AR108388A2 - Compuestos de oxazol sustituidos con indazol como inhibidores de pi3-quinasas - Google Patents
Compuestos de oxazol sustituidos con indazol como inhibidores de pi3-quinasasInfo
- Publication number
- AR108388A2 AR108388A2 ARP170101175A ARP170101175A AR108388A2 AR 108388 A2 AR108388 A2 AR 108388A2 AR P170101175 A ARP170101175 A AR P170101175A AR P170101175 A ARP170101175 A AR P170101175A AR 108388 A2 AR108388 A2 AR 108388A2
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- optionally substituted
- independently selected
- inhibitors
- halo
- Prior art date
Links
Classifications
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- 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
- A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
- A61K31/5375—1,4-Oxazines, e.g. morpholine
- A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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- 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
- A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
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- 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
- A61K31/4965—Non-condensed pyrazines
- A61K31/497—Non-condensed pyrazines containing further heterocyclic rings
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- A—HUMAN NECESSITIES
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- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
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- 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
- A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
- A61K31/5375—1,4-Oxazines, e.g. morpholine
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
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- 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
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- C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
- C07B2200/00—Indexing scheme relating to specific properties of organic compounds
- C07B2200/13—Crystalline forms, e.g. polymorphs
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- Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
- Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
- Y02A—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
- Y02A50/00—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
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Abstract
Los compuestos son inhibidores de la actividad quinasa, en particular de la actividad de la Pl3-quinasa. Reivindicación 1: Un compuesto de fórmula (1), en la que: R¹ es un heteroarilo bicíclico de 9 ó 10 miembros, en el que el heteroarilo bicíclico de 9 ó 10 miembros contiene de uno a tres heteroátomos seleccionados de forma independiente de entre oxígeno y nitrógeno, y está sustituido opcionalmente con alquilo C₁₋₆, cicloalquilo C₃₋₆, halo, -CN o -NHSO₂R⁵, o piridinilo opcionalmente sustituido con uno o dos sustituyentes seleccionados de forma independiente de entre alquilo C₁₋₆, -OR⁶, halo y -NHSO₂R⁷; R² y R³, junto con el átomo de nitrógeno al que están fijados, están unidos para formar un heterociclilo de 6 ó 7 miembros en el que el heterociclilo de 6 ó 7 miembros contiene, opcionalmente, un átomo de oxígeno u otro átomo de nitrógeno y está opcionalmente sustituido con uno o dos sustituyentes seleccionados de forma independiente de alquilo C₁₋₆; R⁴ es hidrógeno o metilo; R⁶ es hidrógeno o alquilo C₁₋₄; y R⁵ y R⁷ son, cada uno de forma independiente, alquilo C₁₋₆ o fenilo opcionalmente sustituido con uno o dos sustituyentes seleccionados de forma independiente de halo; o una sal de los mismos.
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US17403309P | 2009-04-30 | 2009-04-30 |
Publications (1)
Publication Number | Publication Date |
---|---|
AR108388A2 true AR108388A2 (es) | 2018-08-15 |
Family
ID=42225106
Family Applications (2)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
ARP100101429A AR076435A1 (es) | 2009-04-30 | 2010-04-28 | Compuestos de indazoles sustituidos, composiciones farmaceuticas que los contienen y procesos de obtencion de los mismos |
ARP170101175A AR108388A2 (es) | 2009-04-30 | 2017-05-05 | Compuestos de oxazol sustituidos con indazol como inhibidores de pi3-quinasas |
