AR054386A1 - Moduladores de quinasas con estructuras de alquiloquinolina y alquilquinazolina - Google Patents
Moduladores de quinasas con estructuras de alquiloquinolina y alquilquinazolinaInfo
- Publication number
- AR054386A1 AR054386A1 ARP060102422A ARP060102422A AR054386A1 AR 054386 A1 AR054386 A1 AR 054386A1 AR P060102422 A ARP060102422 A AR P060102422A AR P060102422 A ARP060102422 A AR P060102422A AR 054386 A1 AR054386 A1 AR 054386A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- optionally substituted
- alkoxy
- heteroaryl
- halogen
- Prior art date
Links
- 108091000080 Phosphotransferase Proteins 0.000 title 1
- 102000020233 phosphotransferase Human genes 0.000 title 1
- 125000000217 alkyl group Chemical group 0.000 abstract 30
- 125000003545 alkoxy group Chemical group 0.000 abstract 10
- 125000001072 heteroaryl group Chemical group 0.000 abstract 10
- 125000001424 substituent group Chemical group 0.000 abstract 10
- 229910052736 halogen Inorganic materials 0.000 abstract 9
- 150000002367 halogens Chemical class 0.000 abstract 9
- -1 oxazolidinonyl Chemical group 0.000 abstract 7
- 125000003282 alkyl amino group Chemical group 0.000 abstract 6
- 125000004663 dialkyl amino group Chemical group 0.000 abstract 6
- 125000000623 heterocyclic group Chemical group 0.000 abstract 5
- 125000002887 hydroxy group Chemical group [H]O* 0.000 abstract 5
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 abstract 5
- 125000004093 cyano group Chemical group *C#N 0.000 abstract 4
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 4
- 229910052760 oxygen Inorganic materials 0.000 abstract 3
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 3
- 125000003342 alkenyl group Chemical group 0.000 abstract 2
- 125000003710 aryl alkyl group Chemical group 0.000 abstract 2
- 125000004475 heteroaralkyl group Chemical group 0.000 abstract 2
- 125000000951 phenoxy group Chemical group [H]C1=C([H])C([H])=C(O*)C([H])=C1[H] 0.000 abstract 2
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 abstract 1
- 150000001204 N-oxides Chemical class 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 125000004122 cyclic group Chemical group 0.000 abstract 1
- 125000005553 heteroaryloxy group Chemical group 0.000 abstract 1
- 125000005842 heteroatom Chemical group 0.000 abstract 1
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 abstract 1
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 abstract 1
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 239000012453 solvate Substances 0.000 abstract 1
- 229910052717 sulfur Inorganic materials 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
-
- 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
- A61P35/00—Antineoplastic agents
- A61P35/02—Antineoplastic agents specific for leukemia
-
- 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
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
-
- 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)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Hematology (AREA)
- Oncology (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
Abstract
