AR069636A1 - Triazolo triazinas y triazolopirazinas sustituidas, procedimiento para su preparacion, medicamentos que las contienen y uso de las mismas para el tratamiento y/o profilaxis de trastornos hematologicos,tales como neutropenias y leucopenias. - Google Patents
Triazolo triazinas y triazolopirazinas sustituidas, procedimiento para su preparacion, medicamentos que las contienen y uso de las mismas para el tratamiento y/o profilaxis de trastornos hematologicos,tales como neutropenias y leucopenias.Info
- Publication number
- AR069636A1 AR069636A1 ARP080105333A ARP080105333A AR069636A1 AR 069636 A1 AR069636 A1 AR 069636A1 AR P080105333 A ARP080105333 A AR P080105333A AR P080105333 A ARP080105333 A AR P080105333A AR 069636 A1 AR069636 A1 AR 069636A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- alkoxy
- amino
- aminocarbonyl
- carbonyl
- Prior art date
Links
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 title 1
- 229940079593 drug Drugs 0.000 title 1
- 239000003814 drug Substances 0.000 title 1
- 230000002489 hematologic effect Effects 0.000 title 1
- 238000000034 method Methods 0.000 title 1
- 208000004235 neutropenia Diseases 0.000 title 1
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 abstract 58
- -1 hydroxy, amino, hydroxycarbonyl Chemical group 0.000 abstract 31
- 125000000229 (C1-C4)alkoxy group Chemical group 0.000 abstract 30
- 125000001424 substituent group Chemical group 0.000 abstract 26
- 125000003917 carbamoyl group Chemical group [H]N([H])C(*)=O 0.000 abstract 21
- 125000002915 carbonyl group Chemical group [*:2]C([*:1])=O 0.000 abstract 20
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 abstract 20
- 229910052736 halogen Inorganic materials 0.000 abstract 11
- 150000002367 halogens Chemical class 0.000 abstract 11
- 229910052739 hydrogen Inorganic materials 0.000 abstract 11
- 239000001257 hydrogen Substances 0.000 abstract 11
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 11
- 125000006273 (C1-C3) alkyl group Chemical group 0.000 abstract 9
- 125000000623 heterocyclic group Chemical group 0.000 abstract 9
- 125000006297 carbonyl amino group Chemical group [H]N([*:2])C([*:1])=O 0.000 abstract 8
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 abstract 8
- 125000000217 alkyl group Chemical group 0.000 abstract 6
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 abstract 6
- 125000003545 alkoxy group Chemical group 0.000 abstract 5
- 125000004093 cyano group Chemical group *C#N 0.000 abstract 5
- 125000002887 hydroxy group Chemical group [H]O* 0.000 abstract 5
- 125000004453 alkoxycarbonyl group Chemical group 0.000 abstract 4
- 125000004457 alkyl amino carbonyl group Chemical group 0.000 abstract 4
- 125000006517 heterocyclyl carbonyl group Chemical group 0.000 abstract 4
- 125000004043 oxo group Chemical group O=* 0.000 abstract 4
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 4
- 125000003282 alkyl amino group Chemical group 0.000 abstract 3
- 125000003806 alkyl carbonyl amino group Chemical group 0.000 abstract 3
