AR085607A1 - Inhibidores de la mst1 quinasa y metodos para su utilizacion - Google Patents

Inhibidores de la mst1 quinasa y metodos para su utilizacion

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Publication number
AR085607A1
AR085607A1 ARP120100691A ARP120100691A AR085607A1 AR 085607 A1 AR085607 A1 AR 085607A1 AR P120100691 A ARP120100691 A AR P120100691A AR P120100691 A ARP120100691 A AR P120100691A AR 085607 A1 AR085607 A1 AR 085607A1
Authority
AR
Argentina
Prior art keywords
independently
hydrogen
optionally substituted
halo
cyano
Prior art date
Application number
ARP120100691A
Other languages
English (en)
Inventor
David John Augeri
Jeffrey Thomas Bagdanoff
Kenneth Gordon Carson
Tamas Oravecz
John Anthony Gilleran
Simon David Peter Baugh
Marianne Carlsen
Wei He
Konstantin Salojin
Leonard Sung
Original Assignee
Lexicon Pharmaceuticals Inc
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Lexicon Pharmaceuticals Inc filed Critical Lexicon Pharmaceuticals Inc
Publication of AR085607A1 publication Critical patent/AR085607A1/es

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    • 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
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    • 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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/4353—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/4365—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system having sulfur as a ring hetero atom, e.g. ticlopidine
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    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4418—Non condensed pyridines; Hydrogenated derivatives thereof having a carbocyclic group directly attached to the heterocyclic ring, e.g. cyproheptadine
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    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/444—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
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    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/47—Quinolines; Isoquinolines
    • A61K31/472—Non-condensed isoquinolines, e.g. papaverine
    • A61K31/4725—Non-condensed isoquinolines, e.g. papaverine containing further heterocyclic rings
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    • 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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    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
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    • A61K31/551—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogen atoms, e.g. dilazep
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    • A61K31/553—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having at least one nitrogen and one oxygen as ring hetero atoms, e.g. loxapine, staurosporine
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  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Pyridine Compounds (AREA)
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Abstract

Composiciones que los comprenden y métodos de uso de los mismos, en el tratamiento, manejo o prevención de enfermedades o trastornos inflamatorios o autoinmunes.Reivindicación 1: Un compuesto de la fórmula (1) o una sal farmacéuticamente aceptables del mismo, en donde: A es arilo o heterociclo de 4 - 7 miembros; X es N o CH; Y1 e Y2 son cada uno, de manera independiente, S, N o CH, siempre que al menos uno de Y e Y2 es N o CH; cada R1 es, de manera independiente, R1A, -(R1B)nSOpR1C, -(R1B)nSOpN(R1C)2, -(R1B)nNR1CSOpR1C, -(R1B)nC(O)N(R1C)2 o -(R1B)nNR1CC(O)R1C, o hidrocarbilo C1-12 opcionalmente sustituido o heterocarbilo de 2 - 12 miembros, en el cual la sustitución opcional es con uno o más de R1A; cada R1A es, de manera independiente, amino, alcoxilo, carboxilo, ciano, halo o hidroxilo; cada R1B es, de manera independiente, hidrocarbilo C1-12 opcionalmente sustituido con uno o más de amino, alcoxilo, carboxilo, ciano, halo o hidroxilo; cada R1C es, de manera independiente, hidrógeno o hidrocarbilo C1-12 opcionalmente sustituido o heterocarbilo de 2 - 12 miembros, en el cual la sustitución opcional es con uno o más de amino, alcoxilo, carboxilo, ciano, halo o hidroxilo; R2 y R3 se toman juntos para formar un heterociclo de 5 - 7 miembros, opcionalmente sustituido con uno o más de R3A, o: R2 es hidrógeno o C1-4 alquilo; y R3 es hidrógeno o hidrocarbilo C1-12 o heterocarbilo de 2 - 12 miembros, opcionalmente sustituidos, en el cual la sustitución opcional es con uno o más de R3A; cada R3A es, de manera independiente, amino, alcoxilo, carboxilo, ciano, halo, o hidroxilo; k es 0 ó 1; m es 0 - 3; n es 0 ó 1; y p es 0 - 2; con la condición que R3 no sea hidrógeno cuando X es CH, Y1 es CH, Y2 es CH, y R2 es hidrógeno.
ARP120100691A 2011-03-04 2012-03-02 Inhibidores de la mst1 quinasa y metodos para su utilizacion AR085607A1 (es)

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EP (1) EP2681206B1 (es)
JP (1) JP5997709B2 (es)
KR (1) KR20140014205A (es)
CN (1) CN103429582A (es)
AR (1) AR085607A1 (es)
AU (1) AU2012225805B2 (es)
CA (1) CA2828578A1 (es)
ES (1) ES2639426T3 (es)
IL (1) IL227953A0 (es)
MX (1) MX2013009953A (es)
RU (1) RU2013144579A (es)
SG (1) SG193293A1 (es)
TW (1) TW201247626A (es)
WO (1) WO2012121992A1 (es)
ZA (1) ZA201306188B (es)

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ES2921576T3 (es) 2008-12-19 2022-08-29 Vertex Pharma Compuestos útiles como inhibidores de la quinasa ATR
NZ603477A (en) 2010-05-12 2014-09-26 Vertex Pharma Compounds useful as inhibitors of atr kinase
EP2568984A1 (en) * 2010-05-12 2013-03-20 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of atr kinase
US9334244B2 (en) 2010-05-12 2016-05-10 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of ATR kinase
CA2798760A1 (en) * 2010-05-12 2011-11-17 Vertex Pharmaceuticals Incorporated 2-aminopyridine derivatives useful as inhibitors of atr kinase
CN108685922A (zh) 2011-09-30 2018-10-23 沃泰克斯药物股份有限公司 用atr抑制剂治疗胰腺癌和非小细胞肺癌
CN106496173A (zh) 2011-09-30 2017-03-15 沃泰克斯药物股份有限公司 用于制备可用作atr激酶抑制剂的化合物的方法
LT2814820T (lt) * 2012-02-17 2016-10-25 University Of Cape Town Antimaliariniai agentai
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