wie krebs |
| TW200505452A (en) * | 2003-06-17 | 2005-02-16 | Astrazeneca Ab | Chemical compounds |
| GB0320793D0 (en) * | 2003-09-05 | 2003-10-08 | Astrazeneca Ab | Chemical process |
| PT2213661E (pt) | 2003-09-26 | 2011-12-15 | Exelixis Inc | Moduladores de c-met e métodos de uso |
| US20080051414A1 (en) * | 2003-10-14 | 2008-02-28 | Arizona Board Of Regents On Behalf Of The University Of Arizona | Protein Kinase Inhibitors |
| AU2004282179B2 (en) * | 2003-10-14 | 2011-05-19 | Arizona Board Of Regents On Behalf Of The University Of Arizona | Protein kinase inhibitors |
| US20090099165A1 (en) | 2003-10-14 | 2009-04-16 | Arizona Board Of Regents On Behalf Of The University Of Arizona | Protein Kinase Inhibitors |
| US20090143399A1 (en) * | 2003-10-14 | 2009-06-04 | Arizona Board Of Regents On Behalf Of The University Of Arizona | Protein Kinase Inhibitors |
| CA2540342A1 (en) * | 2003-10-31 | 2005-05-12 | Neurogen Corporation | 4-amino (aza) quinoline derivatives as capsaicin receptor agonists |
| CN1902193B (zh) * | 2003-12-04 | 2011-07-13 | 沃泰克斯药物股份有限公司 | 可用作蛋白激酶抑制剂的喹喔啉 |
| WO2005061519A1 (en) | 2003-12-19 | 2005-07-07 | Takeda San Diego, Inc. | Kinase inhibitors |
| WO2005066152A1 (en) * | 2003-12-30 | 2005-07-21 | The Brigham And Women's Hospital, Inc. | Thiophene derivatives for up-regulating hla-dm activity |
| JPWO2005090332A1 (ja) * | 2004-03-23 | 2008-01-31 | 萬有製薬株式会社 | 置換キナゾリン又はピリドピリミジン誘導体 |
| WO2005105788A1 (en) * | 2004-04-23 | 2005-11-10 | Takeda San Diego, Inc. | Indole derivatives and use thereof as kinase inhibitors |
| US7550598B2 (en) | 2004-08-18 | 2009-06-23 | Takeda Pharmaceutical Company Limited | Kinase inhibitors |
| WO2006040522A1 (en) * | 2004-10-12 | 2006-04-20 | Astrazeneca Ab | Quinoline derivatives |
| KR20070084172A (ko) * | 2004-10-12 | 2007-08-24 | 아스트라제네카 아베 | 퀴나졸린 유도체 |
| ATE479687T1 (de) | 2004-10-15 | 2010-09-15 | Takeda Pharmaceutical | Kinaseinhibitoren |
| CN1854130B (zh) * | 2005-04-15 | 2011-04-20 | 中国医学科学院药物研究所 | 喹唑啉衍生物、及其制法和药物组合物与用途 |
| GB0509227D0 (en) * | 2005-05-05 | 2005-06-15 | Chroma Therapeutics Ltd | Intracellular enzyme inhibitors |
| GB0510963D0 (en) * | 2005-05-28 | 2005-07-06 | Astrazeneca Ab | Chemical compounds |
| US7737151B2 (en) * | 2005-08-18 | 2010-06-15 | Vertex Pharmaceuticals Incorporated | Pyrazine kinase inhibitors |
| US8119655B2 (en) | 2005-10-07 | 2012-02-21 | Takeda Pharmaceutical Company Limited | Kinase inhibitors |
| CA2627808A1 (en) * | 2005-11-03 | 2007-05-18 | Vertex Pharmaceuticals Incorporated | Aminopyrimidines useful as kinase inhibitors |
| EP1785420A1 (en) * | 2005-11-14 | 2007-05-16 | 4Sc Ag | Thiazole analogues and uses thereof |
| US7560551B2 (en) | 2006-01-23 | 2009-07-14 | Amgen Inc. | Aurora kinase modulators and method of use |
| HRP20160039T1 (hr) | 2006-01-23 | 2016-02-12 | Amgen, Inc | Modulatori aurora kinaze i postupak uporabe |
