AR081204A1 - Pirrolopirazinas como inhibidores de quinasas - Google Patents

Pirrolopirazinas como inhibidores de quinasas

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Publication number
AR081204A1
AR081204A1 ARP110101698A ARP110101698A AR081204A1 AR 081204 A1 AR081204 A1 AR 081204A1 AR P110101698 A ARP110101698 A AR P110101698A AR P110101698 A ARP110101698 A AR P110101698A AR 081204 A1 AR081204 A1 AR 081204A1
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Argentina
Prior art keywords
independently
pyrrolo
pyrazine
carboxylic acid
hydroxy
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ARP110101698A
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English (en)
Inventor
Robert Than Hendricks
Johannes Cornelius Hermann
Rama K Kondru
Yan Lou
Stephen M Lynch
Timothy D Owens
Michael Soth
Calvin Wesley Yee
Saul Jaime-Figueroa
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Hoffmann La Roche
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Publication of AR081204A1 publication Critical patent/AR081204A1/es

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    • 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
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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
    • A61K31/4985—Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
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    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00

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  • Orthopedic Medicine & Surgery (AREA)
  • Hospice & Palliative Care (AREA)
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  • Obesity (AREA)
  • Pain & Pain Management (AREA)
  • Transplantation (AREA)
  • Emergency Medicine (AREA)
  • Epidemiology (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