- 125000006310 cycloalkyl amino group Chemical group 0.000 abstract 3
- 229910052757 nitrogen Inorganic materials 0.000 abstract 3
- 125000001724 1,2,3-oxadiazol-4-yl group Chemical group [H]C1=C(*)N=NO1 0.000 abstract 2
- 125000001766 1,2,4-oxadiazol-3-yl group Chemical group [H]C1=NC(*)=NO1 0.000 abstract 2
- 125000001414 1,2,4-triazol-5-yl group Chemical group [H]N1N=C([H])N=C1[*] 0.000 abstract 2
- 125000004105 2-pyridyl group Chemical group N1=C([*])C([H])=C([H])C([H])=C1[H] 0.000 abstract 2
- 125000004448 alkyl carbonyl group Chemical group 0.000 abstract 2
- 125000003118 aryl group Chemical group 0.000 abstract 2
- 125000000051 benzyloxy group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])O* 0.000 abstract 2
- 125000006254 cycloalkyl carbonyl group Chemical group 0.000 abstract 2
- 125000001072 heteroaryl group Chemical group 0.000 abstract 2
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 abstract 2
- 150000003839 salts Chemical class 0.000 abstract 2
- 239000012453 solvate Substances 0.000 abstract 2
- 125000000876 trifluoromethoxy group Chemical group FC(F)(F)O* 0.000 abstract 2
- 125000004760 (C1-C4) alkylsulfonylamino group Chemical group 0.000 abstract 1
- 125000006570 (C5-C6) heteroaryl group Chemical group 0.000 abstract 1
- WNXJIVFYUVYPPR-UHFFFAOYSA-N 1,3-dioxolane Chemical compound C1COCO1 WNXJIVFYUVYPPR-UHFFFAOYSA-N 0.000 abstract 1
- RYHBNJHYFVUHQT-UHFFFAOYSA-N 1,4-Dioxane Chemical compound C1COCCO1 RYHBNJHYFVUHQT-UHFFFAOYSA-N 0.000 abstract 1
- 125000003830 C1- C4 alkylcarbonylamino group Chemical group 0.000 abstract 1
- 125000000172 C5-C10 aryl group Chemical group 0.000 abstract 1
- 125000001313 C5-C10 heteroaryl group Chemical group 0.000 abstract 1
- 101000869592 Daucus carota Major allergen Dau c 1 Proteins 0.000 abstract 1
- 101000650136 Homo sapiens WAS/WASL-interacting protein family member 3 Proteins 0.000 abstract 1
- 101001043818 Mus musculus Interleukin-31 receptor subunit alpha Proteins 0.000 abstract 1
- 102100027539 WAS/WASL-interacting protein family member 3 Human genes 0.000 abstract 1
- 125000004656 alkyl sulfonylamino group Chemical group 0.000 abstract 1
- 125000004432 carbon atom Chemical group C* 0.000 abstract 1
- SYGWYBOJXOGMRU-UHFFFAOYSA-N chembl233051 Chemical group C1=CC=C2C3=CC(C(N(CCN(C)C)C4=O)=O)=C5C4=CC=CC5=C3SC2=C1 SYGWYBOJXOGMRU-UHFFFAOYSA-N 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- ORTFAQDWJHRMNX-UHFFFAOYSA-N hydroxidooxidocarbon(.) Chemical group O[C]=O ORTFAQDWJHRMNX-UHFFFAOYSA-N 0.000 abstract 1
- 229910052760 oxygen Inorganic materials 0.000 abstract 1
- 125000006296 sulfonyl amino group Chemical group [H]N(*)S(*)(=O)=O 0.000 abstract 1
- 125000000472 sulfonyl group Chemical group *S(*)(=O)=O 0.000 abstract 1
- 229910052717 sulfur Inorganic materials 0.000 abstract 1
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/04—Ortho-condensed systems
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- Orthopedic Medicine & Surgery (AREA)
Abstract