| US7868177B2 (en) * | 2006-02-24 | 2011-01-11 | Amgen Inc. | Multi-cyclic compounds and method of use |
| WO2007099323A2 (en) * | 2006-03-02 | 2007-09-07 | Astrazeneca Ab | Quinoline derivatives |
| UY30183A1 (es) | 2006-03-02 | 2007-10-31 | Astrazeneca Ab | Derivados de quinolina |
| WO2007113005A2 (en) * | 2006-04-03 | 2007-10-11 | European Molecular Biology Laboratory (Embl) | 2-substituted 3-aminosulfonyl-thiophene derivatives as aurora kinase inhibitors |
| GEP20135728B (en) | 2006-10-09 | 2013-01-25 | Takeda Pharmaceuticals Co | Kinase inhibitors |
| US8883790B2 (en) | 2006-10-12 | 2014-11-11 | Astex Therapeutics Limited | Pharmaceutical combinations |
| WO2008044041A1 (en) | 2006-10-12 | 2008-04-17 | Astex Therapeutics Limited | Pharmaceutical combinations |
| WO2008057280A1 (en) | 2006-10-27 | 2008-05-15 | Amgen Inc. | Multi-cyclic compounds and methods of use |
| WO2008055233A1 (en) * | 2006-10-31 | 2008-05-08 | Supergen, Inc. | Protein kinase inhibitors |
| WO2008057940A1 (en) * | 2006-11-02 | 2008-05-15 | Vertex Pharmaceuticals Incorporated | Aminopyridines and aminopyrimidines useful as inhibitors of protein kinases |
| MX2009006690A (es) * | 2006-12-19 | 2009-07-31 | Vertex Pharma | Aminopirimidinas utiles como inhibidores de proteinas cinasas. |
| ES2435997T3 (es) * | 2007-03-09 | 2013-12-26 | Vertex Pharmaceuticals, Inc. | Aminopirimidinas útiles como inhibidores de las proteínas cinasas |
| JP2010520887A (ja) | 2007-03-09 | 2010-06-17 | バーテックス ファーマシューティカルズ インコーポレイテッド | 蛋白キナーゼの阻害剤として有用なアミノピリジン |
| JP5393489B2 (ja) * | 2007-03-09 | 2014-01-22 | バーテックス ファーマシューティカルズ インコーポレイテッド | 蛋白キナーゼの阻害剤として有用なアミノピリミジン |
| AU2008236670B2 (en) * | 2007-04-05 | 2011-12-01 | Amgen Inc. | Aurora kinase modulators and method of use |
| EP2146982A2 (en) | 2007-04-13 | 2010-01-27 | Vertex Pharmaceuticals Incorporated | Aminopyrimidines useful as kinase inhibitors |
| JP5572087B2 (ja) * | 2007-05-02 | 2014-08-13 | バーテックス ファーマシューティカルズ インコーポレイテッド | キナーゼ阻害として有用なアミノピリミジン |
| CA2685876A1 (en) | 2007-05-02 | 2008-11-13 | Vertex Pharmaceuticals Incorporated | Thiazoles and pyrazoles useful as kinase inhibitors |
| WO2008137621A1 (en) * | 2007-05-02 | 2008-11-13 | Vertex Pharmaceuticals Incorporated | Aminopyrimidines useful as kinase inhibitors |
| GB0709031D0 (en) * | 2007-05-10 | 2007-06-20 | Sareum Ltd | Pharmaceutical compounds |
| WO2008147626A2 (en) * | 2007-05-24 | 2008-12-04 | Vertex Pharmaceuticals Incorporated | Thiazoles and pyrazoles useful as kinase inhibitors |
| JP5478488B2 (ja) * | 2007-06-20 | 2014-04-23 | メルク・シャープ・アンド・ドーム・コーポレーション | Ｊａｎｕｓキナーゼの阻害剤 |
| EA201000003A1 (ru) * | 2007-06-21 | 2010-06-30 | Айрм Ллк | Ингибиторы протеинкиназ и способы их применения |
| AR067762A1 (es) * | 2007-07-31 | 2009-10-21 | Vertex Pharma | Proceso para preparar 5-fluoro-1h-pirazolo (3,4-b) piridin-3-amina y derivados de la misma |