Reivindicacion 1: Un compuesto de formula (1) y ss N-oxidos, sales, solvatos e isomeros estereoquímicos aceptables desde el punto de vista farmacéutico, donde: Q es CH2 o un enlace directo; G es O, o S; X es N o CH; Z es NH, N8alquilo), o CH2; B es fenilo, cicloalquilo, heteroarilo, un heteroarilo benzo-fusionado de nueve a diez miembros, o un heterociclilo benzo-fusionado de nueve a diez miembros, R1 y R2 se seleccionan en forma independientemente de: (a-1) a (a-6), donde n es 1, 2, 3 o 4; Y es un enlace directo, O, S, NH, o N(alquilo); Ra es alcoxi, fenoxi, heteroarilo sustituido en forma opcional con R5, hidroxilo, alquilamino, dialquilamino, oxazolidinonilo sustituido en forma opcional con R5, pirrolidinonilo sustituido en forma opcional con R5, piperidinonilo sustituido en forma opcional con R5, piperazinil-2-ona sustituida en forma opcional con R5, heterodionilo cíclico sustituido en forma opcional con R5, heterociclilo sustituido en forma opcional con R5, escuarilo sustituido en forma opcional con R5, -COORy, -CONRwRx, -N(Ry)CON(Rw)(Rx), -N(Rw)C(O)ORx, -N(Rw)CORy, -SRy, -SORy, -SO2Ry, -NRwSO2Ry, -NRwSO2Rx, -SO3Ry, -OSO2NRwRx o -SO2NRwRx; Rw y Rx se seleccionan en forma independiente de: H, alquilo, alquenilo, aralquilo o heteroaralquilo, o Rw y Rx pueden tomarse juntos, en forma opcional, para formar un anillo de 5 a 7 miembros, que cntiene en forma opcional un resto con heteroátomo seleccionado de O, NH, N(alquilo), SO, SO2, o S; Ry se selecciona de: H, alquilo, alquenilo, cicloalquilo, fenilo, aralquilo, heteroaralquilo, o heteroarilo; R5 es 1, 2 o 3 sustituyentes selecionados de manera independiente de: halogeno, ciano, trifluorometilo, amno, hidroxilo, heteroarilo, alcoxi, -C(O)alquilo, - SO2alquilo, -C(O)NH(alquilo), -C(O)N(alquilo)2, -C(O)-alquil C1-4-N(alquilo)2, alquilo, -alquilC1-4-OH, -alquil C1-4-OCH3, -C(O)alquilC1-4-OH, -C(O)alquil C1-4-OCH3, dialquilamino o alquilamino; siempre que el mismo sustituyente R5 no esté presente más de una vez, salvo que dcho sustituyente R5 sea halogeno, hidroxilo, alcoxi o alquilo; Rbb es H, halogeno, alcoxi, dialquilamino, fenilo sustituido en forma opcional con R6, heteroarilo sustituido en forma opcional con R6, piperazinil-2-ona sustituida en forma opcional con R6, imidazolidinil-2-ona sustituida en forma opcional con R6, oxazolidinil-2-ona sustituida en forma opcional con R6, o heterociclilo sustituido en forma opcional con R6; R6 es 1, 2 o 3 sustituyentes seleccionados de manera independiente de: halogeno, ciano, trifluorometilo, amino, hidroxilo, heteroarilo, alcoxi, -C(O)alquilo, -SO2alquilo, -C(O)NH(alquilo), -C(O)N(alquilo)2, -C(O)-alquilC1-4-N(alquilo)2, alquilo, -alquilC1-4-OH, -alquilC1-4-OCH3, -C(O)alquilC1-4- OH, -C(O)alquilC1-4-OCH3, dialquilamino o alquilamino, siempre que el mismo sustituyente R6 no esté presente más de una vez, salvo que dicho sustituyente R6 sea halogeno, hidroxilo, alcoxi o alquilo; Rc es heterociclilo sustituido en forma opcional con R7, o heteroarilo, y R7 es 1, 2 o 3 sustituyentes seleccionados de manera independiente de: halogeno, ciano, trifluorometilo, amino, hidroxilo, heteroarilo, alcoxi, -C(O)alquilo, -SO2alquilo, -C(O)NH(alquilo), -C(O)N(alquilo)2, -C(O)-alquilC1-4- N(alquilo)2, alquilo, -alquilC1-4-OH, -alquilC1-4-OCH3, -C(O)alquilC1-4-OH, -C(O)alquilC1-4-OCH3, dialquilamino o alquilamino, siempre que el mismo sustituyente R7 no esté presente más de una vez, a no ser que dicho sustituyente R7 sea halogeno, hidroxilo, alcoxi o alquilo; R3 es uno o más sustituyentes seleccionados de manera independiente de: H siempre que Rbb no sea H, alquilo, alcoxi, halogeno, amino sustituido en forma opcional con R4, (alquilC1-2-OH, nitro, cicloalquilo sustituido en forma opcional con R4, heteroarilo sustituido en forma opcional con R4, alquilamino, heterociclilo sustituido en forma opcional con R4, alcoxiéter, -O(cicloalquilo), pirrolidinonilo sustituido en forma opcional con R4, fenoxi sustituido en forma opcional con R4, -CN, -OCHF2, -OCF3, -CF3, alquilo halogenado, heteroariloxi sustituido en forma opcional con R4, dialquilamino, -NHSO2alquilo o -SO2alquilo; donde R4 se selecciona de manera independiente de: halogeno, cian, trifluorometilo, amino, hidroxilo, alcoxi, -C(O)alquilo, -CO2alquilo, -SO2alquilo, -C(O)N(alquilo)2, alquilo o alquilamino.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US68938405P | 2005-06-10 | 2005-06-10 | |
