AR070467A1 - Inhibidores de quinasa de pirrolopirazina - Google Patents

Inhibidores de quinasa de pirrolopirazina

Info

Publication number
AR070467A1
AR070467A1 ARP090100620A ARP090100620A AR070467A1 AR 070467 A1 AR070467 A1 AR 070467A1 AR P090100620 A ARP090100620 A AR P090100620A AR P090100620 A ARP090100620 A AR P090100620A AR 070467 A1 AR070467 A1 AR 070467A1
Authority
AR
Argentina
Prior art keywords
phenyl
lower alkyl
haloalkyl
heterocycloalkyl
heteroaryl
Prior art date
Application number
ARP090100620A
Other languages
English (en)
Inventor
Robert Than Hendricks
Bois Daisy Joe Du
Timothy D Owens
David Bernard Smith
Yan Lou
Rama K Kondru
Todd Richard Elworthy
Michael Soth
Johannes Cornelius Hermann
Jaehyeon Park
Original Assignee
Hoffmann La Roche
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
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=40514045&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=AR070467(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Hoffmann La Roche filed Critical Hoffmann La Roche
Publication of AR070467A1 publication Critical patent/AR070467A1/es

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Classifications

    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/06—Antiasthmatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/02—Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/06—Antipsoriatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • 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
    • A61P37/00—Drugs for immunological or allergic disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/08—Antiallergic agents
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00—Drugs for disorders of the endocrine system
    • A61P5/14—Drugs for disorders of the endocrine system of the thyroid hormones, e.g. T3, T4

Landscapes

  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • General Chemical & Material Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Public Health (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Immunology (AREA)
  • Diabetes (AREA)
  • Dermatology (AREA)
  • Pulmonology (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Hematology (AREA)
  • Rheumatology (AREA)
  • Endocrinology (AREA)
  • Hospice & Palliative Care (AREA)
  • Emergency Medicine (AREA)
  • Pain & Pain Management (AREA)
  • Obesity (AREA)
  • Transplantation (AREA)
  • Psychiatry (AREA)
  • Oncology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Abstract

Inhiben la JAK y la SYK y son utiles para el tratamiento de enfermedades inflamatorias y autoinmunes. Reivindicacion 1: Un compuesto de la formula 1 en la que: R es R1, R2, R3 o R4; R1 es alquilo inferior, alcoxi inferior, fenilo, bencilo, heteroarilo, cicloalquilo, heterocicloalquilo o cicloalquilalquilo, opcionalmente sustituido por uno o más R1a; R1a es R1b o R1c; R1b es halogeno, oxo, hidroxi o -CN; R1c es -C(=O)O(R1f), -C(=O)(CH2)m(R1e), -O(CH2)m(R1e), -S(R1f), -S(O)2(R1f) o -S(=O)(R1f), alquilo inferior, alcoxi inferior, amino, amido, haloalquilo inferior, fenilo, heteroarilo, cicloalquilo, heterocicloalquilo, cicloalquiloxi o heterocicloalquiloxi opcionalmente sustituido por uno o más R1d; R1d es H, halogeno, hidroxi, alquilo inferior, amino, alcoxi inferior o haloalquilo inferior; R1e es H, alquilo inferior, alcoxi inferior, ciano, haloalquilo inferior, fenilo, heteroarilo, cicloalquilo o heterocicloalquilo; R1f es H, alquilo inferior, haloalquilo inferior, fenilo, heteroarilo, cicloalquilo o heterocicloalquilo; m es el numero 0, 1 o 2; R2 es N(R2a)2; cada R2a es con independencia H o R2b; cada R2b es con independencia alquilo inferior, fenilo, heteroarilo, cicloalquilo, heterocicloalquilo o heterocicloalquil-alquileno, opcionalmente sustituido por uno o más R2c; R2c es R2d o R2e; R2d es halogeno, oxo o hidroxi; R2e es -N(R2g)2, -C(=O)(R2g), -C(=O)O(R2g), -C(=O)N(R2g)2, -N(R2g)C(=O)(R2g), -S(=O)2(R2g), -S(O)2N(R2g)2, alquilo inferior, alcoxi inferior, haloalquilo inferior, fenilo, heteroarilo, heteroariloxi, cicloalquilo o heterocicloalquilo, opcionalmente sustituido por uno o más R2f; cada R2f es con independencia H, halogeno, alquilo inferior, alcoxi inferior, haloalquilo inferior; cada R2g es con independencia H, alquilo inferior, alcoxi inferior, haloalquilo inferior o fenilo; R3 es -C(=O)R3a; R3a es alquilo inferior, alcoxi inferior, fenilo o N(R3b)2; cada R3b es con independencia H o alquilo inferior; R4 es -O(R4a); R4a es H o R4b; R4b es alquilo inferior, fenilo, bencilo, haloalquilo inferior, cicloalquilo, heterocicloalquilo, heteroarilo, opcionalmente sustituido por uno o más R4c; R4c es halogeno, hidroxi, alquilo inferior, haloalquilo inferior o alcoxi inferior; Q4 es Q4a o Q4b; Q4a es H, hidroxi, ciano o halogeno; Q4b es alquilo inferior, alquenilo inferior, alquinilo inferior, hidroxialquilo inferior, amino o haloalquilo inferior, opcionalmente sustituido por uno o más Q4c; Q4c es Q4d o Q4e; cada Q4d es con independencia halogeno, hidroxi o ciano; cada Q4e es con independencia alquilo inferior, haloalquilo inferior, alcoxi inferior, amino, cicloalquilo, fenilo, heterocicloalquilo o heteroarilo, opcionalmente sustituido por uno o más Q4f; cada Q4f es con independencia hidroxi, halogeno, alquilo inferior, alquenilo inferior, oxo, haloalquilo inferior, alcoxi inferior, hidroxialquilo inferior o amino; con la condicion de que cuando R es R4, R4 es -O(R4a), R4a es H y Q4 es Q4a, entonces Q4a no sea H; o una sal farmacéuticamente aceptable del mismo.
ARP090100620A 2008-02-25 2009-02-23 Inhibidores de quinasa de pirrolopirazina AR070467A1 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US3103508P 2008-02-25 2008-02-25
US14651409P 2009-01-22 2009-01-22