| DE102008015032A1 (de) | 2008-03-17 | 2009-09-24 | Aicuris Gmbh & Co. Kg | Substituierte Pyrazolamide und ihre Verwendung |
| DE102008015033A1 (de) | 2008-03-17 | 2009-09-24 | Aicuris Gmbh & Co. Kg | Substituierte (Pyrazolyl-carbonyl)imidazolidinone und ihre Verwendung |
| US8404694B2 (en) * | 2008-03-20 | 2013-03-26 | Amgen Inc. | Aurora kinase modulators and method of use |
| WO2010019473A1 (en) | 2008-08-14 | 2010-02-18 | Amgen Inc. | Aurora kinase modulators and methods of use |
| JP2012501971A (ja) * | 2008-09-03 | 2012-01-26 | バーテックス ファーマシューティカルズ インコーポレイテッド | 共結晶および共結晶を含む薬学的処方物 |
| GB0820819D0 (en) | 2008-11-13 | 2008-12-24 | Sareum Ltd | Pharmaceutical compounds |
| CA2745266C (en) * | 2008-12-03 | 2018-04-10 | Yue Xu | Stem cell cultures |
| DE102008062863A1 (de) | 2008-12-17 | 2010-06-24 | Aicuris Gmbh & Co. Kg | Substituierte (Thiophenyl-carbonyl)imidazolidinone und ihre Verwendung |
| DE102008062878A1 (de) | 2008-12-17 | 2010-06-24 | Aicuris Gmbh & Co. Kg | Substituierte Furancarboxamide und ihre Verwendung |
| EP2387563B2 (en) | 2009-01-16 | 2022-04-27 | Exelixis, Inc. | Malate salt of n- (4- { [ 6, 7-bis (methyloxy) quinolin-4-yl]oxy}phenyl-n' - (4 -fluorophenyl) cyclopropane-1,1-dicarboxamide, and crystalline forms thereof for the treatment of cancer |
| KR101699991B1 (ko) * | 2009-02-11 | 2017-01-26 | 메르크 파텐트 게엠베하 | 신규의 아미노 아자헤테로시클릭 카르복사미드 |
| UA108618C2 (uk) | 2009-08-07 | 2015-05-25 | Застосування c-met-модуляторів в комбінації з темозоломідом та/або променевою терапією для лікування раку | |
| ES2467923T3 (es) | 2009-09-30 | 2014-06-13 | Transtech Pharma, Llc | Derivados de imidazol substituidos para el tratamiento de la enfermedad de Alzheimer |
| US8592396B2 (en) | 2010-04-14 | 2013-11-26 | Bristol-Myers Squibb Company | Glucokinase activators and methods of using same |
| JP5898687B2 (ja) * | 2010-11-18 | 2016-04-06 | カシナ ライラ イノバ ファーマシューティカルズ プライベート リミテッド | 置換４−（セレノフェン−２（または３）−イルアミノ）ピリミジン化合物およびその使用方法 |
| US9090633B2 (en) | 2010-11-18 | 2015-07-28 | Kasina Laila Innova Pharmaceuticals Private Limited | Substituted 4-(arylamino) selenophenopyrimidine compounds and methods of use thereof |
| US8785459B2 (en) * | 2011-12-27 | 2014-07-22 | Development Center For Biotechnology | Quinazoline compounds as kinase inhibitors |
| GB201202027D0 (en) | 2012-02-06 | 2012-03-21 | Sareum Ltd | Pharmaceutical compounds |
| US20130231340A1 (en) | 2012-03-02 | 2013-09-05 | Sareum Limited | Pharmaceutical compounds |
| CN103788085B (zh) * | 2012-10-31 | 2016-09-07 | 复旦大学 | 2-（喹唑啉-4-氨基）-5-噻唑甲酰胺类衍生物及其生物药物用途 |
| CN104098551B (zh) * | 2013-04-03 | 2019-03-22 | 广东东阳光药业有限公司 | 作为欧若拉激酶抑制剂的取代喹唑啉类衍生物 |
| JP6543258B2 (ja) | 2013-09-16 | 2019-07-10 | アストラゼネカ アクチボラグ | 治療用重合性ナノ粒子とそれを作製して使用する方法 |
| 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 |
| GB201617871D0 (en) | 2016-10-21 | 2016-12-07 | Sareum Limited | Pharmaceutical compounds |