Reivindicacion 1: Compuesto de la formula (1) en la que u representa N, V representa CR12, w representa N, A representa CR15; o u representa N, v representa N, w representa CR16, A representa N, donde R12 representa hidrogeno, hidroxilo, amino, hidroxicarbonilo, aminocarbonilo, trifluorometilo, trifluorometoxi, ciano, alquilo C1-4, alcoxi C1-4, (alquil C1-4)amino, (alquil C1-4)carbonilo, (alcoxi C1-4)carbonilo, (alquil C1-4)aminocarbonilo, (alquil C1-4)carbonilamino, alquil C1-4-sulfonilamino, heterociclilcarbonilo de 5 o 6 miembros, -CH2R13 o -CH2CH2R14, donde heterociclilcarbonilo está sustituido con 1 a 3 sustituyentes, seleccionándose los sustituyentes independientemente uno de otro del grupo constituido por halogeno, oxo, alquilo C1-4, alcoxi C1-4, (alquil C1-4)amino, (alquil C1-4)carbonilo, (alcoxi C1-4)-carbonilo y (alquil C1-4)aminocarbonilo, y donde alcoxi, alquilamino, alquilcarbonilo, alcoxicarbonilo, alquilaminocarbonilo, alquilcarbonilamino y alquilsulfonilamino pueden estar sustituidos con un sustituyente, seleccionándose el sustituyente del grupo constituido por hidroxilo, amino, hidroxicarbonilo, aminocarbonilo, alcoxi C1-4, (alquil C1-4)amino, (alcoxi C1-4)carbonilo, (alquil C1-4)aminocarbonilo, alquil C1-4-carbonilamino, heterociclilo de 5 o 6 miembros y fenilo, donde fenilo puede estar sustituido con 1 a 3 sustituyentes, seleccionándose los sustituyentes independientemente uno de otro del grupo constituido por halogeno, ciano, trifluorometilo, trifluorometoxi, aminocarbonilo, alquilo C1-4, alcoxi C1-4, (alquil C1-4)amino, (alquil C1-4)carbonilo, (alcoxi C1-4)carbonilo, (alquil C1-4)aminocarbonilo y (alquil C1-4)carbonilamino, y donde heterociclilo puede estar sustituido con 1 a 3 sustituyentes, seleccionándose los sustituyentes independientemente uno de otro del grupo constituido por halogeno, oxo, alquilo C1-4, alcoxi C1-4, (alquil C1-4)amino, (alquil C1-4)carbonilo, (alcoxi C1-4)-carbonilo y (alquil C1-4)aminocarbonilo, y donde R13 representa hidroxilo, amino, ciano, hidroxicarbonilo, aminocarbonilo, alcoxi C1-4, (alquil C1-4)amino, (alcoxi C1-4)carbonilo, (alquil C1-4)aminocarbonilo, (alquil C1-4)carbonilamino o heterociclilo de 5 o 6 miembros, donde alcoxi, alquilamino, alcoxicarbonilo, alquilaminocarbonilo y alquilcarbonilamino pueden estar sustituidos con un sustituyente, seleccionándose el sustituyente del grupo constituido por hidroxilo, amino, hidroxicarbonilo, aminocarbonilo, alcoxi C1-4, (alquil C1-4)amino, (alcoxi C1-4)carbonilo, (alquil C1-4)aminocarbonilo y (alquil C1-4)carbonilamino, y donde heterociclilo puede estar sustituido con 1 a 3 sustituyentes, seleccionándose los sustituyentes independientemente uno de otro del grupo constituido por halogeno, oxo, alquilo C1-4, alcoxi C1-4, (alquil C1-4)amino, (alquil C1-4)carbonilo, (alcoxi C1-4)-carbonilo y (alquil C1-4)aminocarbonilo, y donde R14 representa hidroxilo, amino, ciano, hidroxicarbonilo, aminocarbonilo, alcoxi C1-4, (alquil C1-4)amino, (alcoxi C1-4)carbonilo, (alquil C1-4)aminocarbonilo, (alquil