AR080699A1 - Pirrolopirazinas como inhibidores de jak y syk - Google Patents

Pirrolopirazinas como inhibidores de jak y syk

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Publication number
AR080699A1
AR080699A1 ARP110100907A ARP110100907A AR080699A1 AR 080699 A1 AR080699 A1 AR 080699A1 AR P110100907 A ARP110100907 A AR P110100907A AR P110100907 A ARP110100907 A AR P110100907A AR 080699 A1 AR080699 A1 AR 080699A1
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AR
Argentina
Prior art keywords
lower alkyl
independently
cyano
cycloalkyl
alkoxy
Prior art date
Application number
ARP110100907A
Other languages
English (en)
Inventor
Robert Than Hendricks
Johannes Cornelius Hermann
Rama K Kondru
Yan Lou
Stephen M Lynch
Timothy D Owens
Michael Soth
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
Application filed by Hoffmann La Roche filed Critical Hoffmann La Roche
Publication of AR080699A1 publication Critical patent/AR080699A1/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
    • 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
    • A61P17/06—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
    • A61P37/04—Immunostimulants
    • 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
    • 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
    • A61P5/02—Drugs for disorders of the endocrine system of the hypothalamic hormones, e.g. TRH, GnRH, CRH, GRH, somatostatin
    • A—HUMAN NECESSITIES
    • 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)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Immunology (AREA)
  • Diabetes (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Endocrinology (AREA)
  • Pulmonology (AREA)
  • Biomedical Technology (AREA)
  • Rheumatology (AREA)
  • Dermatology (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Psychiatry (AREA)
  • Transplantation (AREA)
  • Oncology (AREA)
  • Hospice & Palliative Care (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Emergency Medicine (AREA)
  • Pain & Pain Management (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Cardiology (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Abstract

Estos compuestos inhiben JAK y SYK, resultan utiles para el tratamiento de enfermedades autoinmunologicas e inflamatorias. Reivindicacion 1: Compuesto de formula (1) en la que Y es C(R1)2(C(R1')2)m, m es 0 o 1; cada R1 es H o R1a; cada R1a es, independientemente, alquilo inferior, alcoxi inferior, fenilo, bencilo, heteroarilo, cicloalquilo, heterocicloalquilo o cicloalquil-alquilo inferior, opcionalmente sustituido con uno o más R1a', R1a' es halogeno, alquilo inferior, haloalquilo inferior, alcoxi inferior, hidroxialquilo inferior, oxo, hidroxi o ciano, cada R1' es, independientemente, H, alquilo inferior o haloalquilo inferior, R2 es, independientemente, H o R2a, R2a es, independientemente, alquilo inferior, haloalquilo inferior, alcoxi inferior, hidroxialquilo inferior, ciano, alquilo inferior, cicloalquilo o heterocicloalquilo, o R2a y R1a conjuntamente forman un anillo, opcionalmente sustituido con uno o más de entre halogeno, alquilo inferior, ciano, ciano-alquilo inferior, hidroxi, haloalquilo inferior, hidroxialquilo inferior, alcoxi inferior, alquilamino inferior o dialquilamino inferior, R3 es, independientemente, H o R3a, R3a es, independientemente, alquilo inferior, haloalquilo inferior, alcoxi inferior, hidroxialquilo inferior, ciano-alquilo inferior, C(=O)R3a' o S(=O)2R3a', cada R3a' es, independientemente, H o alquilo inferior, Q es H, halogeno, hidroxi, ciano o Q', Q' es alquilo inferior, alquenilo inferior, alquinilo inferior, cicloalquilo, fenilo, cicloalquenilo, heterocicloalquilo o heteroarilo, opcionalmente sustituidos con uno o más Qa, Qa es Qb o Qc, Qb es halogeno, oxo, hidroxi, -CN, -SCH3, -S(O)2CH3, o -S(=O)CH3, Qc es Qd o Qe; o dos Qa conjuntamente forman un sistema de anillos bicíclico, opcionalmente sustituido con uno o más Qb o Qc; Qd es -O(Qe), -S(=O)2(Qe), -C(=O)N(Qe)2, -S(O)2(Qe), -C(=O)(Qe), -C(=O)O(Qe), -N(Qe)2, N(Qe)C(=O)(Qe), -N(Qe)C(=O)O(Qe), o -N(Qe)C(=O)N(Qe)2; cada Qe es, independientemente, H o Qe', cada Qe' es, independientemente, alquilo inferior, alcoxi inferior, fenilo, bencilo, heteroarilo, cicloalquilo, heterocicloalquilo o cicloalquil-alquilo inferior, opcionalmente sustituido con uno o más Qf, Qf es Qg o Qh, Qg es halogeno, hidroxi, ciano, oxo, o C(=O)(Qh), Qh es alquilo inferior, haloalquilo inferior, alcoxi inferior, amino, fenilo, bencilo, cicloalquilo, heterocicloalquilo o heteroarilo, opcionalmente sustituidos con uno o más Qi, y Qi es halogeno, hidroxi, ciano, alquilo inferior, haloalquilo inferior o alcoxi inferior, o una sal farmacéuticamente aceptable de los mismos.
ARP110100907A 2010-03-22 2011-03-21 Pirrolopirazinas como inhibidores de jak y syk AR080699A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US31599910P 2010-03-22 2010-03-22

Publications (1)

Publication Number Publication Date
AR080699A1 true AR080699A1 (es) 2012-05-02

Family

ID=43983677

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP110100907A AR080699A1 (es) 2010-03-22 2011-03-21 Pirrolopirazinas como inhibidores de jak y syk

Country Status (12)

Country Link
US (1) US8481541B2 (es)
EP (1) EP2550274A1 (es)
JP (1) JP5667692B2 (es)
KR (1) KR20130004342A (es)
CN (1) CN102812029A (es)
AR (1) AR080699A1 (es)
BR (1) BR112012023752A2 (es)
CA (1) CA2786402A1 (es)
MX (1) MX2012010610A (es)
RU (1) RU2012142550A (es)
TW (1) TW201136936A (es)
WO (1) WO2011117160A1 (es)

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BR112012029437A2 (pt) * 2010-05-20 2017-03-07 F Hoffmann - La Roche Ag derivados de pirrolo[2,3-b]pirazina-7-carboxamida e seu uso como inibidores de jak e syk
EP2571881A1 (en) * 2010-05-20 2013-03-27 F.Hoffmann-La Roche Ag Pyrrolopyrazine derivatives as syk and jak inhibitors
KR20140074912A (ko) 2011-09-01 2014-06-18 에프. 호프만-라 로슈 아게 피롤로피라진 키나아제 억제제
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KR20140108594A (ko) 2012-01-10 2014-09-11 에프. 호프만-라 로슈 아게 피리다진 아미드 화합물 및 syk 저해제로서의 이의 용도
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Also Published As

Publication number Publication date
JP5667692B2 (ja) 2015-02-12
CA2786402A1 (en) 2011-09-29
MX2012010610A (es) 2012-10-03
EP2550274A1 (en) 2013-01-30
BR112012023752A2 (pt) 2019-09-24
KR20130004342A (ko) 2013-01-09
RU2012142550A (ru) 2014-04-27
US8481541B2 (en) 2013-07-09
WO2011117160A1 (en) 2011-09-29
CN102812029A (zh) 2012-12-05
JP2013522337A (ja) 2013-06-13
US20110230414A1 (en) 2011-09-22
TW201136936A (en) 2011-11-01

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