| AR112027A1 (es) | 2017-06-15 | 2019-09-11 | Biocryst Pharm Inc | Inhibidores de alk 2 quinasa que contienen imidazol |
| GB201816369D0 (en) | 2018-10-08 | 2018-11-28 | Sareum Ltd | Pharmaceutical compounds |
| CN114302876A (zh) * | 2019-09-06 | 2022-04-08 | 英夫拉索姆有限公司 | Nlrp3抑制剂 |
| CN110746398A (zh) * | 2019-10-18 | 2020-02-04 | 刘沛友 | 4-杂环取代喹唑啉类衍生物及其制备方法和用途 |
| EP3901151A1 (en) * | 2020-04-21 | 2021-10-27 | iOmx Therapeutics AG | Halogenated-heteroaryl and other heterocyclic kinase inhibitors, and uses thereof |
| CN111574473A (zh) * | 2020-06-04 | 2020-08-25 | 宁夏农林科学院农业资源与环境研究所（宁夏土壤与植物营养重点实验室） | 一种氨基噻唑类化合物的合成方法 |
| CN113311166B (zh) * | 2021-04-28 | 2022-10-28 | 新疆农垦科学院 | 一种用于绵羊早期妊娠诊断的蛋白生物标志物及其用于绵羊早期妊娠检测的方法 |
| CN115557601B (zh) * | 2022-11-08 | 2024-11-08 | 成都理工大学 | 生物质微球及其制备方法与应用、生物反应器、地下井 |
| AU2024231943A1 (en) * | 2023-03-09 | 2025-10-16 | Cancer Research Technology Limited | Biarylamide derivatives and their use as pkmyt1 inhibitors |
Family Cites Families (15)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US3870725A (en) * | 1971-03-30 | 1975-03-11 | Lilly Industries Ltd | Nitrothiazole derivatives |
| US5710158A (en) | 1991-05-10 | 1998-01-20 | Rhone-Poulenc Rorer Pharmaceuticals Inc. | Aryl and heteroaryl quinazoline compounds which inhibit EGF and/or PDGF receptor tyrosine kinase |
| 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 |
| EP0584222B1 (en) | 1991-05-10 | 1997-10-08 | Rhone-Poulenc Rorer International (Holdings) Inc. | Bis mono-and bicyclic aryl and heteroaryl compounds which inhibit egf and/or pdgf receptor tyrosine kinase |
| NZ243082A (en) * | 1991-06-28 | 1995-02-24 | Ici Plc | 4-anilino-quinazoline derivatives; pharmaceutical compositions, preparatory processes, and use thereof |
| GB9300059D0 (en) * | 1992-01-20 | 1993-03-03 | Zeneca Ltd | Quinazoline derivatives |
| IL117620A0 (en) * | 1995-03-27 | 1996-07-23 | Fujisawa Pharmaceutical Co | Heterocyclic compounds processes for the preparation thereof and pharmaceutical compositions containing the same |
| US5651028A (en) * | 1995-05-09 | 1997-07-22 | Unisys Corporation | Data transmission system with a low peak-to-average power ratio based on distorting frequently occuring signals |
| GB9514265D0 (en) | 1995-07-13 | 1995-09-13 | Wellcome Found | Hetrocyclic compounds |
| US6716575B2 (en) * | 1995-12-18 | 2004-04-06 | Sugen, Inc. | Diagnosis and treatment of AUR1 and/or AUR2 related disorders |
| TW436485B (en) * | 1997-08-01 | 2001-05-28 | American Cyanamid Co | Substituted quinazoline derivatives |
| GB9800575D0 (en) * | 1998-01-12 | 1998-03-11 | Glaxo Group Ltd | Heterocyclic compounds |
| GB9800569D0 (en) | 1998-01-12 | 1998-03-11 | Glaxo Group Ltd | Heterocyclic compounds |
| ES2241324T3 (es) * | 1998-10-08 | 2005-10-16 | Astrazeneca Ab | Derivados de quinazolina. |
| GB9922171D0 (en) * | 1999-09-21 | 1999-11-17 | Zeneca Ltd | Chemical compounds |
-
2001