Estos compuestos inhiben la JAK y la SYK y son útiles para el tratamiento de enfermedades autoinmunes e inflamatorias. Reivindicación 1: Un compuesto de la fórmula (1) en la que R es H, ciano, alquilo inferior, R' o *-(R1a)(R1b)(R1c); R' es cicloalquilo, heterocicloalquilo, heteroarilo o fenilo, cada uno está opcionalmente sustituido por uno o más R"; cada R" es con independencia halógeno, hidroxi, ciano, alquilo inferior, haloalquilo interior, alcoxi inferior, hidroxialquilo inferior, cicloalquilo, C(=O)R"' o S(=O)2R'''; cada R"' es con independencia OH o alquilo inferior; R1a y R1b con independencia entre sí son H, hidroxi, halógeno, alquilo inferior, alquenilo inferior, alquinilo inferior, haloalquilo inferior, alcoxi inferior, haloalcoxi inferior, hidroxialquilo inferior, amino, (alquilo inferior)-amino, di(alquilo inferior)-amino, ciano, C(=O)R''', S(=O)2R''' o CH2S(=O)2R"'; R1c es fenilo, cicloalquilo, heterocicloalquilo o heteroarilo, opcionalmente sustituidos por uno o más R1d; cada R1d es con independencia hidroxi, halógeno, alquilo inferior, hidroxialquilo inferior, halógeno-alquilo inferior o alcoxi inferior; R2 es H, hidroxi-alquilo inferior, haloalquilo inferior o alquilo inferior; R3 es H, hidroxi, ciano, ciano-alquilo inferior o R3'; cada R3' es con independencia alquilo inferior, hidroxialquilo inferior, alcoxi inferior, haloalquilo inferior, haloalcoxi inferior, fenil-alquilo inferior, cicloalquilo o cicloalquil-alquilo inferior, cada uno de ellos está opcionalmente sustituido por uno o más R3"; cada R3" es con independencia alquilo inferior, halógeno, hidroxi, alcoxi inferior, haloalquilo inferior, hidroxialquilo inferior, oxo, amino, ciano, ciano-alquilo inferior, S(=O)2R3''', C(=O)R3''', cicloalquilo, heterocicloalquilo, heteroarilo o heterocicloalquenilo; cada R3''' es con independencia H, hidroxi o alquilo inferior; Q es Q2, Q3 o Q4; Q2 es heterocicloalquilo, cicloalquilo, cicloalquenilo, heterocicloalquilo fenilo, heteroarilo, biarilo o heterobiarilo, opcionalmente sustituidos por uno o más Q2a; Q2a es Q2b o Q2c; cada Q2b es con independencia halógeno, oxo, hidroxi, -CN, -SCH3, -S(O)2CH3 o -S(=O)CH3; cada Q2c es con independencia Q2d o Q2e; o dos Q2a juntos forman un sistema de anillo bicíclico, opcionalmente sustituido por uno o más Q2b o Q2c; cada Q2d es con independencia -O(Q2e), -S(=O)2(Q2e), -C(=O)N(Q2e)2, -S(O)2(Q2e), -C(=O)(Q2e), -C(=O)O(Q2e), -N(Q2e)C(=O)(Q2e), -N(Q2e)C(=O)O(Q2e) o -N(Q2e)C(=O)N(Q2e)2; cada Q2e es con independencia H o Q2e'; cada Q2e' es con independencia alquilo inferior, fenilo, bencilo, 5, 6,7,8-tetrahidro-naftaleno, haloalquilo inferior, alcoxi inferior, cicloalquilo, cicloalquenilo, heterocicloalquilo, heterocicloalquilo espirocíclico o heteroarilo, opcionalmente sustituidos por uno o más Q2f; cada Q2f es con independencia Q2g o Q2h; cada Q2g es con independencia halógeno, hidroxi, ciano, oxo, -S(=O)2(Q2i'), -S(=O)2N(Q2i')2, -C(=O)OH, C(=O)N(Q2i')2 o -C(=O)(Q2i'); cada Q2h es con independencia alquilo inferior, alquenilo inferior, haloalquilo inferior, alcoxi inferior, amino, fenilo, bencilo, cicloalquilo, heterocicloalquilo o heteroarilo, opcionalmente sustituidos por uno o más Q2i; y cada Q2i es con independencia halógeno, hidroxi, ciano, alquilo inferior, haloalquilo inferior o alcoxi inferior; cada Q2i' es con independencia H o alquilo inferior; Q3 es -O-Q3a, -S-Q3a, -C(=O)(Q3a), -O(CH2)mC(=O)(Q3a), -S(=O)(Q3a), -S(=O)2(Q3a), -N(Q3a)2, -N(Q3a)S(=O)2(Q3a), -N(Q3a)C(=O)(Q3a), -C(=O)N(Q3a)2, N(Q3a)C(=O)N(Q3a)2 o -N(Q3a)(CH2)mC(=O)N(Q3a)2; cada Q3a es con independencia Q3b o Q3c; cada m es con independencia el número 0, 1 o 2; cada Q3b es con independencia H; cada Q3c es con independencia alquilo inferior, haloalquilo inferior, fenilo, 5, 6,7,8-tetrahidro-naftaleno, naftaleno, 2,2-dimetil-2,3-dihidro-benzofuranilo, indanilo, indenilo, indolilo, cicloalquilo, heterocicloalquilo o heteroarilo, opcionalmente sustituidos por uno o más Q3d; y cada Q3d es con independencia Q3e o Q3f; cada Q3e es con independencia halógeno, oxo, ciano, hidroxi, -NHS(=O)2(Q3f), -NHC(=O)(Q3f), NHC(=O)N(Q3f)2 o N(Q3f)2; cada Q3f es con independencia H o Q3f'; cada Q3f' es con independencia alquilo inferior, alcoxi inferior, haloalquilo inferior, fenilo, bencilo, cicloalquilo, heterocicloalquilo o heteroarilo, opcionalmente sustituidos por uno o más Q3g; y cada Q3g es con independencia halógeno, hidroxi, alquilo inferior, hidroxialquilo inferior, haloalquilo inferior o alcoxi inferior; Q4 es Q4a o Q4b; Q4a es hidroxi, halógeno o ciano; Q4b es alquilo inferior, alcoxi inferior, alquinilo inferior, alquenilo inferior, hidroxialquilo inferior, amino o haloalquilo inferior, opcionalmente sustituidos por uno o más Q4c; cada Q4c es con independencia Q4d o Q4e; cada Q4d es con independencia halógeno, hidroxi o ciano; cada Q4e es con independencia alquilo inferior, haloalquilo inferior, alcoxi inferior, amino, cicloalquilo, fenilo, heterocicloalquilo o heteroarilo, opcionalmente sustituidos por uno o más Q4f; cada Q4f es con independencia hidroxi, halógeno, alquilo inferior, alquenilo inferior, oxo, haloalquilo inferior, alcoxi inferior, hidroxialquilo inferior o amino; con la condición de que el compuesto de la fórmula (1) no sea la isopropilamida del ácido 2-tiofen-2-il-5H-pirrolo[2,3-b]-pirazina-7-carboxílico, (4-hidroxi-3,3-dimetil-butil)-amida del ácido 2-ciclopropil-5H-pirrolo[2,3-b]pirazina-7-carboxílico, 2-[1-(7-isopropilcarbamoil-5H-pirrolo[2,3-b]-pirazin-2-il)-piperidin-3-il]-propionato de tert-butilo, tert-butilamida del ácido 2-ciclopropil-5H-pirrolo[2,3-b]-pirazina-7-carboxílico, isopropilamida del ácido 2-ciclo-hexil-5H-pirrolo[2,3-b]pirazina-7-carboxílico, isopropilamida del ácido 2-ciclohex-1-enil-5H-pirrolo[2,3-b]pirazina-7-carboxílico, isopropilamida del ácido 2-cloro-5H-pirrolo[2,3-b]pirazina-7-carboxílico, isopropilamida del ácido 2-iso-propil-5H-pirrolo[2,3-b]pirazina-7-carboxílico, isopropilamida del ácido 2-isopropenil-5H-pirrolo[2,3-b]pirazina-7-carboxílico, isopropilamida del ácido 2-(ciclopentil-metil-amino)-5H-pirrolo[2,3-b]pirazina-7-carboxílico, [1-(7-isopropilcarbamoil-5H-pirrolo[2,3-b]pirazin-2-il)-piperidin-3-il]-metil-carbamato de tert-butilo, isopropilamida del ácido 2-(3-metilamino-piperidin-1-il)-5H-pirrolo[2,3-b]pirazina-7-carboxílico, isopropilamida del ácido 2-(ciclopentil-metil-amino)-5H-pirrolo[2,3-b]pirazina-7-carboxílico, isopropilamida del ácido 2-cloro-5H-pirrolo[2,3-b]pirazina-7-carboxílico, isopropilamida del ácido 2-isopropenil-5H-pirrolo [2,3-b]-pirazina-7-carboxílico, isopropilamida del ácido 2-isopropil-5H-pirrolo[2,3-b]pirazina-7-carboxílico, isopropilamida del ácido 2-ciclohex-1-enil-5H-pirrolo[2,3-b]pirazina-7-carboxílico, (3-hidroxi-2,2-dimetil-propil)-amida del ácido 2-ciclopropil-5H-pirrolo[2,3b]pirazina-7-carboxílico, ((S)2-hidroxi-1,2-dimetil-propil)-amida del ácido 2-ciclopropil-5H-pirrolo[2,3-b]pirazina-7-carboxílico, tert-butilamida del ácido 2-ciclopropil-5H-pirrolo[2,3-b]pirazina-7-carboxílico, isopropilamida del ácido 2-ciclohexil-5H-pirrolo[2,3-b]-pirazina-7-carboxílico, (3-hidroxi-2,2dimetil-propil)-amida del ácido 2-tiofen-2-il-5H-pirrolo[2,3-b]pirazina-7-carboxílico, [1-(7-isopropilcarbamoil-5H-pirrolo[2,3-b]-pirazin-2-il)-piperidin-3-il]-metil-carbamato de tert-butilo; isopropilamida del ácido 2-(3-metilamino-piperidin-1-il)-5H-pirrolo[2,3-b]pirazina-7-carboxílico, compuesto con ácido trifluoracético; [1-(7-isopropilcarbamoil-5H-pirrolo [2,3-b]pirazin-2-il)-piperidin-3-il]-metil-carbamato de tert-butilo o isopropilamida del ácido 2-(3-metilamino-piperidin-1-il)-5H-pirrolo[2,3-b]pirazina-7-carboxílico, compuesto con ácido trifluoracético; o una sal farmacéuticamente aceptable del mismo.
ARP110101698A 2010-05-20 2011-05-18 Pirrolopirazinas como inhibidores de quinasas AR081204A1 (es)