C1-4)carbonilamino o heterociclilo de 5 o 6 miembros, donde alcoxi, alquilamino, alcoxicarbonilo, alquilaminocarbonilo y alquilcarbonilamino pueden estar sustituidos con un sustituyente, seleccionándose el sustituyente del grupo constituido por hidroxilo, amino, hidroxicarbonilo, aminocarbonilo, alcoxi C1-4, (alquil C1-4)amino, (alcoxi C1-4)carbonilo, (alquil C1-4)aminocarbonilo y (alquil C1-4)carbonilamino, y donde heterociclilo puede estar sustituido con 1 a 2 sustituyentes, seleccionándose los sustituyentes independientemente uno de otro del grupo constituido por halogeno, oxo, alquilo C1-4, alcoxi C1-4, (alquil C1-4)amino, (alquil C1-4)carbonilo, (alcoxi C1-4)-carbonilo y (alquil C1-4)aminocarbonilo, R15 representa hidrogeno, halogeno, ciano, trifluorometilo, alquilo C1-3, metoxi, metiltio o ciclopropilo, R16 representa hidrogeno o metilo; representa un resto del grupo de formulas (2) en las que * es el punto de union al heterociclo, n representa el numero 0 o 1; X representa NR10, S u O, donde R10 representa hidrogeno, alquilo C1-3 o ciclopropilo, Y representa NR11 o S, donde R11 representa hidrogeno, alquilo C1-3 o ciclopropilo, R3 representa pirid-2-ilo, pirimid-2-ilo, 2-aminopirimid-4-ilo, 2-(mono-(alquil C1-4)-amino)pirimid-4-ilo, 2-(mono-cicloalquilamino C3-4)pirimid-4-ilo, piridazin-3(2H)-on-6-ilo; 1,3-oxazol-2-ilo, 1,3-oxazol-4-ilo, 1,2,4-oxadiazol-3-ilo, 1,2,3-oxadiazol-4-ilo, 1,3-tiazol-2-ilo, 1,3-tiazol-4-ilo, 1H-1,2,4-triazol-5-ilo, 2,4-dihidro-3H-1,2,4-triazol-3-on-5-ilo o 1,2-pirazol-5-ilo, donde pirid-2-ilo, pirimid-2-ilo, 1,3-oxazol-2-ilo, 1,3-oxazol-4-ilo, 1,3-tiazol-2-ilo y 1,3-tiazol-4-ilo están sustituidos con 1 o 2 sustituyentes, seleccionándose los sustituyentes independientemente uno de otro del grupo constituido por halogeno, ciano, nitro, amino, trifluorometilo, trifluorometoxi, aminocarbonilo, trifluorometilcarbonilo, alquilo C1-4, alcoxi C1-4, (alquil C1-4)amino, cicloalquilamino C3-4, (alquil C1-4)carbonilo, (alcoxi C1-4)carbonilo, (alquil C1-4)aminocarbonilo y ciclo alquilcarbonilo C3-6, donde alquilo, alcoxi, alquilamino, alquilcarbonilo, alcoxicarbonilo, alquilaminocarbonilo y cicloalquilcarbonilo pueden estar sustituidos con un sustituyente, seleccionándose el sustituyente del grupo constituido por halogeno, ciano, hidroxilo, amino, trifluorometilo y cicloalquilo C3-5, y donde 2-aminopirimid-4-ilo, 2-(mono-(alquil C1-4)-amino)pirimid-4-ilo, 2-(mono-C3-4-cicloalquilamino)pirinlid-4-ilo, piridazin-3(2H)-on-6-ilo, 1,2,4-oxadiazol-3-ilo, 1,2,3-oxadiazol-4-ilo, 1H-1,2,4-triazol-5-ilo, 2,4-dihidro-3H-1,2,4-triazol-3-on-5-ilo y 1,2-pirazol-5-ilo pueden estar sustituidos con un sustituyente, seleccionándose el sustituyente del grupo constituido por halogeno, ciano, nitro, amino, trifluorometilo, trifluorometoxi, aminocarbonilo, trifluorometilcarbonilo, alquilo C1-4, alcoxi C1-4, (alquil C1-4)amino, cicloalquilamino C3-4, (alcoxi C1-4)carbonilo, (alquil C1-4)aminocarbonilo y cicloalquilcarbonilo C3-6, R4 representa hidrogeno, alquilo C1-3 