- 2001-06-21 EE EEP200200715A patent/EE200200715A/xx unknown
- 2001-06-21 CZ CZ20024120A patent/CZ20024120A3/cs unknown
- 2001-06-21 HU HU0301236A patent/HUP0301236A2/hu unknown
- 2001-06-21 ES ES01944061T patent/ES2305081T3/es not_active Expired - Lifetime
- 2001-06-21 JP JP2002505773A patent/JP2004501914A/ja active Pending
- 2001-06-21 RU RU2003102389/04A patent/RU2283311C2/ru not_active IP Right Cessation
- 2001-06-21 EP EP01944061A patent/EP1299381B1/en not_active Expired - Lifetime
- 2001-06-21 NZ NZ522696A patent/NZ522696A/en unknown
- 2001-06-21 CA CA002412592A patent/CA2412592A1/en not_active Abandoned
- 2001-06-21 IL IL15324601A patent/IL153246A0/xx unknown
- 2001-06-21 AT AT01944061T patent/ATE394102T1/de not_active IP Right Cessation
- 2001-06-21 PL PL01360439A patent/PL360439A1/xx not_active Application Discontinuation
- 2001-06-21 US US10/311,916 patent/US6919338B2/en not_active Expired - Fee Related
- 2001-06-21 CN CNB018146201A patent/CN1267431C/zh not_active Expired - Fee Related
- 2001-06-21 WO PCT/SE2001/001450 patent/WO2002000649A1/en not_active Ceased
- 2001-06-21 MX MXPA02011974A patent/MXPA02011974A/es unknown
- 2001-06-21 AU AU2001266505A patent/AU2001266505A1/en not_active Abandoned
- 2001-06-21 KR KR1020027017913A patent/KR20030014411A/ko not_active Ceased
- 2001-06-21 SK SK1810-2002A patent/SK18102002A3/sk unknown
- 2001-06-21 DE DE60133897T patent/DE60133897D1/de not_active Expired - Fee Related
- 2001-06-21 BR BR0111754-8A patent/BR0111754A/pt not_active IP Right Cessation
- 2001-06-28 AR ARP010103092A patent/AR030432A1/es not_active Application Discontinuation
-
2002
- 2002-11-19 ZA ZA200209412A patent/ZA200209412B/en unknown
- 2002-12-11 BG BG107376A patent/BG107376A/bg unknown
- 2002-12-13 NO NO20026010A patent/NO20026010D0/no unknown
- 2002-12-17 IS IS6656A patent/IS6656A/is unknown
-
2005
- 2005-03-02 US US11/070,057 patent/US20060046987A1/en not_active Abandoned
Also Published As
| Publication number | Publication date |
|---|---|
| SK18102002A3 (sk) | 2003-07-01 |
| BR0111754A (pt) | 2003-04-29 |
| JP2004501914A (ja) | 2004-01-22 |
| IS6656A (is) | 2002-12-17 |
| MXPA02011974A (es) | 2004-09-06 |
| ATE394102T1 (de) | 2008-05-15 |
| CZ20024120A3 (cs) | 2003-03-12 |
| EP1299381B1 (en) | 2008-05-07 |
| EE200200715A (et) | 2004-08-16 |
| NO20026010L (no) | 2002-12-13 |
| HUP0301236A2 (hu) | 2003-10-28 |
| HK1053124A1 (en) | 2003-10-10 |
| NO20026010D0 (no) | 2002-12-13 |
| WO2002000649A9 (en) | 2007-09-20 |
| US20060046987A1 (en) | 2006-03-02 |
| DE60133897D1 (de) | 2008-06-19 |
| US20030187002A1 (en) | 2003-10-02 |
| WO2002000649A1 (en) | 2002-01-03 |
| ES2305081T3 (es) | 2008-11-01 |
| RU2283311C2 (ru) | 2006-09-10 |
| IL153246A0 (en) | 2003-07-06 |
| AU2001266505A1 (en) | 2002-01-08 |
| NZ522696A (en) | 2004-08-27 |
| BG107376A (bg) | 2003-09-30 |
| PL360439A1 (en) | 2004-09-06 |
| EP1299381A1 (en) | 2003-04-09 |
