AR081203A1 - Pirrolopirazinas como inhibidores de quinasas - Google Patents

Pirrolopirazinas como inhibidores de quinasas

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Publication number
AR081203A1
AR081203A1 ARP110101697A ARP110101697A AR081203A1 AR 081203 A1 AR081203 A1 AR 081203A1 AR P110101697 A ARP110101697 A AR P110101697A AR P110101697 A ARP110101697 A AR P110101697A AR 081203 A1 AR081203 A1 AR 081203A1
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AR
Argentina
Prior art keywords
heterocycloalkyl
cycloalkyl
optionally substituted
independently
hydroxy
Prior art date
Application number
ARP110101697A
Other languages
English (en)
Inventor
Stephen M Lynch
Timothy D Owens
Michael Soth
Calvin Wesley Yee
Rama K Kondru
Yan Lou
Robert Than Hendricks
Johannes Cornelius Hermann
Original Assignee
Hoffmann La Roche
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Filing date
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Application filed by Hoffmann La Roche filed Critical Hoffmann La Roche
Publication of AR081203A1 publication Critical patent/AR081203A1/es

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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
    • 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
    • A61K31/495—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
    • 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
    • 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
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    • 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
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    • 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
    • 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
    • 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
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A61P37/02—Immunomodulators
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/08—Antiallergic agents
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    • 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
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system

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

Abstract

Composiciones farmacéuticas que 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 R1 es H u OH; R2 es fenilo, heterocicloalquilo, heteroarilo o cicloalquilo, cada uno de ellos está opcionalmente sustituido por uno o más R2'; cada R2' es con independencia hidroxi, halógeno, oxo, alquilo inferior, alquenilo inferior, alquinilo inferior, halo-alquilo inferior, alcoxi inferior, haloalcoxi inferior, hidroxialquilo inferior, amino, (alquilo inferior)-amino, di(alquilo inferior)-amino, ciano, cianoalquilo inferior, cicloalquilo, heterocicloalquilo, C(=O)R3 o S(=O)2R3; cada R3 es con independencia OH, cicloalquilo o alquilo inferior; Q es Q2, Q3 o Q4; Q2 es heterocicloalquilo, cicloalquilo, cicloalquenilo, heterocicloalquilo, fenilo, heteroarilo, biarilo o hetero-biarilo, opcionalmente sustituidos por uno o más Q2a; Q2a es Q2b o Q2c; Q2b es halógeno, oxo, hidroxi, -CN, -SCH3, -S(O)2CH3 o -S(=O)CH3; Q2c es Q2d o Q2e; o dos Q2a juntos forman un sistema de anillo bicíclico, opcionalmente sustituido por uno o más Q2b o Q2c; Q2d es -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, haloalquilo inferior, cicloalquilo, cicloalquenilo, heterocicloalquilo o heteroarilo, opcionalmente sustituidos por uno o más Q2f; Q2f es Q2g o Q2h; Q2g es halógeno, hidroxi, ciano, oxo o -C(=O)(Q2h); Q2h es alquilo inferior, haloalquilo inferior, alcoxi inferior, amino, fenilo, bencilo, cicloalquilo, heterocicloalquilo o heteroarilo, opcionalmente sustituidos por uno o más Q2i; Q2i es halógeno, hidroxi, ciano, alquilo inferior, haloalquilo inferior o alcoxi 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; m es el número 0, 1 o 2; Q3b es H; Q3c es alquilo inferior, haloalquilo inferior, fenilo, cicloalquilo, heterocicloalquilo o heteroarilo, opcionalmente sustituidos por uno o más Q3d; cada Q3d es con independencia Q3e o Q3f; Q3e es halógeno o hidroxi; Q3f es alquilo inferior, alcoxi inferior, haloalquilo inferior, fenilo, cicloalquilo, heterocicloalquilo o heteroarilo, opcionalmente sustituidos por uno o más Q3g; o dos Q3f juntos forman un cicloalquilo, heterocicloalquilo o heteroarilo, opcionalmente sustituidos por uno o más Q3g; cada Q3g es con independencia halógeno, hidroxi, alquilo inferior, hidroxialquilo inferior, haloalquilo inferior, amido 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; Q4c es 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; y cada Q4f es con independencia hidroxi, halógeno, alquilo inferior, alquenilo inferior, oxo, haloalquilo inferior, alcoxi inferior, hidroxialquilo inferior o amino; o una sal farmacéuticamente aceptable del mismo.
ARP110101697A 2010-05-20 2011-05-18 Pirrolopirazinas como inhibidores de quinasas AR081203A1 (es)

Applications Claiming Priority (2)

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US34650210P 2010-05-20 2010-05-20
US201161475286P 2011-04-14 2011-04-14

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AR081203A1 true AR081203A1 (es) 2012-07-04

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Country Status (11)

Country Link
US (1) US8329699B2 (es)
EP (1) EP2571881A1 (es)
JP (1) JP2013526558A (es)
KR (1) KR20130083387A (es)
CN (1) CN102906095A (es)
AR (1) AR081203A1 (es)
CA (1) CA2798970A1 (es)
MX (1) MX2012013194A (es)
RU (1) RU2012152354A (es)
TW (1) TWI496785B (es)
WO (1) WO2011144584A1 (es)

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RU2012152354A (ru) 2014-06-27
TWI496785B (zh) 2015-08-21
US8329699B2 (en) 2012-12-11
MX2012013194A (es) 2013-01-22
US20110288097A1 (en) 2011-11-24
KR20130083387A (ko) 2013-07-22
EP2571881A1 (en) 2013-03-27
TW201204730A (en) 2012-02-01

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