Family Applications Before (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
ARP100101429A AR076435A1 (es) | 2009-04-30 | 2010-04-28 | Compuestos de indazoles sustituidos, composiciones farmaceuticas que los contienen y procesos de obtencion de los mismos |
Country Status (40)
Country | Link |
---|---|
US (14) | US8575162B2 (es) |
EP (3) | EP3260453B1 (es) |
JP (1) | JP5570589B2 (es) |
KR (2) | KR101679642B1 (es) |
CN (1) | CN102459253B (es) |
AR (2) | AR076435A1 (es) |
AU (1) | AU2010243613B2 (es) |
BR (1) | BRPI1016219B8 (es) |
CA (1) | CA2759476C (es) |
CL (1) | CL2011002706A1 (es) |
CO (1) | CO6390057A2 (es) |
CR (1) | CR20110603A (es) |
CY (1) | CY1119515T1 (es) |
DK (2) | DK2899191T3 (es) |
DO (1) | DOP2011000328A (es) |
EA (1) | EA021056B1 (es) |
ES (3) | ES2644724T3 (es) |
HK (2) | HK1165801A1 (es) |
HR (2) | HRP20150173T1 (es) |
HU (1) | HUE034724T2 (es) |
IL (1) | IL215803A (es) |
JO (1) | JO3025B1 (es) |
LT (1) | LT2899191T (es) |
MA (1) | MA33304B1 (es) |
ME (2) | ME02900B (es) |
MX (1) | MX2011011534A (es) |
MY (1) | MY160454A (es) |
NZ (1) | NZ596071A (es) |
PE (1) | PE20120321A1 (es) |
PL (2) | PL2424864T3 (es) |
PT (2) | PT2899191T (es) |
RS (2) | RS56433B1 (es) |
SG (2) | SG10201401881QA (es) |
SI (2) | SI2424864T1 (es) |
SM (1) | SMT201500043B (es) |
TW (3) | TWI562992B (es) |
UA (1) | UA101098C2 (es) |
UY (1) | UY32585A (es) |
WO (1) | WO2010125082A1 (es) |
ZA (1) | ZA201107878B (es) |
Families Citing this family (47)
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EP2280959B1 (en) * | 2008-06-05 | 2012-04-04 | Glaxo Group Limited | 4-amino-indazoles |
ES2445199T3 (es) | 2008-06-05 | 2014-02-28 | Glaxo Group Limited | Derivados de benzpirazol como inhibidores de PI3-quinasas |
ES2526966T3 (es) | 2008-06-05 | 2015-01-19 | Glaxo Group Limited | Compuestos novedosos |
ES2542551T3 (es) | 2009-03-09 | 2015-08-06 | Glaxo Group Limited | 4-Oxadiazol-2-il-indazoles como inhibidores de PI3 cinasas |
EA021056B1 (ru) | 2009-04-30 | 2015-03-31 | Глаксо Груп Лимитед | Оксазолзамещенные индазолы в качестве ингибиторов pi3-киназ, содержащая их фармацевтическая композиция и их применение в лечении расстройств, опосредованных ненадлежащей активностью pi3-киназ |
CN102372675B (zh) * | 2010-08-14 | 2013-12-18 | 王娜 | 6-氯-4-碘吲唑及其制备方法与应用 |
DK2614058T3 (en) | 2010-09-08 | 2015-09-28 | Glaxosmithkline Ip Dev Ltd | Polymorphs, and the salts of N- [5- [4- (5 - {[(2R, 6S) -2,6-dimethyl-4-morpholinyl] methyl} -1,3-oxazol-2-yl) -1H-indazole -6-yl] -2- (methyloxy) -3-pyridinyl] methanesulfonamide. |
US9102668B2 (en) | 2010-09-08 | 2015-08-11 | Glaxo Group Limited | Polymorphs and salts |
US9326987B2 (en) | 2010-09-08 | 2016-05-03 | Glaxo Group Limited | Indazole derivatives for use in the treatment of influenza virus infection |
GB201018124D0 (en) | 2010-10-27 | 2010-12-08 | Glaxo Group Ltd | Polymorphs and salts |
US9512111B2 (en) | 2010-11-08 | 2016-12-06 | Lycera Corporation | N-sulfonylated tetrahydroquinolines and related bicyclic compounds for inhibition of RORγ activity and the treatment of disease |
BR112014014327A2 (pt) | 2011-12-15 | 2017-06-13 | Novartis Ag | uso de inibidores da atividade ou função de pi3k |
AU2013259624B2 (en) | 2012-05-08 | 2017-10-19 | Lycera Corporation | Tetrahydro[1,8]naphthyridine sulfonamide and related compounds for use as agonists of RORy and the treatment of disease |
US9657033B2 (en) | 2012-05-08 | 2017-05-23 | Lycera Corporation | Tetrahydronaphthyridine and related bicyclic compounds for inhibition of RORγ activity and the treatment of disease |
CA2877983A1 (en) | 2012-07-16 | 2014-01-23 | Neuropore Therapies, Inc. | Di- and tri-heteroaryl derivatives as inhibitors of protein aggregation |
WO2014068070A1 (en) | 2012-10-31 | 2014-05-08 | INSERM (Institut National de la Santé et de la Recherche Médicale) | Methods for preventing antiphospholipid syndrome (aps) |
JPWO2014098232A1 (ja) * | 2012-12-21 | 2017-01-12 | 学校法人東京理科大学 | Pi3キナーゼ阻害剤を含む医薬組成物、ビタミンd受容体に作用する化合物を含む医薬組成物、凍結乾燥組成物、凍結乾燥組成物の製造方法、及び経肺投与用医薬組成物 |
CA2923995A1 (en) | 2013-10-17 | 2015-04-23 | Glaxosmithkline Intellectual Property Development Limited | Pi3k inhibitor for treatment of respiratory disease |
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