Publications (1)

Publication Number Publication Date
AR070467A1 true AR070467A1 (es) 2010-04-07

Family

ID=40514045

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP090100620A AR070467A1 (es) 2008-02-25 2009-02-23 Inhibidores de quinasa de pirrolopirazina

Country Status (18)

Country Link
US (1) US8119636B2 (es)
EP (1) EP2247593B1 (es)
JP (1) JP5284377B2 (es)
KR (1) KR20100114095A (es)
CN (1) CN101952296B (es)
AR (1) AR070467A1 (es)
AT (1) ATE519763T1 (es)
AU (1) AU2009218609A1 (es)
BR (1) BRPI0907928A2 (es)
CA (1) CA2713718A1 (es)
CL (1) CL2009000405A1 (es)
IL (1) IL206818A0 (es)
MX (1) MX2010009023A (es)
PE (1) PE20091738A1 (es)
RU (1) RU2010139284A (es)
TW (1) TW200942543A (es)
WO (1) WO2009106444A1 (es)
ZA (1) ZA201004942B (es)

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JP2015502925A (ja) 2011-11-09 2015-01-29 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Ｖｅｒｔｅｘ Ｐｈａｒｍａｃｅｕｔｉｃａｌｓ Ｉｎｃｏｒｐｏｒａｔｅｄ Ａｔｒキナーゼの阻害剤として有用なピラジン化合物
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WO2014062604A1 (en) 2012-10-16 2014-04-24 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of atr kinase
SI2941432T1 (en) 2012-12-07 2018-07-31 Vertex Pharmaceuticals Incorporated 2-AMINO-6-FLUORO-N- (5-FLUORO-4- (4- (4- (OXETHAN-3-YL) PIPERAZIN-1-CARBONYL) PIPERIDIN-1-YLIPRIDIN-3-YL) 1,5 ALFA) PYRIMIDINE-3-CARBOXAMIDE AS ATR KINAZE INHIBITOR
WO2014143240A1 (en) 2013-03-15 2014-09-18 Vertex Pharmaceuticals Incorporated Fused pyrazolopyrimidine derivatives useful as inhibitors of atr kinase
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RU2720408C2 (ru) 2013-12-06 2020-04-29 Вертекс Фармасьютикалз Инкорпорейтед Способ получения ингибиторов atr киназы (варианты)
RU2719583C2 (ru) 2014-06-05 2020-04-21 Вертекс Фармасьютикалз Инкорпорейтед Радиоактивно меченные производные 2-амино-6-фтор-n-[5-фтор-пиридин-3-ил]-пиразоло[1, 5-а]пиримидин-3-карбоксамида, используемые в качестве ингибитора atr киназы, препараты на основе этого соединения и его различные твердые формы
CA2950780C (en) 2014-06-17 2023-05-16 Vertex Pharmaceuticals Incorporated Method for treating cancer using a combination of chk1 and atr inhibitors
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Publication number Publication date
MX2010009023A (es) 2010-09-07
JP2011513263A (ja) 2011-04-28
JP5284377B2 (ja) 2013-09-11
ZA201004942B (en) 2011-12-28
WO2009106444A1 (en) 2009-09-03
ATE519763T1 (de) 2011-08-15
PE20091738A1 (es) 2009-11-13
IL206818A0 (en) 2010-12-30
CN101952296B (zh) 2013-08-21
EP2247593A1 (en) 2010-11-10
US8119636B2 (en) 2012-02-21
CA2713718A1 (en) 2009-09-03
CL2009000405A1 (es) 2010-02-26
AU2009218609A1 (en) 2009-09-03
EP2247593B1 (en) 2011-08-10
KR20100114095A (ko) 2010-10-22
TW200942543A (en) 2009-10-16
CN101952296A (zh) 2011-01-19
US20090215785A1 (en) 2009-08-27
BRPI0907928A2 (pt) 2015-07-28
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