| US73091905P | 2005-10-27 | 2005-10-27 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR054386A1 true AR054386A1 (es) | 2007-06-20 |
Family
ID=37038081
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP060102422A AR054386A1 (es) | 2005-06-10 | 2006-06-09 | Moduladores de quinasas con estructuras de alquiloquinolina y alquilquinazolina |
Country Status (18)
| Country | Link |
|---|---|
| US (1) | US8071768B2 (es) |
| EP (1) | EP1893598A1 (es) |
| JP (1) | JP2009501135A (es) |
| KR (1) | KR20080028912A (es) |
| AR (1) | AR054386A1 (es) |
| AU (1) | AU2006257945A1 (es) |
| BR (1) | BRPI0611964A2 (es) |
| CA (1) | CA2611242A1 (es) |
| CR (1) | CR9652A (es) |
| EA (1) | EA200800017A1 (es) |
| EC (1) | ECSP077997A (es) |
| GT (1) | GT200600251A (es) |
| IL (1) | IL187692A0 (es) |
| NO (1) | NO20080174L (es) |
| PE (1) | PE20070014A1 (es) |
| TW (1) | TW200716599A (es) |
| UY (1) | UY29588A1 (es) |
| WO (1) | WO2006135721A1 (es) |
Families Citing this family (14)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US8071768B2 (en) | 2005-06-10 | 2011-12-06 | Janssen Pharmaceutica, N.V. | Alkylquinoline and alkylquinazoline kinase modulators |
| US7825244B2 (en) * | 2005-06-10 | 2010-11-02 | Janssen Pharmaceutica Nv | Intermediates useful in the synthesis of alkylquinoline and alkylquinazoline kinase modulators, and related methods of synthesis |
| US8760507B2 (en) * | 2008-08-05 | 2014-06-24 | Inspectron, Inc. | Light pipe for imaging head of video inspection device |
| WO2011078369A1 (ja) * | 2009-12-25 | 2011-06-30 | 持田製薬株式会社 | 新規アリールウレア誘導体 |
| WO2012041872A1 (en) | 2010-09-29 | 2012-04-05 | Intervet International B.V. | N-heteroaryl compounds with cyclic bridging unit for the treatment of parasitic diseases |
| WO2013014170A1 (en) | 2011-07-27 | 2013-01-31 | Ab Science | Oxazole and thiazole derivatives as selective protein kinase inhibitors (c-kit) |
| NZ716598A (en) * | 2012-11-20 | 2017-02-24 | Merial Inc | Anthelmintic compounds and compositions and method of using thereof |
| BR112016008080B1 (pt) * | 2013-10-16 | 2021-02-23 | Fujifilm Corporation | sal de ácido carboxílico ou um sal de ácido mineral, cristal de succinato, cristal de fumarato e composição farmacêutica |
| US20170305857A1 (en) * | 2013-12-20 | 2017-10-26 | Pfizer Limited | N-acylpiperidine ether tropomyosin-related kinase inhibitors |
| UY36390A (es) * | 2014-11-05 | 2016-06-01 | Flexus Biosciences Inc | Compuestos moduladores de la enzima indolamina 2,3-dioxigenasa (ido), sus métodos de síntesis y composiciones farmacéuticas que los contienen |
| CN107205970A (zh) | 2014-11-05 | 2017-09-26 | 弗莱塞斯生物科学公司 | 免疫调节剂 |
| JP6412471B2 (ja) * | 2015-07-15 | 2018-10-24 | 富士フイルム株式会社 | 含窒素複素環化合物の製造方法およびその中間体 |
| TWI731420B (zh) * | 2018-09-27 | 2021-06-21 | 大陸商深圳微芯生物科技股份有限公司 | 具有吲哚胺-2,3-雙加氧酶抑制活性的喹啉衍生物及其製備方法、藥物組合物、聯合用藥物與用途 |
| US20220154220A1 (en) * | 2018-12-21 | 2022-05-19 | MAX-PLANCK-Gesellschaft zur Förderung der Wissenschaften e.V. | Small molecules for increasing precise genome editing efficiency |