o ciclopropilo, R5 representa hidrogeno o alquilo C1-3, R6 representa hidrogeno, alquilo C1-3 o ciclopropilo, R7 representa hidrogeno o alquilo C1-3, R8 representa hidrogeno, alquilo C1-3 o ciclopropilo, R9 representa hidrogeno o alquilo C1-3, R2 representa arilo C5-10 o heteroarilo de 5 a 10 miembros, donde arilo y heteroarilo pueden estar sustituidos con 1 a 3 sustituyentes, seleccionándose los sustituyentes independientemente uno de otro del grupo constituido por hidroxilo, hidroximetilo, amino, halogeno, ciano, trifluorometilo, trifluorometoxi, aminocarbonilo, alquilo C1-4, alcoxi C1-4, (alcoxi C1-4)metilo, (alquil C1-4)amino, (alquil C1-4)-aminometilo, (alquil C1-4)carbonilo, (alcoxi C1-4)carbonilo, (alquil C1-4)aminocarbonilo, (alquil C1-4)carbonilamino, (alquil C1-4)sulfonilo, (alquil C1-4)sulfonilamino, (alquil C1-4)-aminosulfonilo, fenilo, benciloxi, heterociclilo de 5 o 6 miembros, heterociclilcarbonilo de 5 o 6 miembros, heterociclilmetilo de 5 o 6 miembros y heteroarilo de 5 o 6 miembros, donde fenilo, benciloxi, heterociclilo, heterociclilcarbonilo, heterociclilmetilo y heteroarilo pueden estar sustituidos con 1 a 3 sustituyentes, seleccionándose los sustituyentes independientemente uno de otro del grupo constituido por halogeno, ciano, trifluorometilo, trifluorometoxi, aminocarbonilo, alquilo C1-4, alcoxi C1-4, (alquil C1-4)amino, (alquil C1-4)carbonilo, (alcoxi C1-4)carbonilo, (alquil C1-4)aminocarbonilo y (alquil C1-4)carbonilamino, o dos de los sustituyentes en arilo junto con los átomos de carbono a los que están unidos forman un 1,3-dioxolano o 1,4-dioxano; o una de sus sales, sus solvatos o los solvatos de sus sales.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| DE102007060172A DE102007060172A1 (de) | 2007-12-13 | 2007-12-13 | Triazolotriazine und Triazolopyrazine und ihre Verwendung |
| DE200810035209 DE102008035209A1 (de) | 2008-07-29 | 2008-07-29 | Triazolotriazine und Triazolopyrazine und ihre Verwendung |
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| AR069636A1 true AR069636A1 (es) | 2010-02-10 |
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| Application Number | Title | Priority Date | Filing Date |
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| ARP080105333A AR069636A1 (es) | 2007-12-13 | 2008-12-09 | Triazolo triazinas y triazolopirazinas sustituidas, procedimiento para su preparacion, medicamentos que las contienen y uso de las mismas para el tratamiento y/o profilaxis de trastornos hematologicos,tales como neutropenias y leucopenias. |
Country Status (11)
| Country | Link |
|---|---|
| US (1) | US20090258877A1 (es) |
| EP (1) | EP2229392A1 (es) |
| JP (1) | JP2011506364A (es) |
| AR (1) | AR069636A1 (es) |
| CA (1) | CA2708783A1 (es) |
| CL (1) | CL2008003602A1 (es) |
| PA (1) | PA8806501A1 (es) |
| PE (1) | PE20091074A1 (es) |
| TW (1) | TW200938546A (es) |
| UY (1) | UY31508A1 (es) |
| WO (1) | WO2009074259A1 (es) |
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| Publication number | Priority date | Publication date | Assignee | Title |