| CN1267431C (zh) | 2006-08-02 |
| CA2412592A1 (en) | 2002-01-03 |
| ZA200209412B (en) | 2004-02-19 |
| US6919338B2 (en) | 2005-07-19 |
| KR20030014411A (ko) | 2003-02-17 |
| CN1496364A (zh) | 2004-05-12 |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| AR030432A1 (es) | Uso de derivados de quinazolina en la preparacion de un medicamento para ser usado en la inhibicion de la quinasa aurora2, compuestos relacionados, y composicion farmaceutica. | |
| AR038476A1 (es) | Derivados de quinazolina | |
| AR037881A1 (es) | Uso de derivados de oxindol | |
| AR045691A1 (es) | Derivados de heteroarilamida como receptores antagonistas p2x7 y sus usos | |
| HUP0400365A2 (hu) | 3-Fluor-pirrolidinek, mint cukorbetegség elleni szerek és a vegyületeket tartalmazó gyógyszerkészítmények | |
| AR046779A1 (es) | Derivados de pirazol, metodos para su preparacion y usos de los mismos en la fabricacion de composiciones farmaceuticas y medicamentos que los contienen con actividad inhibitoria de trk para el tratamiento o profilaxis del cancer. | |
| AR038052A1 (es) | Derivados de quinazolina como inhibidores de auroraquinasas | |
| ATE330959T1 (de) | Allosterische adenosin-rezeptor-modulatore | |
| AR025735A1 (es) | Compuestos terapeuticos | |
| ECSP066314A (es) | Derivados piridilo y su uso como agentes terapéuticos | |
| CR8859A (es) | Derivados de piridina | |
| TW200626572A (en) | Heterocyclic derivatives and their use as therapeutic agents | |
| GB9426103D0 (en) | Therapeutic agents | |
| SE0102438D0 (sv) | New compounds | |
| NO963053D0 (no) | Kosmetiske eller farmasöytiske preparater inneholdende mangiferin eller derivater derav | |
| CY1112178T1 (el) | Παραγωγα πιπεραζινης και χρηση αυτων ως θεραπευτικων παραγοντων | |
| AR036114A1 (es) | Tetrahidroimidazol[1,2-a]pirazinas y tetrahidrotriazol[4,3-a]pirazinas como inhibidores de la dipeptidil peptidasa utiles para el tratamiento o la prevencion de la diabetes | |
| AR088808A2 (es) | Derivados de 2h-piridazin-3-ona, composiciones farmaceuticas que los contienen y un proceso para la preparacion de dichos derivados y el uso de dichos derivados para la preparacion de una composicion farmaceutica | |
| DK2314582T3 (da) | Heterocykliske forbindelser som antivirusmidler | |
| AR061918A1 (es) | Compuesto biciclico que contiene nitrogeno, su uso para la fabricacion de un medicamento y composicion farmaceutica que lo comprende | |
| BR0113838A (pt) | Derivados de n-fenil-2-pirimidina-amina | |
| PT1000035E (pt) | 6-fenilfenantridinas substituidas | |
| PA8442201A1 (es) | Derivados de 6-fenilpiridil-2-amina | |
| EE200100491A (et) | Tetrahüdropüraani derivaadid, nende saamine ja kasutamine ravimainetena ning neid sisaldav farmatseutiline kompositsioon | |
| MXPA05012247A (es) | Derivados de bencimidazol nuevos. |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FA | Abandonment or withdrawal |