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| CL2003002353A1 (es) | 2002-11-15 | 2005-02-04 | Vertex Pharma | Compuestos derivados de diaminotriazoles, inhibidores d ela proteina quinasa; composicion farmaceutica; procedimiento de preparacion; y su uso del compuesto en el tratamiento de enfermedades de desordenes alergicos, proliferacion, autoinmunes, condic |
| DE60326646D1 (de) | 2002-12-18 | 2009-04-23 | Vertex Pharma | Benzisoxazolderivate, die sich als inhibitoren von proteinkinasen eigen |
| AU2003299791A1 (en) | 2002-12-20 | 2004-07-22 | Bayer Pharmaceuticals Corporation | Substituted 3,5-dihydro-4h-imidazol-4-ones for the treatment of obesity |
| TW200508224A (en) | 2003-02-12 | 2005-03-01 | Bristol Myers Squibb Co | Cyclic derivatives as modulators of chemokine receptor activity |
| US7163937B2 (en) | 2003-08-21 | 2007-01-16 | Bristol-Myers Squibb Company | Cyclic derivatives as modulators of chemokine receptor activity |
| CA2542076C (en) | 2003-10-14 | 2013-02-26 | Arizona Board Of Regents On Behalf Of The University Of Arizona | Substituted tricyclic compounds as protein kinase inhibitors |
| US20050130954A1 (en) | 2003-11-21 | 2005-06-16 | Mitchell Ian S. | AKT protein kinase inhibitors |
| US8071768B2 (en) | 2005-06-10 | 2011-12-06 | Janssen Pharmaceutica, N.V. | Alkylquinoline and alkylquinazoline kinase modulators |
| US7825244B2 (en) | 2005-06-10 | 2010-11-02 | Janssen Pharmaceutica Nv | Intermediates useful in the synthesis of alkylquinoline and alkylquinazoline kinase modulators, and related methods of synthesis |
-
2006
- 2006-06-06 US US11/422,349 patent/US8071768B2/en active Active
- 2006-06-07 KR KR1020087000405A patent/KR20080028912A/ko not_active Withdrawn
- 2006-06-07 CA CA002611242A patent/CA2611242A1/en not_active Abandoned
- 2006-06-07 BR BRPI0611964-6A patent/BRPI0611964A2/pt not_active Application Discontinuation
- 2006-06-07 EA EA200800017A patent/EA200800017A1/ru unknown
- 2006-06-07 PE PE2006000627A patent/PE20070014A1/es not_active Application Discontinuation
- 2006-06-07 AU AU2006257945A patent/AU2006257945A1/en not_active Abandoned
- 2006-06-07 EP EP06772652A patent/EP1893598A1/en not_active Withdrawn
- 2006-06-07 WO PCT/US2006/022414 patent/WO2006135721A1/en not_active Ceased
- 2006-06-07 JP JP2008515954A patent/JP2009501135A/ja not_active Withdrawn
- 2006-06-08 GT GT200600251A patent/GT200600251A/es unknown
- 2006-06-08 UY UY29588A patent/UY29588A1/es unknown
- 2006-06-09 AR ARP060102422A patent/AR054386A1/es not_active Application Discontinuation
- 2006-06-09 TW TW095120477A patent/TW200716599A/zh unknown
-
2007
- 2007-11-27 IL IL187692A patent/IL187692A0/en unknown
- 2007-12-10 EC EC2007007997A patent/ECSP077997A/es unknown
-
2008
- 2008-01-09 CR CR9652A patent/CR9652A/es not_active Application Discontinuation
- 2008-01-10 NO NO20080174A patent/NO20080174L/no not_active Application Discontinuation
Also Published As
| Publication number | Publication date |
|---|---|
| PE20070014A1 (es) | 2007-03-08 |
| CA2611242A1 (en) | 2006-12-21 |
| KR20080028912A (ko) | 2008-04-02 |
| JP2009501135A (ja) | 2009-01-15 |
| TW200716599A (en) | 2007-05-01 |
| IL187692A0 (en) | 2008-08-07 |
| CR9652A (es) | 2008-09-09 |
| AU2006257945A1 (en) | 2006-12-21 |
| BRPI0611964A2 (pt) | 2009-01-27 |
| GT200600251A (es) | 2007-01-12 |
| UY29588A1 (es) | 2006-10-02 |
| US8071768B2 (en) | 2011-12-06 |
| ECSP077997A (es) | 2008-01-23 |
| EP1893598A1 (en) | 2008-03-05 |
| NO20080174L (no) | 2008-02-19 |
| WO2006135721A1 (en) | 2006-12-21 |
| EA200800017A1 (ru) | 2008-08-29 |
| US20060281772A1 (en) | 2006-12-14 |
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