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US34650310P 2010-05-20 2010-05-20
US201161475281P 2011-04-14 2011-04-14

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AR081204A1 true AR081204A1 (es) 2012-07-04

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US (2) US20110288067A1 (es)
EP (1) EP2571880A1 (es)
JP (1) JP2013529204A (es)
KR (1) KR20130083386A (es)
CN (1) CN103003281A (es)
AR (1) AR081204A1 (es)
BR (1) BR112012029437A2 (es)
CA (1) CA2799904A1 (es)
MX (1) MX2012013378A (es)
RU (1) RU2012152352A (es)
WO (1) WO2011144585A1 (es)

Families Citing this family (59)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
PT3354650T (pt) 2008-12-19 2022-06-20 Vertex Pharma Compostos úteis como inibidores da cinase atr
EP2569286B1 (en) 2010-05-12 2014-08-20 Vertex Pharmaceuticals Inc. Compounds useful as inhibitors of atr kinase
MX2012013081A (es) 2010-05-12 2013-05-09 Vertex Pharma Compuestos utiles como inhibidores de cinasa atr.
CN102947272A (zh) 2010-05-12 2013-02-27 沃泰克斯药物股份有限公司 用作atr激酶抑制剂的2-氨基吡啶衍生物
JP2013526540A (ja) 2010-05-12 2013-06-24 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 Ａｔｒキナーゼ阻害剤として有用な化合物
EP2568984A1 (en) 2010-05-12 2013-03-20 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of atr kinase
EP2569289A1 (en) 2010-05-12 2013-03-20 Vertex Pharmaceuticals Incorporated Pyrazines useful as inhibitors of atr kinase
US8623869B2 (en) 2010-06-23 2014-01-07 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of ATR kinase
MX2013011450A (es) 2011-04-05 2014-02-03 Vertex Pharma Compuestos de aminopirazina utiles como inhibidores de la cinasa ataxia telangiectasia mutada y rad3 relacionados (atr).
CN103502249A (zh) 2011-05-17 2014-01-08 普林斯匹亚生物制药公司 作为酪氨酸激酶抑制剂的氮杂吲哚衍生物
EP2723745A1 (en) 2011-06-22 2014-04-30 Vertex Pharmaceuticals Inc. Compounds useful as inhibitors of atr kinase
JP2014522818A (ja) * 2011-06-22 2014-09-08 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 Ａｔｒキナーゼ阻害剤として有用な化合物
WO2012178125A1 (en) 2011-06-22 2012-12-27 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of atr kinase
BR112014004569A2 (pt) * 2011-09-01 2017-06-13 F. Hoffmann-La Roche Ag composto da fórmula i, métodos para tratar condição inflamatória, artrite reumatoide, asma e distúrbio imune, composição farmacêutica e uso do composto
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CA2799904A1 (en) 2011-11-24
CN103003281A (zh) 2013-03-27
US20110288067A1 (en) 2011-11-24
KR20130083386A (ko) 2013-07-22
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BR112012029437A2 (pt) 2017-03-07
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