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| EP2314293B1 (en) | 2001-01-16 | 2017-01-04 | Vascular Therapies, LLC | Implantable device containing resorbable matrix material and rapamycin for preventing or treating vasuloproliferative diseases |
| WO2015157955A1 (en) * | 2014-04-17 | 2015-10-22 | Abbvie Inc. | Heterocyclic btk inhibit ors |
| MA52422A (fr) | 2018-02-27 | 2021-01-06 | Incyte Corp | Imidazopyrimidines et triazolopyrimidines en tant qu'inhibiteurs a2a/a2b |
| MX2020012376A (es) | 2018-05-18 | 2021-03-09 | Incyte Corp | Derivados de pirimidina fusionados como inhibidores de los receptores de adenosina a2a/a2b. |
| MA53097A (fr) | 2018-07-05 | 2021-05-12 | Incyte Corp | Dérivés de pyrazine fusionnés en tant qu'inhibiteurs d'a2a/a2b |
| TWI829857B (zh) | 2019-01-29 | 2024-01-21 | 美商英塞特公司 | 作為a2a / a2b抑制劑之吡唑并吡啶及三唑并吡啶 |
| JP2022520671A (ja) | 2019-02-08 | 2022-03-31 | フリークエンシー・セラピューティクス・インコーポレイテッド | 耳障害を治療するためのバルプロ酸化合物及びｗｎｔ作動薬 |
| CN117396490A (zh) * | 2021-05-14 | 2024-01-12 | Bm医药咨询有限公司 | 用于预防和治疗病毒感染的双环杂环化合物 |
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| Publication number | Priority date | Publication date | Assignee | Title |
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| MXPA04005510A (es) * | 2001-12-07 | 2006-02-24 | Vertex Pharma | Compuestos basados en pirimidina utiles como inhibidores de gsk-3. |
| ATE377600T1 (de) * | 2002-09-23 | 2007-11-15 | Schering Corp | Imidazopyrazine als cdk-inhibitoren |
| ATE369370T1 (de) * | 2003-10-10 | 2007-08-15 | Pfizer Prod Inc | Substituierte 2h-(1,2,4)triazolo(4,3-a)pyrazine als gsk-3-inhibitoren |
| EP1812439B2 (en) * | 2004-10-15 | 2017-12-06 | Takeda Pharmaceutical Company Limited | Kinase inhibitors |
-
2008
- 2008-12-02 PE PE2008002006A patent/PE20091074A1/es not_active Application Discontinuation
- 2008-12-03 UY UY31508A patent/UY31508A1/es not_active Application Discontinuation
- 2008-12-03 PA PA20088806501A patent/PA8806501A1/es unknown
- 2008-12-03 CL CL2008003602A patent/CL2008003602A1/es unknown
- 2008-12-04 CA CA2708783A patent/CA2708783A1/en not_active Abandoned
- 2008-12-04 JP JP2010537294A patent/JP2011506364A/ja active Pending
- 2008-12-04 EP EP08858450A patent/EP2229392A1/de not_active Withdrawn
- 2008-12-04 WO PCT/EP2008/010279 patent/WO2009074259A1/de not_active Ceased
- 2008-12-09 AR ARP080105333A patent/AR069636A1/es unknown
- 2008-12-12 US US12/334,131 patent/US20090258877A1/en not_active Abandoned
- 2008-12-12 TW TW097148327A patent/TW200938546A/zh unknown
Also Published As
| Publication number | Publication date |
|---|---|
| CA2708783A1 (en) | 2009-06-18 |
| CL2008003602A1 (es) | 2009-10-09 |
| WO2009074259A1 (de) | 2009-06-18 |
| US20090258877A1 (en) | 2009-10-15 |
| PA8806501A1 (es) | 2009-08-26 |
| JP2011506364A (ja) | 2011-03-03 |
| PE20091074A1 (es) | 2009-07-26 |
| UY31508A1 (es) | 2009-08-03 |
| TW200938546A (en) | 2009-09-16 |
| EP2229392A1 (de) | 2010-09-22 |
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